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      News & Perspective Drugs & Diseases CME & Education Academy Video Decision Point
      Drugs & Diseases

      alpelisib (Rx)

      Brand and Other Names:Piqray, Vijoice
      • Print

      Dosing & Uses

      AdultPediatricGeriatric

      Dosage Forms & Strengths

      tablet (Piqray)

      • 50mg
      • 150mg
      • 200mg

      tablet (Vijoice)

      • 50mg
      • 125mg
      • 200mg

      Breast Cancer

      Piqray only

      Kinase inhibitor indicated in combination with fulvestrant for treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer following progression on or after an endocrine-based regimen

      Alpelisib 300 mg PO qDay AND

      Fulvestrant 500 mg IM on Days 1, 15, and 29, and once monthly thereafter

      Continue treatment until disease progression or unacceptable toxicity occurs

      Refer to the full prescribing information for fulvestrant

      PIK3CA-Related Overgrowth Spectrum

      Vijoice only

      Indicated for patients aged ≥2 years with severe manifestations of PIK3CA-related overgrowth spectrum (PROS) who require systemic therapy

      250 mg PO qDay

      Continue until disease progression or unacceptable toxicity

      Dosage Modifications

      Breast cancer dose reduction recommendations

      • First-dose reduction: 250 mg PO qDay
      • Second-dose reduction: 200 mg PO qDay
      • Only 1 dose reduction permitted for pancreatitis
      • If dose reduction <200 mg qDay required, discontinue treatment

      PROS dose reduction recommendations

      • Adults
        • First-dose reduction: 125 mg PO qDay
        • Second-dose reduction: 50 mg PO qDay; discontinue if 50 mg/day not tolerated

      Hyperglycemia

      • Monitor by using only fasting glucose (FG) values (fasting plasma glucose [FPG] or fasting blood glucose)
      • Initiate or adjust applicable antihyperglycemic medications, including metformin, SGLT2 inhibitors, or insulin sensitizers (eg, thiazolidinediones, dipeptidyl peptidase-4 inhibitors)
      • Metformin dose was recommended in SOLAR-1 trial: Initiate metformin 500 mg PO qDay; may increase to 500 mg BID based on tolerability, followed by 500 mg with breakfast, and 1,000 mg with dinner, followed by further increase to 1,000 mg BID if needed
      • May use insulin for 1-2 days until hyperglycemia resolves; may not be necessary in most drug-induced hyperglycemia, given short half-life of alpelisib and glucose levels normalizing after dose interruption
      • Grade 1
        • FG >ULN to 160mg/dL OR >ULN to 8.9 mmol/L
        • No dosage adjustment required
        • Initiate/intensify antidiabetic therapy
      • Grade 2
        • FG >160-250 mg/dL OR >8.9-13.9 mmol/L
        • No dosage adjustment required
        • Initiate/intensify antidiabetic treatment
        • If FG not decreased to ≤160 mg/dL or 8.9 mmol/L within 21 days under appropriate antidiabetic treatment, reduce dose by 1 level and follow FG value specific recommendation
      • Grade 3
        • FG >250-500 mg/dL OR >13.9-27.8 mmol/L
        • Interrupt dose
        • Initiate/intensify oral antidiabetic therapy and consider additional antidiabetic medications (eg, insulin) for 1-2 days until hyperglycemia improves
        • Administer IV hydration and consider appropriate treatment (eg, intervention for electrolyte/ketoacidosis/hyperosmolar disturbances)
        • If FG decreases to ≤160 mg/dL or 8.9 mmol/L within 3-5 days under appropriate antidiabetic treatment, resume at 1 lower dose level
        • If FG not decreased to ≤160 mg/dL or 8.9 mmol/L within 3-5 days under appropriate antidiabetic treatment, consult with a physician specialist for treatment of hyperglycemia
        • If FG not decreased to ≤160 mg/dL or 8.9 mmol/L within 21 days following appropriate antidiabetic treatment, permanently discontinue
      • Grade 4
        • FG >500 mg/dL or ≤27.8 mmol/L
        • Interrupt dose
        • Initiate/intensify appropriate antidiabetic treatment
        • Administer IV hydration and consider appropriate treatment (eg, intervention for electrolyte/ketoacidosis/hyperosmolar disturbances); recheck FG within 24 hr and as clinically indicated
        • If FG decreases to ≤500 mg/dL or 27.8 mmol/L, follow recommendations for Grade 3 hyperglycemia
        • If FG confirmed at >500 mg/dL or 27.8 mmol/L, permanently discontinue

