afatinib (Rx)

Brand and Other Names:Gilotrif
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 20mg
  • 30mg
  • 40mg

Non-Small Cell Lung Cancer

Metastatic Non-Small Cell Lung Cancer

  • Indicated for first-line treatment in metastatic non-small cell lung cancer (NSCLC) whose tumors have nonresistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test
  • 40 mg PO qDay until disease progression or no longer tolerated by the patient
  • See also Administration and Dosing Considerations

Metastatic Squamous Non-Small Cell Lung Cancer

  • Indicated for metastatic squamous NSCLC progressing after platinum-based chemotherapy
  • 40 mg PO qDay until disease progression or no longer tolerated by the patient
  • See also Administration

Dosage Modifications

Withhold dose for any drug-related adverse reactions

  • National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade ≥3
  • Diarrhea Grade ≥2 persisting for 2 or more consecutive days while taking anti-diarrhea medication
  • Cutaneous reactions Grade 2 that are prolonged (>7 days) or intolerable
  • Renal impairment Grade ≥2
  • Resume treatment when the adverse reaction fully resolves, returns to baseline, or improves to Grade 1
  • Reinstitute afatinib at a reduced dose (eg, 10 mg/day less than the dose at which the adverse reaction occurred)

Permanently discontinue

  • Life-threatening bullous, blistering, or exfoliative skin lesions
  • Confirmed interstitial lung disease (ILD)
  • Severe drug-induced hepatic impairment
  • Persistent ulcerative keratitis
  • Symptomatic left ventricular dysfunction
  • Severe or intolerable adverse reaction occurring at a dose of 20 mg/day

Coadministration with P-gp inhibitors

  • For patients who require therapy with a P-gp inhibitor, reduce afatinib daily dose by 10 mg if not tolerated
  • Resume previous dose after P-gp inhibitor is discontinued as tolerated

Coadministration with P-gp inducers

  • For patients who require chronic therapy with a P-gp inducer, increase afatinib daily dose by 10 mg as tolerated
  • Resume the previous dose 2-3 days after P-gp inducer is discontinued

Renal impairment

  • Mild-to-moderate (CrCl 30-89 mL/min/1.73 m²): No dosage adjustment necessary
  • Severe (CrCl 15-29 mL/min/1.73 m²): 30 mg PO qDay
  • Severe (CrCl<15 mL/min/1.73 m²): Not studied

Hepatic impairment

  • Mild-to-moderate (Child Pugh A or B): No dosage adjustment necessary
  • Severe (Child Pugh C): Closely monitor and adjust dose if not tolerated

Dosing Considerations

EGFR mutation-positive metastatic NSCLC

  • Limitation of use: Safety and efficacy have not been established in patients whose tumors have resistant EGFR mutations
  • Afatinib was approved concurrently with the diagnostic companion test, therascreen EGFR RGQ PCR Kit
  • Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics

Orphan Designations

Malignant brain and CNS tumors

Pancreatic cancer

Orphan sponsor

  • Boehringer Ingelheim Pharmaceuticals, Inc; 900 Ridgebury Road, PO Box 368; Ridgefield, CT 06877-0368

Safety and efficacy not established

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Interactions

Interaction Checker

and afatinib

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              Serious - Use Alternative (59)

              • aminolevulinic acid oral

                aminolevulinic acid oral, afatinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • aminolevulinic acid topical

                afatinib, aminolevulinic acid topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.

              • amiodarone

                amiodarone increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • atorvastatin

                atorvastatin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • carbamazepine

                carbamazepine decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • carvedilol

                carvedilol increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • clarithromycin

                clarithromycin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • cyclosporine

                cyclosporine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • darunavir

                darunavir increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • dipyridamole

                dipyridamole increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • dronedarone

                dronedarone increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • edoxaban

                afatinib will increase the level or effect of edoxaban by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Dose adjustment may be required with strong P-gp inhibitors. DVT/PE treatment: Decrease dose to 30 mg PO once daily. NVAF: No dose reduction recommended

              • erdafitinib

                erdafitinib will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration unavoidable, separate administration by at least 6 hr before or after administration of P-gp substrates with narrow therapeutic index.

