Generic Name and Formulations:
Neratinib 40mg; tabs.
Indications for NERLYNX:
Extended adjuvant treatment of early stage HER2-overexpressed/amplified breast cancer following adjuvant trastuzumab-based therapy.
Initiate antidiarrheal prophylaxis (loperamide) with the first dose and continue during the first 2 treatment cycles (56 days); see full labeling. Swallow whole. Take with food. 240mg once daily for 1 year. Severe hepatic impairment (Child-Pugh C): reduce initial dose to 80mg. Dose modifications for adverse reactions: First dose reduction: 200mg/day; Second dose reduction: 160mg/day; Third dose reduction: 120mg/day; discontinue if unable to tolerate 120mg/day. Dose modifications for diarrhea, hepatotoxicity, or other general toxicities: see full labeling.
Monitor and treat diarrhea as needed; interrupt and reduce subsequent doses if severe diarrhea with dehydration occurs. Perform stool cultures as clinically indicated to exclude infectious causes of Grade 3/4 or any grade of diarrhea with complications. Measure total bilirubin, AST/ALT, alkaline phosphatase prior to initiation, monthly for the first 3 months, then every 3 months during treatment and as clinically indicated. Severe hepatic impairment: reduce dose. Embryo-fetal toxicity. Use effective contraception during therapy and for at least 1 month (females) or 3 months (males) after last dose. Pregnancy; exclude status prior to initiation. Nursing mothers: not recommended (during and for at least 1 month after last dose).
Avoid concomitant PPIs, H2-receptor antagonists, strong or moderate CYP3A4 inhibitors (eg, boceprevir, clarithromycin, cobicistat, conivaptan, danoprevir/ritonavir, diltiazem, elvitegravir/ritonavir, grapefruit juice, idelalisib, indinavir/ritonavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, paritaprevir/ritonavir and [ombitasvir and/or dasabuvir], posaconazole, ritonavir, saquinavir/ritonavir, tipranavir/ritonavir, troleandomycin, voriconazole, aprepitant, cimetidine, ciprofloxacin, clotrimazole, crizotinib, cyclosporine, dronedarone, erythromycin, fluconazole, fluvoxamine, imatinib, tofisopam, verapamil), and strong or moderate CYP3A4 inducers (eg, carbamazepine, enzalutamide, mitotane, phenytoin, rifampin, St. John's wort, bosentan, efavirenz, etravirine, modafinil). Separate dosing by 3hrs after antacids. Increased cardiotoxicity risk with digoxin. May inhibit transport of P-gp substrates (eg, dabigatran, fexofenadine).
Diarrhea, nausea, abdominal pain, fatigue, vomiting, rash, stomatitis, decreased appetite, muscle spasms, dyspepsia, AST/ALT increase, nail disorder, dry skin, abdominal distention, weight decreased, urinary tract infection; hepatotoxicity.