cabotegravir (Rx)

Brand and Other Names:Vocabria, Apretude
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 30mg (Vocabria)

injection, extended-release IM suspension

  • 600mg/3mL (Apretude)

HIV Infection Treatment

Oral cabotegravir is indicated in combination with rilpivirine PO as a complete regimen for short-term treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral therapy (ART) regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine

Indication specifics

  • Oral lead-in to assess tolerability of cabotegravir before administration of cabotegravir extended-release injectable IM suspension, a component of Cabenuva (cabotegravir; rilpivirine extended-release injectable suspensions)
  • Oral therapy for patients who will miss planned IM injection dosing with cabotegravir

Oral lead-in dosing before Cabenuva

  • 30 mg PO qDay plus rilpivirine 25 mg PO qDay for at least 28 days to assess tolerability
  • Take last oral dose on the same day injections with Cabenuva are started

Oral replacement dose for planned missed Cabenuva injections

  • If patient plans to miss scheduled Cabenuva (cabotegravir; rilpivirine) ER injectable suspensions by >7 days, take daily PO therapy to replace up to 2 consecutive monthly or 1 scheduled every-2-month injection visit(s)
  • 30 mg PO qDay plus rilpivirine 25 mg PO qDay as replacement for up to 2 consecutive months
  • Take first dose of oral therapy at approximately the same time as the planned missed injection and continue until the day injection dosing restarted

HIV Pre-exposure Prophylaxis

IM

  • Indicated in at-risk adults and adolescents weighing ≥35 kg for pre-exposure prophylaxis (PrEP) to reduce risk of sexually acquired HIV-1 infection
  • May be initiated with oral cabotegravir before starting IM injections or may proceed directly to injection without an oral lead-in
  • If an oral lead-in is used, administer initiation injections on last day of oral lead-in or within 3 days thereafter
  • Initiation injections: 600 mg IM x 2 doses 1 month apart; may administer second initiation injection up to 7 days before or after the date scheduled to receive injection, THEN
  • Continuation injections: 600 mg IM q2months

PO

  • Indicated in at-risk adults and adolescents weighing ≥35 kg for short-term pre-exposure prophylaxis (PrEP) to reduce risk of sexually acquired HIV-1 infection
  • Indication specifics
    • Oral lead-in to assess tolerability of cabotegravir before starting ER IM injections (Apretude)
    • Oral PrEP for patients who will miss planned IM injection

Oral lead-in dosing before Apretude IM

  • 30 mg PO qDay for ~1 month (at least 28 days)
  • Following oral lead-in, initiate cabotegravir IM on last day of oral lead-in or within 3 days

Oral replacement dose for planned missed Apretude injections

  • If patient plans to miss scheduled Apretude (cabotegravir) ER injectable suspension by >7 days, take daily PO therapy to replace up to 2 consecutive monthly injection visits
  • 30 mg PO qDay as replacement for up to 2 consecutive months
  • Take first oral dose ~2 months after the last injection of cabotegravir IM injection
  • Restart cabotegravir IM q2months on day oral dosing completes or within 3 days

Dosage Modifications

Renal impairment

  • PO
    • Mild-to-severe (CrCl ≥30 to <90 mL/min): No dosage adjustment required
    • ESRD (<15 mL/min): Pharmacokinetic effects are unknown
    • Dialysis: Cabotegravir is >99% protein bound; dialysis is not expected to alter systemic exposure
  • IM
    • Mild-to-moderate (CrCl ≥60 to <90 mL/min): No dosage adjustment required
    • Severe (15 to <30 mL/min) or ESRD (<15 mL/min): Increase monitoring
    • ESRD not on dialysis: Pharmacokinetic effects are unknown
    • Dialysis: Cabotegravir is >99% protein bound; dialysis is not expected to alter systemic exposure

Hepatic impairment

  • Mild or moderate (Child-Pugh A or B): No dosage adjustment required
  • Severe (Child-Pugh C): Pharmacokinetic effects are unknown