      Cutaneous adverse reactions

      • Confirmed etiology is severe cutaneous adverse reaction (SCAR)
        • Permanently discontinue
        • Do not reintroduce in patients who previously experienced SCAR during treatment
      • Grade 1
        • <10% BSA with active skin toxicity
        • No dosage adjustment required unless etiology determined to be SCAR (then permanently discontinue)
        • Initiate topical corticosteroid treatment; consider adding oral antihistamine to manage symptoms
        • Active rash not improved ≤28 days of appropriate treatment: Add a low dose systemic corticosteroid
      • Grade 2
        • 10-30% BSA with active skin toxicity
        • No dosage adjustment required unless etiology determined to be SCAR (then permanently discontinue)
        • Initiate or intensify topical corticosteroid and oral antihistamine treatment
        • Consider low-dose systemic corticosteroid treatment
        • Rash improves to Grade ≤1 within 10 days: May discontinue systemic corticosteroid
      • Grade 3
        • Severe rash not responsive to medical management; >30% BSA with active skin toxicity
        • Interrupt dose and initiate or intensify topical/systemic corticosteroid and oral antihistamine treatment
        • If etiology is not SCAR, once improved to Grade ≤1, resume at next lower dose level
      • Grade 4
        • Severe bullous, blistering, or exfoliating skin conditions; any % BSA associated with extensive superinfection, with IV antibiotics indicated; life-threatening consequences
        • Permanently discontinue

      Diarrhea or colitis

      • All grades: Initiate or intensify appropriate medical therapy and monitor as clinically indicated
      • Grade 1: No dosage adjustment required
      • Grade 2: Interrupt dose until recovery to Grade ≤1, then resume at same dose level
      • Grade 2 and 3 colitis: Consider additional treatment (eg, enteric-acting and/or systemic steroids)
      • Grade ≥2 recurs or Grade 3: Interrupt dose until recovery to Grade ≤1, then resume at next lower dose level
      • Grade 4: Permanently discontinue

      Pneumonitis

      • Any grade: Interrupt dose if suspected
      • Permanently discontinue if confirmed

      Pancreatitis

      • Grades 2 or 3: Interrupt until improvement to Grade <2; resume at next lower dose (only 1 dose reduction permitted); if recurs, permanently discontinue
      • Grade 4: Permanently discontinue

      Other toxicities

      • Grades 1 or 2: No dosage adjustment required; initiate appropriate medical therapy and monitor as clinically indicated
      • Grade 2 elevated total bilirubin: Interrupt dose until recovery to Grade ≤1 and resume at same dose if resolved in ≤14 days or resume at next lower dose level if resolved in >14 days
      • Grade 3: Interrupt dose until recovery to Grade ≤1 and initiate/intensify appropriate therapy, then resume at the next lower dose level
      • Grade 4: Permanently discontinue

      Renal impairment

      • Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage adjustment required
      • Severe (CrCl <30 mL/min): Pharmacokinetic data are unknown

      Dosing Considerations

      Patient selection (breast cancer)

      • Select based on presence of ≥1 PIK3CA mutations in tumor tissue or plasma specimens
      • If no mutation is detected in a plasma specimen, test tumor tissue
      • Information on FDA-approved tests is available at: http://www.fda.gov/CompanionDiagnostics

      Monitoring parameters

      • Before initiation: FPG, HbA1c, and optimize blood glucose
      • Verify pregnancy status in females of reproductive potential
      • During treatment
        • FG: At least qWeek for first 2 weeks, then at least q4Weeks, and as clinically indicated
        • HbA1c: Every 3 months and as clinically indicated
        • Closely monitor FG for first few weeks in patients with risk factors for hyperglycemia, such as obesity (BMI ≥30), elevated FG, HbA1c ≥ULN, use of systemic corticosteroids, or age ≥75 yr
        • Signs and symptoms of SCARs (eg, a prodrome of fever, flu-like symptoms, mucosal lesions, progressive skin rash, lymphadenopathy)

      Dosage Forms & Strengths

      tablet (Vijoice)

      • 50mg
      • 125mg

      PIK3CA-Related Overgrowth Spectrum

      Vijoice only

      Indicated for patients aged ≥2 years with severe manifestations of PIK3CA-related overgrowth spectrum (PROS) who require systemic therapy

      <2 years: Safety and efficacy not established

      2 to <6 years

      • 50 mg PO qDay
      • Continue until disease progression or unacceptable toxicity

      6 to <18 years

      • Initial: 50 mg PO qDay
      • After 24 week: Consider increasing to 125 mg qDay for response optimization (clinical/radiological)
      • Continue until disease progression or unacceptable toxicity

      ≥18 years

      • Consider gradually increase up to 250 mg qDay

      Dosage Modifications

      PROS dose reduction recommendations

      • Pediatrics
        • Dose prior to reduction is 125 mg qDay: Reduce to 50 mg PO qDay
        • Dose prior to reduction is 50 mg qDay: Discontinue if 50 mg/day not tolerated