              • erythromycin base

                erythromycin base increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • erythromycin lactobionate

                erythromycin lactobionate increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • erythromycin stearate

                erythromycin stearate increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • etravirine

                etravirine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • fosphenytoin

                fosphenytoin decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • grapefruit

                grapefruit increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • itraconazole

                itraconazole increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • ketoconazole

                ketoconazole increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • lapatinib

                lapatinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • lasmiditan

                lasmiditan increases effects of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

              • lopinavir

                lopinavir increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • lovastatin

                lovastatin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • mefloquine

                mefloquine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • methyl aminolevulinate

                afatinib, methyl aminolevulinate. Either increases levels of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Each drug may increase the photosensitizing effect of the other.

              • mifepristone

                mifepristone increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • nefazodone

                nefazodone will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

              • nelfinavir

                nelfinavir increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • nifedipine

                nifedipine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • nilotinib

                nilotinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • palifermin

                palifermin increases toxicity of afatinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

              • paliperidone

                paliperidone increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • phenobarbital

                phenobarbital decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • phenytoin

                phenytoin decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • ponatinib

                ponatinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • posaconazole

                posaconazole increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • progesterone micronized

                progesterone micronized increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • propafenone

                propafenone increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • propranolol

                propranolol increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • quinidine

                quinidine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • quinine

                quinine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • ranolazine

                ranolazine increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • rifampin

                rifampin decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • riociguat

                afatinib will increase the level or effect of riociguat by decreasing metabolism. Avoid or Use Alternate Drug. Coadministration of riociguat (substrate of CYP isoenzymes 1A1, 2C8, 3A, 2J2) with strong CYP inhibitors may require a decreased initial dose of 0.5 mg PO TID; monitor for signs of hypotension and reduce dose if needed

              • ritonavir

                ritonavir increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • saquinavir

                saquinavir increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • simvastatin

                simvastatin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • sotorasib

                sotorasib will decrease the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.

              • St John's Wort

                St John's Wort decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • sunitinib

                sunitinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • tacrolimus

                tacrolimus increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • tamoxifen

                tamoxifen increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • tepotinib

                tepotinib will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.

              • tipranavir

                tipranavir decreases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Increase afatinib daily dose by 10 mg as tolerated if chronic therapy with P-gp inducer required; resume previous afatinib dose 2-3 days after P-gp inducer discontinued.

              • venetoclax

                afatinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.

              • verapamil

                verapamil increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              Monitor Closely (21)

              • azithromycin

                azithromycin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

              • berotralstat

                berotralstat will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.

              • betrixaban

                afatinib increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.

              • ceritinib

                afatinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • cholera vaccine

                afatinib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.

              • dabigatran

                afatinib will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Atrial fibrillation: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <30 mL/min. DVT/PE treatment: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <50 mL/min

              • dengue vaccine

                afatinib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.

              • dichlorphenamide

                dichlorphenamide and afatinib both decrease serum potassium. Use Caution/Monitor.

              • elagolix

                elagolix will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • eliglustat

                eliglustat increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.

              • fostamatinib

                fostamatinib will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp substrates. Monitor for toxicities of the P-gp substrate drug that may require dosage reduction when given concurrently with fostamatinib.

              • glecaprevir/pibrentasvir

                afatinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

                glecaprevir/pibrentasvir will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.

              • istradefylline

                istradefylline will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.

              • lonafarnib

                lonafarnib will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.

              • naldemedine

                afatinib increases levels of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with P-gp inhibitors.

              • nintedanib

                afatinib increases levels of nintedanib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. If nintedanib adverse effects occur, management may require interruption, dose reduction, or discontinuation of therapy .

              • rifaximin

                afatinib increases levels of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • sarecycline

                sarecycline will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.

              • siponimod

                siponimod and afatinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • stiripentol

                stiripentol will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

              • tucatinib

                tucatinib will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.

              Minor (0)

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                Adverse Effects

                All grades included unless otherwise noted

                >10%

                Diarrhea (75-96%)

                Rash/dermatitis acneiform (70-90%)

                Stomatitis (30-71%)

                Paronychia (11-58%)

                Increased ALT (10-54%)

                Decreased creatinine clearance (49%)

                Increase alkaline phosphate (34-51%)

                Increased AST (7-46%)

                Decreased lymphocytes (38%)

                Dry skin (31%)

                Decreased potassium (11-30%)

                Decreased appetite (25%)

                Pruritus (21%)

                Nausea (21%)

                Epistaxis (17%)

                Decreased weight (17%)

                Rash/dermatitis acneiform, Grade 3 or 4 (7-16%)

                Increased bilirubin (3-16%)

                Diarrhea, Grade 3 or 4 (11-15%)

                Vomiting (13%)

                Cystitis (13%)

                Decreased WBC (12%)

                Cheilitis (12%)