Dosing Considerations

Individuals must have a negative HIV-1 test before initiating PrEP

Dosage Forms & Strengths

tablet

  • 30mg (Vocabria)

injection, extended-release IM suspension

  • 600mg/3mL (Apretude)

HIV Pre-exposure Prophylaxis

Adolescents who weigh <35 kg: Safety and efficacy not established

IM

  • Indicated in at-risk adults and adolescents who weigh ≥35 kg for pre-exposure prophylaxis (PrEP) to reduce risk of sexually acquired HIV-1 infection
  • May be initiated with oral cabotegravir before starting IM injections or may proceed directly to injection without an oral lead-in
  • If an oral lead-in is used, administer initiation injections on last day of oral lead-in or within 3 days thereafter
  • Initiation injections: 600 mg IM x 2 doses 1 month apart; may administer second initiation injection up to 7 days before or after the date scheduled to receive injection, THEN
  • Continuation injections: 600 mg IM q2months

PO

  • Indicated in at-risk adults and adolescents who weigh ≥35 kg for short-term pre-exposure prophylaxis (PrEP) to reduce risk of sexually acquired HIV-1 infection
  • Indication specifics
    • Oral lead-in to assess tolerability of cabotegravir before starting ER IM injections (Apretude)
    • Oral PrEP for patients who will miss planned IM injection

Oral lead-in dosing before Apretude IM

  • 30 mg PO qDay for ~1 month (at least 28 days)
  • Following oral lead-in, initiate cabotegravir IM on last day of oral lead-in or within 3 days

Oral replacement dose for planned missed Apretude injections

  • If patient plans to miss scheduled Apretude (cabotegravir) ER injectable suspension by >7 days, take daily PO therapy to replace up to 2 consecutive monthly injection visits
  • 30 mg PO qDay as replacement for up to 2 consecutive months
  • Take first oral dose ~2 months after the last injection of cabotegravir IM injection
  • Restart cabotegravir IM q2months on day oral dosing completes or within 3 days

Dosage Modifications

Renal impairment

  • PO
    • Mild-to-severe (CrCl ≥30 to <90 mL/min): No dosage adjustment required
    • ESRD (<15 mL/min): Pharmacokinetic effects are unknown
    • Dialysis: Cabotegravir is >99% protein bound; dialysis is not expected to alter systemic exposure
  • IM
    • Mild-to-moderate (CrCl ≥60 to <90 mL/min): No dosage adjustment required
    • Severe (15 to <30 mL/min) or ESRD (<15 mL/min): Increase monitoring
    • ESRD not on dialysis: Pharmacokinetic effects are unknown
    • Dialysis: Cabotegravir is >99% protein bound; dialysis is not expected to alter systemic exposure

Hepatic impairment

  • Mild or moderate (Child-Pugh A or B): No dosage adjustment required
  • Severe (Child-Pugh C): Pharmacokinetic effects are unknown

Dosing Considerations

Individuals must have a negative HIV-1 test before initiating PrEP

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Interactions

Interaction Checker

and cabotegravir

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            Contraindicated (16)

            • apalutamide

              apalutamide will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • carbamazepine

              carbamazepine will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • cigarette smoking

              cigarette smoking will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • desogestrel

              desogestrel will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • lamotrigine

              lamotrigine will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • nicotine gum

              nicotine gum will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • nicotine inhaled

              nicotine inhaled will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • nicotine intranasal

              nicotine intranasal will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • nicotine lozenge

              nicotine lozenge will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • nicotine transdermal

              nicotine transdermal will decrease the level or effect of cabotegravir by increasing elimination. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • phenobarbital

              phenobarbital will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • phenytoin

              phenytoin will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • primidone

              primidone will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • rifabutin

              rifabutin will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response. Note: Rifabutin can be coadministered with cabotegravir PO; however, it is contraindicated with Cabenuva (cabotegravir; rilpivirine) extended-release injectable suspensions.