      Hyperglycemia

      • Monitor by using only fasting glucose (FG) values (fasting plasma glucose [FPG] or fasting blood glucose)
      • Initiate or adjust applicable antihyperglycemic medications
      • May use insulin for 1-2 days until hyperglycemia resolves; may not be necessary in most drug-induced hyperglycemia, given short half-life of alpelisib and glucose levels normalizing after dose interruption
      • Grade 1
        • FG >ULN to 160mg/dL OR >ULN to 8.9 mmol/L
        • No dosage adjustment required
        • Initiate/intensify antidiabetic therapy
      • Grade 2
        • FG >160-250 mg/dL OR >8.9-13.9 mmol/L
        • No dosage adjustment required
        • Initiate/intensify antidiabetic treatment
        • If not decreased to ≤160 mg/dL or 8.9 mmol/L within 21 days under appropriate anti-hyperglycemic treatment, interrupt dosing until improvement to Grade ≤1, then resume at 50 mg and follow FG value specific recommendations
      • Grade 3
        • FG >250-500 mg/dL OR >13.9-27.8 mmol/L
        • Interrupt dose
        • Initiate/intensify oral antidiabetic therapy and consider additional antidiabetic medications (eg, insulin) for 1-2 days until hyperglycemia improves
        • Administer IV hydration and consider appropriate treatment (eg, intervention for electrolyte/ketoacidosis/hyperosmolar disturbances)
        • If FG decreases to ≤160 mg/dL or 8.9 mmol/L within 3-5 days under appropriate antidiabetic treatment, resume at 50 mg
        • If FG not decreased to ≤160 mg/dL or 8.9 mmol/L within 3-5 days under appropriate antidiabetic treatment, consult with a physician specialist for treatment of hyperglycemia if treatment should be resumed or permanently discontinued
        • If FG not decreased to ≤160 mg/dL or 8.9 mmol/L within 21 days following appropriate antidiabetic treatment, permanently discontinue
        • If hyperglycemia recurs at Grade ≥3, consider permanent discontinuation
      • Grade 4
        • FG >500 mg/dL or ≤27.8 mmol/L
        • Interrupt dose
        • Initiate/intensify appropriate antidiabetic treatment
        • Administer IV hydration and consider appropriate treatment (eg, intervention for electrolyte/ketoacidosis/hyperosmolar disturbances); recheck FG within 24 hr and as clinically indicated
        • If FG decreases to ≤500 mg/dL or 27.8 mmol/L, follow recommendations for Grade 3 hyperglycemia
        • If FG confirmed at >500 mg/dL or 27.8 mmol/L, permanently discontinue

      Cutaneous adverse reactions

      • Confirmed etiology is severe cutaneous adverse reaction (SCAR)
        • Permanently discontinue
        • Do not reintroduce in patients who previously experienced SCAR during treatment
      • Grade 1
        • <10% BSA with active skin toxicity
        • No dosage adjustment required unless etiology determined to be SCAR (then permanently discontinue)
        • Initiate topical corticosteroid treatment; consider adding oral antihistamine to manage symptoms
        • Active rash not improved ≤28 days of appropriate treatment: Add a low dose systemic corticosteroid
      • Grade 2
        • 10-30% BSA with active skin toxicity
        • No dosage adjustment required unless etiology determined to be SCAR (then permanently discontinue)
        • Initiate or intensify topical corticosteroid and oral antihistamine treatment
        • Consider low-dose systemic corticosteroid treatment
        • Rash improves to Grade ≤1 within 10 days: May discontinue systemic corticosteroid
      • Grade 3
        • Severe rash not responsive to medical management; >30% BSA with active skin toxicity
        • Interrupt dose and initiate or intensify topical/systemic corticosteroid and oral antihistamine treatment
        • If etiology is not SCAR, once improved to Grade ≤1 may resume at 50 mg while continuing PO antihistamine treatment or permanently discontinue
        • Permanently discontinue if patient was receiving antihistamines and antihistamine dose cannot be increased or if Grade >3 recurs
      • Grade 4
        • Severe bullous, blistering, or exfoliating skin conditions; any % BSA associated with extensive superinfection, with IV antibiotics indicated; life-threatening consequences
        • Permanently discontinue treatment

      Diarrhea or colitis

      • Consider consultation with physician experienced in treating gastrointestinal conditions
      • All grades: Initiate or intensify appropriate medical therapy and monitor as clinically indicated
      • Grade 1: No dosage adjustment required
      • Grade 2: Interrupt dose until recovery to Grade ≤1, then resume at same dose level
      • Grade ≥2 recurs: Interrupt dose until recovery to Grade ≤1, then resume at 50 mg
      • Grade 2 and 3 colitis: Consider additional treatment (eg, enteric-acting and/or systemic steroids)
      • Grade 3: Interrupt dose until recovery to Grade ≤1, either resume at 50 mg or permanently discontinue; consider permanent discontinuation if Grade >3 recurs
      • Grade 4: Permanently discontinue

      Pneumonitis

      • Any grade: Interrupt dose if suspected
      • Permanently discontinue if confirmed

      Pancreatitis

      • Grade 2: Interrupt until improvement to Grade <2; resume at 50 mg; if recurs, permanently discontinue
      • Grades 3 or 4: Permanently discontinue