                Rhinorrhea (11%)

                Paronychia, Grade 3 or 4 (1-11%)

                1-10%

                Stomatitis, Grade 3 or 4 (9%)

                Decreased lymphocytes, Grade 3 or 4 (9%)

                Decreased potassium, Grade 3 or 4 (1-8%)

                Stomatitis, Grade 3 or 4 (4%)

                Decreased appetite, Grade 3 or 4 (3%)

                Increased AST, Grade 3 or 4 (1-3%)

                Increase alkaline phosphate, Grade 3 or 4 (2-3%)

                Decreased creatinine clearance (2%)

                Nausea, Grade 3 or 4 (2%)

                Increased ALT, Grade 3 or 4 (1-2%)

                Decreased WBC, Grade 3 or 4 (1%)

                Vomiting, Grade 3 or 4 (1%)

                Cystitis, Grade 3 or 4 (1%)

                Decreased weight, Grade 3 or 4 (1%)

                Increased bilirubin, Grade 3 or 4 (1%)

                <1%

                Keratitis (0.8%)

                Postmarketing Reports

                Pancreatitis

                Toxic epidermal necrolysis/Stevens Johnson syndrome

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                Warnings

                Contraindications

                None

                Cautions

                May cause diarrhea that results in dehydration with or without renal impairment; some reported cases were fatal; withhold therapy for severe and prolonged diarrhea not responsive to antidiarrheal agents (see Dosage Modifications)

                Postmarketing cases consistent with toxic epidermal necrolysis (TEN), including bullous and exfoliative skin disorders, and Stevens Johnson syndrome (SJS) reported; discontinue if life-threatening bullous, blistering, or exfoliating lesions occur; withhold therapy for severe and prolonged cutaneous reactions (see Dosage Modifications)

                May increase risk for sunburn/phototoxicity; may worsen rash or acne; caution patients to limit sun exposure and where sunscreen and protective clothing

                Interstitial lung disease (ILD) or ILD-like adverse reactions reported (eg, lung infiltration, pneumonitis, acute respiratory distress syndrome, alveolitis allergy) occurred in 1%, of these, 0.4% were fatal; discontinue therapy if ILD diagnosed (see Dosage Modifications)

                Hepatotoxicity reported; monitor with periodic liver testing; withhold or discontinue therapy for severe or worsening liver tests

                Keratitis, characterized as acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye occurred in 0.8%; withhold or discontinue therapy for confirmed ulcerative keratitis

                Gastrointestinal perforation, including fatal cases, reported; patients receiving concomitant corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs) or anti-angiogenic agents, or patients with increasing age or who have an underlying history of gastrointestinal ulceration, underlying diverticular disease or bowel metastases may be at increased risk of perforation; permanently discontinue therapy in patients who develop gastrointestinal perforation

                Based on its mechanism of action, afatinib can cause fetal harm; advise pregnant women and females of reproductive potential of potential risk to fetus and to use effective contraception (see Pregnancy)

                Drug interactions overview

                • See also Dosage Modifications
                • Coadministration of P-gp inhibitors (eg, ritonavir, cyclosporine A, ketoconazole, itraconazole, erythromycin, verapamil, quinidine, tacrolimus, nelfinavir, saquinavir, and amiodarone) with afatinib can increase exposure to afatinib
                • Coadministration of P-gp inducers (eg, rifampicin, carbamazepine, phenytoin, phenobarbital, and St. John’s wort) with afatinib can decrease exposure to afatinib
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                Pregnancy & Lactation

                Pregnancy

                Based on findings from animal studies and mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; there are no available data on use in pregnant women; administration to pregnant rabbits during organogenesis at exposures approximately 0.2 times exposure in humans at recommended dose of 40 mg daily resulted in embryotoxicity and, in rabbits showing maternal toxicity, increased abortions at late gestational stages; advise pregnant women of potential risk to a fetus

                Contraception

                • Advise females of reproductive potential to use effective contraception during treatment and for at least 2 weeks after the last dose of afatinib
                • Based on results from an animal fertility study, afatinib may reduce fertility in females and males of reproductive potential
                • Unknown if the effects on fertility are reversible

                Lactation

                There are no data on presence of afatinib in human milk or effects on breastfed infant or on milk production; presence shown in milk of lactating rats; because of potential for serious adverse reactions in nursing infants, advise a lactating woman not to breastfeed during treatment and for 2 weeks after final 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

                Covalently binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation, resulting in downregulation of ErbB signaling