            • rifampin

              rifampin will increase the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            • testosterone

              testosterone will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.

            Serious - Use Alternative (29)

            • abacavir

              abacavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • atazanavir

              atazanavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • bictegravir

              bictegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • darunavir

              darunavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • delavirdine

              delavirdine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • didanosine

              didanosine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • dolutegravir

              dolutegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • doravirine

              doravirine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • efavirenz

              efavirenz, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • elvitegravir

              elvitegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • emtricitabine

              emtricitabine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • enfuvirtide

              enfuvirtide, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • etravirine

              etravirine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • fosamprenavir

              fosamprenavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • fostemsavir

              fostemsavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • ibalizumab

              ibalizumab, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • indinavir

              indinavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • lamivudine

              lamivudine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • maraviroc

              maraviroc, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • nelfinavir

              nelfinavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • nevirapine

              nevirapine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • raltegravir

              raltegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • ritonavir

              ritonavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • saquinavir

              saquinavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • stavudine

              stavudine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • tenofovir DF

              tenofovir DF, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • tipranavir

              tipranavir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • zidovudine

              zidovudine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            Monitor Closely (12)

            • aluminum hydroxide

              aluminum hydroxide will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • aluminum hydroxide/magnesium carbonate

              aluminum hydroxide/magnesium carbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • aluminum hydroxide/magnesium trisilicate

              aluminum hydroxide/magnesium trisilicate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • calcium carbonate

              calcium carbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • calcium/vitamin D

              calcium/vitamin D will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • magaldrate

              magaldrate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • magnesium chloride

              magnesium chloride will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • magnesium citrate

              magnesium citrate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • magnesium hydroxide

              magnesium hydroxide will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • magnesium oxide

              magnesium oxide will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.

            • zinc

              zinc will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation containing products at least 2 hr before or 4 hr after oral cabotegravir.

            Minor (0)

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              Adverse Effects

              >10%

              IM

              • Injection site reaction (38-82%)
              • Creatine phosphokinase ≥10x ULN (2-15%)
              • Headache (4-12%)

              1-10%

              IM

              • Creatinine >1.8x ULN or increased to ≥1.5x baseline (3-5%)
              • Diarrhea (4%)
              • Upper respiratory tract infection (4%)
              • Pyrexia (≤4%)
              • Fatigue (3-4%)
              • Nausea (3-4%)
              • Dizziness (2-4%)
              • AST ≥5x ULN (≤3%)
              • Lipase ≥3x ULN (≤3%)
              • Sleep disorders (1-3%)
              • Abdominal pain (1-2%)
              • Vomiting (≤2%)
              • Myalgia (≤2%)
              • Rash (≤2%)
              • Decreased appetite (≤2%)
              • Somnolence (≤2%)
              • ALT ≥5x ULN (≤2%)
              • Flatulence (≤1%)
              • Back pain (≤1%)

              <1%

              PO

              • Headache
              • Nausea
              • Abnormal dreams
              • Anxiety
              • Insomnia

              IM

              • Hepatobiliary disorders: Hepatotoxicity
              • Investigations: Weight increase
              • Psychiatric disorders: Depression

              Frequency Not Defined

              Hypersensitivity

              Hepatotoxicity

              Depressive disorders

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              Warnings

              Black Box Warning

              PrEP

              • Test individuals for HIV-1 infection before initiating IM or oral cabotegravir for PrEP, and with each subsequent IM injection
              • Drug-resistant HIV-1 variants identified with use of cabotegravir IM for PrEP by individuals with undiagnosed HIV-1 infection
              • Do not initiate for HIV-1 PrEP unless negative infection status confirmed
              • Individuals who become infected with HIV-1 while receiving cabotegravir for PrEP must transition to a complete HIV-1 treatment regimen

              Contraindications

              Previous hypersensitivity to cabotegravir

              Coadministration with UGT1A1/1A9 inducers such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine, owing to possible loss of virologic response