      Other toxicities

      • Grades 1 or 2: No dosage adjustment required; initiate appropriate medical therapy and monitor as clinically indicated
      • Grade 2 elevated total bilirubin: Interrupt dose until recovery to Grade ≤1 and resume at same dose if resolved in ≤14 days or resume at 50 mg if resolved in >14 days
      • Grade 3: Interrupt dose until recovery to Grade ≤1 and initiate/intensify appropriate therapy, resume at 50 mg or consider permanent discontinuation
      • Grade 4: Permanently discontinue

      Dosing Considerations

      Monitoring parameters

      • Before initiation: FPG, HbA1c, and optimize blood glucose
      • Verify pregnancy status in females of reproductive potential
      • During treatment
        • FG: At least qWeek for first 2 weeks, then at least q4Weeks, and as clinically indicated
        • HbA1c: Every 3 months and as clinically indicated
        • Closely monitor FG for first few weeks in patients with risk factors for hyperglycemia, such as obesity (BMI ≥30), elevated FG, HbA1c ≥ULN, use of systemic corticosteroids, or age ≥75 yr
        • Signs and symptoms of SCARs (eg, a prodrome of fever, flu-like symptoms, mucosal lesions, progressive skin rash, lymphadenopathy)

      Breast cancer: Patients aged ≥65 years had higher incidence of grade 3-4 hyperglycemia compared with patients aged <65 years

      Patients aged ≥75 years (breast cancer) or ≥65 years (PIK3CA-related overgrowth spectrum [PROS]): Insufficient number of patients to assess differences in safety and efficacy

      Next:

      Interactions

      Interaction Checker

      and alpelisib

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                  Serious - Use Alternative (58)

                  • abametapir

                    abametapir will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

                  • acalabrutinib

                    acalabrutinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • apalutamide

                    apalutamide will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • atazanavir

                    atazanavir will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                  • bosentan

                    bosentan will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • butabarbital

                    butabarbital will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • butalbital

                    butalbital will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • carbamazepine

                    carbamazepine will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • cobicistat

                    cobicistat will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                    cobicistat will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                  • cyclosporine

                    cyclosporine will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • dabrafenib

                    dabrafenib will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                    dabrafenib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • darolutamide

                    darolutamide will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).

                  • dipyridamole

                    dipyridamole will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • efavirenz

                    efavirenz will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • eltrombopag

                    eltrombopag will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • eluxadoline

                    eluxadoline will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • enzalutamide

                    enzalutamide will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • erdafitinib

                    alpelisib will increase the level or effect of erdafitinib by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. If coadministration of a strong CYP2C9 inhibitors is unavoidable, closely monitor adverse reactions and modify dose of erdafitinib accordingly. If strong CYP2C9 inhibitor is discontinued, consider increasing erdafitinib dose in the absence of any drug-related toxicities.

                  • etravirine

                    etravirine will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • fexinidazole

                    fexinidazole will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

                  • fosphenytoin

                    fosphenytoin will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • gefitinib

                    gefitinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • imatinib

                    imatinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • ivosidenib

                    ivosidenib will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • ketoconazole

                    ketoconazole will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • lapatinib

                    lapatinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • lasmiditan

                    lasmiditan increases levels of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates.

                  • levoketoconazole

                    levoketoconazole will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • lonafarnib

                    lonafarnib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

                  • lopinavir

                    lopinavir will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                  • lorlatinib

                    lorlatinib will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • lumacaftor/ivacaftor

                    lumacaftor/ivacaftor will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • mitotane

                    mitotane will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • nafcillin

                    nafcillin will decrease the level or effect of alpelisib by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • osimertinib

                    osimertinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • pantoprazole

                    pantoprazole will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • pentobarbital

                    pentobarbital will decrease the level or effect of alpelisib by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • phenobarbital

                    phenobarbital will decrease the level or effect of alpelisib by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                    phenobarbital will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                  • phenytoin

                    phenytoin will decrease the level or effect of alpelisib by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                    phenytoin will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

                  • ponatinib

                    ponatinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • primidone

                    primidone will decrease the level or effect of alpelisib by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                    primidone will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • regorafenib

                    regorafenib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • rifabutin

                    rifabutin will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • rifampin

                    rifampin will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • rifapentine

                    rifapentine will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • rolapitant

                    rolapitant will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • safinamide

                    safinamide will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • secobarbital

                    secobarbital will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • St John's Wort

                    St John's Wort will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of alpelisib (CYP3A4 substrate) with strong CYP3A4 inducers.

                  • stiripentol

                    stiripentol will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • sunitinib

                    sunitinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • tacrolimus

                    tacrolimus will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • tafamidis

                    tafamidis will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • tafamidis meglumine

                    tafamidis meglumine will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • vandetanib

                    vandetanib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • velpatasvir

                    velpatasvir will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • vemurafenib

                    vemurafenib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.