                Demonstrates inhibition of autophosphorylation and in vitro proliferation of cell lines expressing wild-type EGFR or those expressing selected EGFR exon 19 deletion mutations or exon 21 L858R mutations, including some with a secondary T790M mutation

                In addition, afatinib inhibited in vitro proliferation of cell lines overexpressing HER2

                Absorption

                Bioavailability: 92%

                Peak plasma time: 2-5 hr

                High fat meal decreases Cmax by 50% and AUC by 39% relative to the fasted condition (take on empty stomach)

                Distribution

                Protein bound: 95%

                Metabolism

                Covalent adducts to proteins are the major circulating metabolites of afatinib and enzymatic metabolism of afatinib is minimal

                Afatinib is a P-gp substrate and an inhibitor; BCRP substrate and an inhibitor

                Elimination

                Half-life: 37 hr

                Excretion: 85% (feces); 4% (urine)

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                Administration

                Oral Administration

                Take PO on empty stomach, at least 1 hr before or 2 hr after a meal

                Missed dose: Do not take a missed dose within 12 hr of the next dose

                Storage

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

                Dispense in the original container to protect from exposure to high humidity and light

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Gilotrif oral
                -
                30 mg tablet
                Gilotrif oral
                -
                40 mg tablet
                Gilotrif oral
                -
                20 mg tablet

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                Patient Education
                afatinib oral

                AFATINIB - ORAL

                (a-FA-ti-nib)

                COMMON BRAND NAME(S): Gilotrif

                USES: Afatinib is used to treat a certain type of lung cancer (non-small cell lung cancer). It belongs to a class of drugs known as kinase inhibitors. It works by slowing or stopping the growth of cancer cells. It binds to a certain protein (epidermal growth factor receptor-EGFR) in some tumors.

                HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking afatinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually once daily at least 1 hour before or 2 hours after a meal.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

                SIDE EFFECTS: Mouth sores, pain/redness/swelling of lips, dry/itchy skin, acne, nose bleed, runny nose, nausea/vomiting, or loss of appetite may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Diarrhea is a common side effect. Drink plenty of fluids as directed by your doctor to reduce your risk of dehydration. Your doctor may prescribe anti-diarrhea medication (such as loperamide) to control your symptoms. Tell your doctor right away if you develop: severe or persistent diarrhea, symptoms of dehydration (such as unusual decreased urination, unusual dry mouth/thirst, fast heartbeat, or dizziness/lightheadedness).Tell your doctor right away if you have any serious side effects, including: signs of eye disease (such as vision changes, eye redness/pain, light sensitivity, eye discharge), signs of low level of potassium in the blood (such as muscle cramps, weakness, irregular heartbeat), signs of bladder infection (such as burning/pain when you urinate, urgent or frequent urination, fever), signs of skin infection around nails/toenails (such as skin irritation/redness around the nail, change in nail color).Get medical help right away if you have any very serious side effects, including: symptoms of lung problems (such as trouble breathing, chest pain), symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain).Afatinib may rarely cause serious (possibly fatal) liver disease or tear in the stomach or intestinal wall (perforation). Get medical help right away if you have symptoms such as: dark urine, persistent nausea/vomiting/loss of appetite, stomach/abdominal pain, yellowing eyes/skin.Afatinib can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                PRECAUTIONS: Before taking afatinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, liver problems, stomach/intestinal problems (such as ulcers, diverticular disease), eye disease (such as severe dry eyes, keratitis), use of contact lenses.This drug may cause blurred vision. Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.This medication may make you more sensitive to the sun. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Tell your doctor right away if you get sunburned or have skin blisters/redness.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication is not recommended for use during pregnancy. It may harm an unborn baby. It is important to prevent pregnancy while taking this medication and for at least 2 weeks after treatment. Females must use reliable forms of birth control (such as condoms, birth control pills) during treatment and for at least 2 weeks after the end of treatment. If you become pregnant or think you may be pregnant, tell your doctor right away.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for 2 weeks after stopping this drug is not recommended. Consult your doctor before breast-feeding.

                DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

                OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe nausea/vomiting/stomach pain, severe dizziness, weakness.

                NOTES: Do not share this medication with others.Certain laboratory tests should be performed before you start treatment to check for the EGFR protein in your tumor.Laboratory and/or medical tests (such as liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

                MISSED DOSE: If you miss a dose and it has been less than 12 hours since your usual dose time, take it as soon as you remember. If it has been more than 12 hours since your usual dose time, then skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

                STORAGE: Store at room temperature in the original container away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

                Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

                IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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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.