              HIV-1 treatment: Before initiating cabotegravir PO, note that use of Cabenuva ER injectable suspensions with rifabutin is contraindicated

              HIV-1 PrEP: Unknown or positive HIV-1 status

              Cautions

              Hepatotoxicity reported in patients with or without known preexisting hepatic disease or known risk factors; monitoring of liver chemistries recommended; discontinue treatment if hepatotoxicity suspected

              Depressive disorders (including depressed mood, depression, mood altered, mood swings) reported; promptly evaluate if symptoms emerge; determine whether risks of continued therapy outweigh benefits

              Owing to use in combination with rilpivirine, consider contraindications, cautions, and drug interactions associated with rilpivirine

              Hypersensitivity

              • Serious or severe hypersensitivity reactions reported with other integrase inhibitors
              • Discontinue immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, mucosal involvement [oral blisters or lesions], conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing)
              • Monitor clinical status, including liver transaminases, and initiate appropriate therapy as warranted

              Drug interaction overview

              • Other antiretroviral medications for HIV-1 infection
                • Cabotegravir plus rilpivirine is a complete ART regimen
                • Coadministration with other ARTs is not recommended
              • UGT1A1 or UGT1A9 inducers
                • Contraindicated
                • Primarily metabolized by UGT1A1 with some contribution from UGT1A9
                • Strong UGT1A1 or 1A9 inducers are expected to decrease cabotegravir plasma concentrations and may result in loss of virologic response
              • Polyvalent cation-containing products
                • Modify dosage schedule
                • Coadministration with antacids containing polyvalent cations (eg, aluminum, magnesium hydroxide, calcium carbonate) may decrease cabotegravir absorption
                • Administer antacids at least 2 hr before or 4 hr after taking cabotegravir
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              Pregnancy & Lactation

              Pregnancy

              Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263; rate of miscarriage is not reported in the APR; the background risk for major birth defects and miscarriage for the indicated population is unknown

              Data are insufficient regarding use during pregnancy to adequately assess drug-associated risk of birth defects and miscarriage

              While there are insufficient human data to assess the risk of neural tube defects (NTDs) with exposure to cabotegravir during pregnancy, NTDs were associated with dolutegravir, another integrase inhibitor

              Data from a birth outcome surveillance study in Botswana showed that dolutegravir, another integrase inhibitor, was associated with increased risk of NTDs when administered at time of conception and in early pregnancy; data from clinical trials are insufficient to address this risk with cabotegravir

              Healthcare providers should discuss benefit-risk of using drug with individuals of childbearing potential or during pregnancy

              Clinical considerations

              • Cabotegravir detected in systemic circulation for up to 12 months or longer after discontinuing IM injections; therefore, consider potential for fetal exposure during pregnancy

              Lactation

              Unknown if present in human breast milk, affects human milk production, or effects on breastfed infants

              Because of potential for HIV-1 transmission (in HIV-1–negative infants), developing viral resistance (in HIV-1–positive infants), and adverse reactions in a breastfed infant similar to those seen in adults, instruct HIV-1–infected mothers not to breastfeed if they are receiving drug for the treatment of HIV-1 infection

              Due to detectable cabotegravir concentrations in systemic circulation for up to 12 months or longer after discontinuing IM injections, females should breastfeed only if the expected benefit justifies the potential risk to infant

              For uninfected mothers receiving the drug for HIV-1 PrEP, assess the benefit-risk of the drug to the infant while breastfeeding

              CDC recommends that females in the United States should not breastfeed their infants because of risk of the following

              • Postnatal HIV transmission (in HIV-negative infants)
              • Developing viral resistance (in HIV-positive infants)
              • Adverse reactions in nursing infants

              Animal data

              • Cabotegravir detected in plasma of nursing pups on lactation day 10 in rat prenatal and postnatal development study

              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

              Inhibits HIV integrase by binding to the integrase-active site and blocking the strand transfer step of retroviral DNA integration, which is essential for the HIV replication cycle