                  • voxelotor

                    voxelotor will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

                  Monitor Closely (50)

                  • armodafinil

                    armodafinil will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • belzutifan

                    belzutifan will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

                  • bexarotene

                    bexarotene will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • bosentan

                    alpelisib will decrease the level or effect of bosentan by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • brigatinib

                    brigatinib will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • celecoxib

                    alpelisib will decrease the level or effect of celecoxib by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • cenobamate

                    cenobamate will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

                  • chlorpropamide

                    alpelisib will decrease the level or effect of chlorpropamide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • diclofenac

                    alpelisib will decrease the level or effect of diclofenac by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • dronabinol

                    alpelisib will decrease the level or effect of dronabinol by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • elagolix

                    elagolix will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

                  • encorafenib

                    encorafenib will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                    encorafenib will increase the level or effect of alpelisib by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.

                  • eslicarbazepine acetate

                    eslicarbazepine acetate will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • etravirine

                    alpelisib will decrease the level or effect of etravirine by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • fedratinib

                    fedratinib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

                  • fluoxetine

                    alpelisib will decrease the level or effect of fluoxetine by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • fluvastatin

                    alpelisib will decrease the level or effect of fluvastatin by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely.

                  • fosphenytoin

                    alpelisib will decrease the level or effect of fosphenytoin by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • fostemsavir

                    fostemsavir will increase the level or effect of alpelisib by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.

                  • glimepiride

                    alpelisib will decrease the level or effect of glimepiride by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • glipizide

                    alpelisib will decrease the level or effect of glipizide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • glyburide

                    alpelisib will decrease the level or effect of glyburide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • imatinib

                    alpelisib will decrease the level or effect of imatinib by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • istradefylline

                    istradefylline will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

                  • ketamine

                    alpelisib will decrease the level or effect of ketamine by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • lacosamide

                    alpelisib will decrease the level or effect of lacosamide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • lenacapavir

                    lenacapavir will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

                  • lesinurad

                    alpelisib will decrease the level or effect of lesinurad by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • losartan

                    alpelisib will decrease the level or effect of losartan by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • mestranol

                    alpelisib will decrease the level or effect of mestranol by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • miconazole oral

                    alpelisib will decrease the level or effect of miconazole oral by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • montelukast

                    alpelisib will decrease the level or effect of montelukast by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

                  • nateglinide

                    alpelisib will decrease the level or effect of nateglinide by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

                  • ospemifene

                    alpelisib will decrease the level or effect of ospemifene by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

                  • oteseconazole

                    oteseconazole will increase the level or effect of alpelisib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.

                  • phenytoin

                    alpelisib will decrease the level or effect of phenytoin by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

                  • propofol

                    alpelisib will decrease the level or effect of propofol by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

                  • rucaparib

                    rucaparib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

                  • siponimod

                    alpelisib will decrease the level or effect of siponimod by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • sulfadiazine

                    alpelisib will decrease the level or effect of sulfadiazine by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • sulfisoxazole

                    alpelisib will decrease the level or effect of sulfisoxazole by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • tamoxifen

                    alpelisib will decrease the level or effect of tamoxifen by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • tazemetostat

                    tazemetostat will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • telotristat ethyl

                    telotristat ethyl will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                  • tolbutamide

                    alpelisib will decrease the level or effect of tolbutamide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • torsemide

                    alpelisib will decrease the level or effect of torsemide by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • trimethoprim

                    alpelisib will decrease the level or effect of trimethoprim by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • voriconazole

                    alpelisib will decrease the level or effect of voriconazole by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • warfarin

                    alpelisib will decrease the level or effect of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  • zafirlukast

                    alpelisib will decrease the level or effect of zafirlukast by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

                  Minor (8)

                  • acetazolamide

                    acetazolamide will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • amobarbital

                    amobarbital will decrease the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • anastrozole

                    anastrozole will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • cyclophosphamide

                    cyclophosphamide will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • dapsone

                    alpelisib will decrease the level or effect of dapsone by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

                  • larotrectinib

                    larotrectinib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • levoketoconazole

                    levoketoconazole will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

                  • ribociclib

                    ribociclib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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                  Adverse Effects

                  >10%

                  Breast cancer

                  • Glucose increased (79%)
                  • Creatinine increased (67%)
                  • Diarrhea (58%)
                  • Rash (52%)
                  • Lymphocyte count decreased (52%)
                  • GGT increased (52%)
                  • Nausea (45%)
                  • ALT increased (44%)
                  • Fatigue (42%)
                  • Hemoglobin decreased (42%)
                  • Lipase increased (42%)
                  • Glucose increased, grade 3-4 (39%)
                  • Decreased appetite (36%)
                  • Stomatitis (30%)
                  • Vomiting (27%)
                  • Decreased weight (27%)
                  • Calcium (corrected) decreased (27%)
                  • Glucose decreased (26%)
                  • aPTT prolonged (21%)
                  • Alopecia (20%)
                  • Rash, grade 3-4 (20%)
                  • Mucosal inflammation (19%)
                  • Pruritus (18%)
                  • Dry skin (18%)
                  • Dysgeusia (18%)
                  • Headache (18%)
                  • Abdominal pain (17%)
                  • Peripheral edema (15%)
                  • Pyrexia (14%)
                  • Platelet count decreased (14%)
                  • Potassium decreased (14%)
                  • Albumin decreased (14%)
                  • Mucosal dryness (12%)
                  • Dyspepsia (11%)
                  • Magnesium decreased (11%)
                  • GGT increased, grade 3-4 (11%)