              Absorption

              PO

              • Peak plasma time: 3 hr
              • Peak plasma concentration: 8 mcg/mL
              • AUC: 145 mcg⋅h/mL

              IM

              Peak plasma time: 7 days

              • Aged ≥18 yr
                • Peak plasma concentration: 8 mcg/mL (initiation); 4 mcg/mL (continuation)
                • AUC: 1,591 mcg⋅hr/mL (initiation); 3,764 mcg⋅hr/mL (continuation)
              • Aged 12 to <18 yr (predicted pharmacokinetics)
                • Peak plasma concentration: 11.2 mcg/mL (initiation); 7.23 mcg/mL (continuation)
                • AUC: 2,123 mcg⋅hr/mL (initiation); 4,871 mcg⋅hr/mL (continuation)

              Distribution

              Protein bound: >99.8%

              Metabolism

              Metabolized by UGT1A1 (major) and UGT1A9 (minor)

              Elimination

              Half-life: 41 hr (PO); 5.6-11.5 weeks (IM)

              Excretion: Urine 27%; feces 59% (47% unchanged)

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              Administration

              Oral Administration

              Take on regular dosing schedule with a meal at the same time as rilpivirine

              Missed dose: Take as soon as remembered

              Do not stop taking the drug or run out of cabotegravir, owing risk for viral resistance

              IM Preparation

              If pack stored in refrigerator, bring to room temperature before administration (not to exceed 30ºC [86ºF])

              Inspect visually for particulate matter and discoloration before administration; vial has brown tint to glass that may limit visual inspection; discard vial if particulate matter or discoloration observed

              Shake vial vigorously so suspension looks uniform before injecting; small air bubbles are expected and acceptable

              Once suspension drawn into syringe, administer as soon as possible, but may remain in the syringe for up to 2 hr

              Do not place filled syringe in refrigerator; discard if not administered within 2 hr

              Do not mix with any other product or diluent

              Consider individual’s BMI to ensure needle length is sufficient to reach gluteus muscle

              Longer needle lengths (not included in dosing kit) may be required with higher BM (eg, >30 kg/m2) to ensure injection is administered IM as opposed to SC

              IM Administration

              Administer as single IM injection in gluteal muscle by health care provider every 2 months

              May administer injection up to 7 days before or after the date scheduled to receive injection

              Injection site

              • Ventrogluteal site recommended
              • Dorsogluteal approach (upper outer quadrant) acceptable, if preferred by healthcare professional
              • Do not administer by any other route or anatomical site

              Missed dose

              • Planned missed injection
                • ≥7 days: Daily oral cabotegravir for up to 2 consecutive months to replace 1 missed scheduled 600-mg every 2-month injection
                • Take first dose of oral PrEP ~2 months after last 600-mg IM
                • Restart injection on day oral dosing completes or within 3 days
                • For oral PrEP durations >2 months, an alternative oral regimen is recommended
              • Unplanned missed injections
                • If a scheduled injection visit is missed or delayed by >7 days and oral dosing has not been taken in the interim, clinically reassess individual to determine if resumption of injection dosing remains appropriate
              • Injection dosing recommendations after second missed injection
                • Time since first injection ≤2 months: 600 mg IM as soon as possible, then continue with q2month schedule
                • Time since first injection >2 months: Restart with 600 mg IM, followed by second 600-mg initiation injection 1 month later, then continue with q2month schedule thereafter
              • Injection dosing recommendations after third or subsequent missed injection
                • Time since last injection ≤3 months: 600 mg IM as soon as possible, then continue with q2month schedule
                • Time since last injection >3 months: Restart with 600 mg IM, followed by second 600-mg initiation injection 1 month later, then continue with q2month schedule thereafter

              Storage

              Tablets: Store below 30ºC (86ºF)

              Unopened IM suspension

              • Store at 2-25ºC (36-77ºF) in original carton until ready to use
              • Exposure up to 30ºC permitted; do not freeze
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              Images

              No images available for this drug.
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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.

              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.

              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.