                  PROS (all grades)

                  • Decreased calcium (60%)
                  • Decreased phosphate (59%)
                  • Increased glucose (56%)
                  • Increased HbA1c (38%)
                  • Increased creatinine (31%)
                  • Increased bilirubin (29%)
                  • Increased potassium (24%)
                  • Decreased leukocytes (22%)
                  • Decreased hemoglobin (20%)
                  • Decreased neutrophils (19%)
                  • Increased triglycerides (19%)
                  • Decreased magnesium (18%)
                  • Increased lymphocytes (17%)
                  • Increased AST (17%)
                  • Diarrhea (16%)
                  • Stomatitis (16%)
                  • Decreased platelets (14%)
                  • Increased cholesterol (13%)
                  • Decreased albumin (13%)
                  • Hyperglycemia (12%)
                  • Decreased sodium (12%)
                  • Decreased potassium (12%)
                  • Increased GGT (11%)

                  PROS (Grade 3 or 4)

                  • Increased glucose (11%)

                  1-10%

                  Breast cancer

                  • Urinary tract infection (10%)
                  • Lymphocyte count decreased, grade 3-4 (8%)
                  • Diarrhea, grade 3-4 (7%)
                  • Lipase increased, grade 3-4 (7%)
                  • Potassium decreased, grade 3-4 (2.1%)
                  • Fatigue, grade 3-4 (5%)
                  • Hemoglobin decreased, grade 3-4 (4.2%)
                  • Decreased weight, grade 3-4 (3.9%)
                  • ALT increased, grade 3-4 (3.5%)
                  • Creatinine increased, grade 3-4 (2.8%)
                  • Nausea, grade 3-4 (2.5%)
                  • Stomatitis, grade 3-4 (2.5%)
                  • Mucosal inflammation, grade 3-4 (2.1%)
                  • Calcium (corrected) decreased (2.1%)
                  • Abdominal pain, grade 3-4 (1.4%)
                  • Platelet count decreased, grade 3-4 (1.1%)

                  PROS (all grades)

                  • Increased ALT (10%)
                  • Eczema (7%)
                  • Dry skin (7%)
                  • Alopecia (5%)
                  • Headache (5%)
                  • Cellulitis (5%)

                  PROS (Grade 3 or 4)

                  • Decreased hemoglobin (6%)
                  • Decreased phosphate (5%)
                  • Cellulitis (3.5%)
                  • Increased bilirubin (2%)
                  • Decreased sodium (2%)
                  • Decreased platelets (2%)

                  <1%

                  Breast cancer

                  • Pruritus, grade 3-4 (0.7%)
                  • Urinary tract infection, grade 3-4 (0.7%)
                  • Headache, grade 3-4 (0.7%)
                  • Decreased appetite, grade 3-4 (0.7%)
                  • Vomiting, grade 3-4 (0.7%)
                  • aPTT prolonged, grade 3-4 (0.7%)
                  • Dry skin, grade 3-4 (0.4%)
                  • Dysgeusia, grade 3-4 (0.4%)
                  • Mucosal dryness, grade 3-4 (0.4%)
                  • Glucose decreased, grade 3-4 (0.4%)
                  • Magnesium decreased, grade 3-4 (0.4%)

                  Postmarketing Reports

                  Breast cancer

                  • Skin and subcutaneous tissue disorders: Drug reaction with eosinophilia and systemic symptoms (DRESS)
                  • Metabolism and nutrition disorders: Hyperglycemic hyperosmolar nonketotic syndrome (HHNKS)

                  PROS

                  • Skin and subcutaneous tissue disorders: Pruritus, rash (including rash maculopapular, rash erythematous, rash papular, and rash pruritic), acne (including dermatitis acneiform)
                  • Metabolism and nutrition disorders: Decreased appetite
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                  Warnings

                  Contraindications

                  Hypersensitivity to alpelisib or any of its components

                  Cautions

                  Angioedema reported in postmarketing setting

                  Severe hypersensitivity reactions (eg, anaphylaxis, anaphylactic shock, angioedema) reported; reactions manifested by symptoms including, but not limited to, dyspnea, flushing, rash, fever, or tachycardia; permanently discontinue if hypersensitivity occurs

                  Severe pneumonitis, including acute interstitial pneumonitis and interstitial lung disease, reported; consider noninfectious pneumonitis in patients presenting with nonspecific respiratory signs and symptoms (eg, hypoxia, cough, dyspnea, or interstitial infiltrates on radiologic examinations) and in whom infectious, neoplastic, and other causes have been excluded; permanently discontinue in all patients if confirmed; advise patients to immediately report new or worsening respiratory symptoms

                  Based on findings in animals and its mechanism of action, fetal harm may occur when administered to pregnant women

                  Diarrhea or Colitis

                  • Severe diarrhea, including dehydration and acute kidney injury, occurred; based on severity of diarrhea, therapy may require dose interruption, reduction, or discontinuation; advise patients to start antidiarrheal treatment, increase oral fluids, and notify their healthcare provider if diarrhea occurs
                  • Colitis reported in postmarketing setting
                  • Monitor for diarrhea and additional symptoms of colitis, such as abdominal pain and mucus or blood in stool; based on severity of diarrhea or colitis, dose interruption, reduction, or discontinuation may be necessary
                  • For patients with colitis, additional treatment, such as enteric-acting and/or systemic steroids, may be required

                  Severe cutaneous adverse reactions

                  • Severe cutaneous reactions, including Stevens-Johnson syndrome (SJS) and erythema multiforme (EM) reported
                  • Do not initiate with history of SJS, EM, or toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS)
                  • If signs or symptoms of cutaneous reactions occur, interrupt therapy until etiology of reaction determined
                  • If SJS, TEN, or EM confirmed, permanently discontinue; do not reintroduce in patients who have experienced previous severe cutaneous reactions during treatment
                  • If cutaneous reactions not confirmed, therapy may require dose modifications, topical corticosteroids, or oral antihistamine treatment

                  Severe hyperglycemia

                  • Closely monitor patients with diabetes
                  • Based on severity of hyperglycemia, therapy may require dose interruption, reduction, or discontinuation
                  • In some cases associated with hyperglycemic hyperosmolar non-ketotic syndrome (HHNKS) or ketoacidosis; some fatal cases of ketoacidosis have occurred in the post marketing setting
                  • Before initiating treatment, test FPG and HbA1c, and optimize blood glucose
                  • After initiation, monitor fasting glucose more frequently for the first few weeks during treatment in patients with risk factors for hyperglycemia such as obesity (BMI greater than or equal to 30), elevated FPG, HbA1c at the upper limit of normal or above, use of concomitant systemic corticosteroids, or age greater than or equal to 75
                  • Monitor blood glucose and/or FPG at least qWeek for the first 2 weeks, then at least q4Weeks, and as clinically indicated; monitor HbA1c every 3 months and as clinically indicated
                  • During treatment with antidiabetic medication, continue monitoring blood glucose or FPG at least once a week for 8 weeks, followed by once q2Weeks and as clinically indicated
                  • Advise patients of signs and symptoms of hyperglycemia (eg, excessive thirst, urinating more often than usual or higher amount of urine than usual, or increased appetite with weight loss)

                  Drug interactions overview

                  • Alpelisib: CYP3A4 and BCRP substrate; CYP2C9 inducer
                  • CYP3A4 inducers
                    • Avoid coadministration
                    • Strong CYP3A4 inducers may decrease alpelisib concentration and/or activity
                  • BCRP inihibitors
                    • Avoid coadministration; if unable to avoid or use alternant drugs, closely monitor for increased adverse effects of alpelisib
                    • BCRP inhibitors may increase alpelisib concentration and/or risk of toxicities
                  • CYP2C9 substrates
                    • Closely monitor for potential reduced activity of CYP2C9 substrate
                    • Coadministration of alpelisib with CYP2C9 substrates (eg, warfarin) may reduce plasma concentration of CYP2C9 substrates
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                  Pregnancy & Lactation

                  Pregnancy

                  Based on animal data and mechanism of action, fetal harm may occur when administered to pregnant women

                  No data available in pregnant women to inform the drug-associated risk

                  Advise pregnant women and females of reproductive potential of fetal risk

                  Verify pregnancy status in females of reproductive potential before initiating

                  Animal data

                  • In animal reproduction studies, oral administration to pregnant rats and rabbits during organogenesis caused adverse developmental outcomes, including embryofetal mortality (postimplantation loss), reduced fetal weights, and increased incidences of fetal malformations at maternal exposures ≥0.8 times the exposure in humans based on AUC at the recommended dose of 300 mg/day

                  Contraception

                  • Females of reproductive potential: Use effective contraception during treatment and for 1 week after the last dose
                  • Male patients with female partners of reproductive potential: Use condoms and effective contraception during treatment and for 1 week after the last dose

                  Infertility

                  • Based on findings from animal studies, fertility in males and females of reproductive potential may be impaired

                  Lactation

                  There are no data on the presence of alpelisib in human milk, its effects on milk production, or the breastfed child

                  Because of potential for serious adverse reactions in the breastfed child, advise lactating women to not breastfeed during treatment and for 1 week after the last dose

                  Pregnancy Categories

                  A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                  B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                  C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                  D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                  X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                  NA: Information not available.

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                  Pharmacology

                  Mechanism of Action

                  Phosphatidylinositol-3-kinase (PI3K) inhibitor with inhibitory activity predominantly against PI3K-alpha

                  Gain-of-function mutations in the gene encoding the catalytic alpha-subunit of PI3K (PIK3CA) lead to activation of PI3K-alpha and Akt-signaling, cellular transformation, and generation of tumors in in vitro and in vivo models

                  Breast cancer

                  • Inhibits the phosphorylation of PI3K downstream targets and has shown activity in cell lines possessing a PIK3CA mutation
                  • PI3K inhibition has been shown to induce an increase in ER transcription in breast cancer cells
                  • Combination with fulvestrant demonstrates an increase in antitumor activity compared with either treatment alone

                  PIK3CA-related overgrowth spectrum (PROS)

                  • Activating mutations in PIK3CA induce a spectrum of overgrowths and malformations comprising a wide group of clinically recognizable disorders commonly known as PROS
                  • Spectrum includes
                    • CLAPO syndrome
                    • CLOVES syndrome
                    • Diffuse capillary malformation with overgrowth (DCMO)
                    • Dysplastic megalencephaly (DMEG)
                    • Fibroadipose hyperplasia (FAH)/fibroadipose overgrowth (FAO)/hemihyperplasia-multiple lipomatosis syndrome (HHML)
                    • Fibroadipose vascular anomaly (FAVA)
                    • Facial infiltrating lipomatosis (FIL)
                    • Hemimegalencephaly (HMEG)
                    • Klippel-Trenaunay syndrome (KTS)
                    • Lipomatosis of nerve (LON)
                    • Macrodactyly
                    • Megalencephaly-capillary malformation syndrome (MCAP syndrome)
                    • Muscular hemihyperplasia (HH)

                  Absorption

                  Peak plasma concentration at steady-state: 2480 ng/mL

                  Peak plasma time: 2-4 hr

                  AUC: 33,224 ng·hr/mL

                  Steady-state reached within 3 days

                  Effects of food following a single dose

                  • High-fat, high-calorie meal (985 calories with 58.1 grams of fat) increased AUC by 73% and peak plasma concentration by 84%
                  • Low-fat, low-calorie meal (334 calories with 8.7 grams of fat) increased AUC by 77% and peak plasma concentration by 145%

                  Distribution

                  Vd: 114 L

                  Protein bound: 89%

                  Metabolism

                  Primarily metabolized by chemical and enzymatic hydrolysis to form its metabolite, BZG791

                  Metabolized to a lesser extent by CYP3A4

                  Elimination

                  Half-life: 8-9 hr

                  Clearance: 9.2 L/hr

                  Excretion

                  • Feces: 81% (36% unchanged, 32% BZG791)
                  • Urine: 14% (2% unchanged, 7.1 BZG791)
                  • CYP3A4-mediated metabolites accounted for 12% of the dose
                  • Glucuronides accounted for ~15% of the dose
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                  Administration

                  Oral Administration

                  Take orally with food

                  Administer dose at approximately same time each day

                  Swallow tablet whole (do not chew, crush, or split)

                  Do not ingest if tablet is broken, cracked, or otherwise not intact

                  Missed dose

                  • Missed dose ≤9 hr of scheduled time: Take dose
                  • Missed dose >9 hr of scheduled time: Skip dose for that day; the next day, take dose at usual time
                  • If dose is vomited, advise not to take an additional dose on that day; resume dosing schedule the next day at the usual time

                  Compounding oral suspension

                  • Place tablets in glass containing 2-4 oz water and let it stand for ~5 minutes
                  • Make suspension with water only
                  • Crush tablets with a spoon and stir until an oral suspension obtained
                  • Administer immediately after preparation
                  • Discard if not administered within 60 minutes after preparation
                  • After administration, add ~2-3 tablespoons of water to the same glass, stir with same spoon to resuspend any remaining particles and administer entire contents of the glass
                  • Repeat if particles remain

                  Storage

                  Store at 20-25°C (68-77°F), excursions permitted to 15-30°C (59-86°F)

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                  Images

                  BRAND FORM. UNIT PRICE PILL IMAGE
                  Piqray oral
                  -
                  		250 mg/day (200 mg x1-50 mg x1) tablet
                  Piqray oral
                  -
                  		300 mg/day (150 mg x 2) tablet
                  Piqray oral
                  -
                  		200 mg/day (200 mg x 1) tablet

                  Copyright © 2010 First DataBank, Inc.

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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Formulary

                  FormularyPatient Discounts

                  Adding plans allows you to compare formulary status to other drugs in the same class.

                  To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                  Create Your List of Plans

                  Adding plans allows you to:

                  • View the formulary and any restrictions for each plan.
                  • Manage and view all your plans together – even plans in different states.
                  • Compare formulary status to other drugs in the same class.
                  • Access your plan list on any device – mobile or desktop.

                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  View explanations for tiers and restrictions
                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.
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