Medically reviewed by Drugs.com. Last updated on Aug 12, 2020.
Applies to the following strengths: 40 mg
Usual Adult Dose for:
Additional dosage information:
Usual Adult Dose for Breast Cancer - Adjuvant
240 mg orally once a day continuously for 1 year
NOTE: Antidiarrheal prophylaxis is recommended during the first 2 cycles (56 days) of therapy and should be initiated with the first dose. Titrate loperamide to 1 to 2 bowel movements per day.
MANUFACTURER SUGGESTED PROPHYLACTIC LOPERAMIDE DOSING:
-Weeks 1 and 2 (days 1 through 14): 4 mg orally 3 times a day
-Weeks 3 through 8 (days 15 through 56): 4 mg orally 2 times a day
-Weeks 9 through 52 (days 57 through 365): 4 mg as needed (not to exceed 16 mg per day)
Use: For the extended adjuvant treatment of adult patients with early stage HER2-overexpressed/amplified breast cancer (to follow adjuvant trastuzumab-based therapy)
Renal Dose Adjustments
There are no dosage recommendations provided in the manufacturer product information; however, renal function does not have a clinically significant effect on the pharmacokinetics of this drug.
Liver Dose Adjustments
DOSE MODIFICATIONS FOR HEPATIC IMPAIRMENT:
-Mild to moderate hepatic impairment (Child Pugh A or B): No adjustment recommended.
-Severe hepatic impairment (Child Pugh C): Reduce the starting dose to 80 mg.
DOSE MODIFICATIONS FOR HEPATOTOXICITY:
-Grade 3 ALT (greater than 5 to 20 times upper limit of normal [ULN]) OR Grade 3 bilirubin (greater than 3 to 10 x ULN): Withhold therapy until recovery to Grade 1 or less; evaluate alternative causes; resume therapy at the next lower dose level if recovery to Grade 1 or less occurs within 3 weeks; if Grade 3 ALT or bilirubin occurs again despite one dose reduction, permanently discontinue therapy.
-Grade 4 ALT (greater than 20 x ULN) OR Grade 4 bilirubin (greater than 10 x ULN): Permanently discontinue therapy; evaluate alternative causes
DOSE MODIFICATIONS FOR ADVERSE REACTIONS:
-Dose modification is recommended based on tolerability.
-Management of some adverse reactions may require dose interruption and/or dose reduction.
-Discontinue therapy in patients who fail to recover to Grade 0 to 1 from therapy-related toxicity, for toxicities that result in therapy delay longer than 3 weeks, or who cannot tolerate 120 mg daily.
Dose Modifications for Adverse Reactions:
-Recommended starting dose: 240 mg daily
-First dose reduction: 200 mg daily
-Second dose reduction: 160 mg daily
-Third dose reduction: 120 mg daily
DOSE MODIFICATIONS FOR TOXICITY:
-Grade 3: Withhold therapy until recovery to Grade 1 or less or baseline within 3 weeks of stopping therapy; resume at the next lower dose level.
-Grade 4: Permanently discontinue therapy.
DOSE MODIFICATIONS FOR DIARRHEA:
-Grade 1 (increase of less than 4 stools per day over baseline) OR Grade 2 (increase of 4 to 6 stools per day over baseline) lasting less than 5 days OR Grade 3 (increase of 7 or more stools per day over baseline; incontinence; hospitalization indicated; limiting self-care activities of daily living) lasting 2 days or less: Adjust antidiarrheal treatment and make diet modifications; fluid intake of approximately 2L should be maintained to avoid dehydration; when event resolves to Grade 1 or less or baseline, start loperamide 4 mg with each subsequent dose of this drug.
-Any grade with complicated features (e.g., dehydration, fever, hypotension, renal failure, Grade 3 or 4 neutropenia) OR Grade 2 diarrhea lasting 5 days or longer (despite treatment) OR Grade 3 diarrhea lasting longer than 2 days (despite treatment): Withhold therapy and make diet modifications; fluid intake of approximately 2L should be maintained to avoid dehydration; if diarrhea resolves to Grade 0 or 1 in one week or less, then resume therapy at the same dose; if diarrhea resolves to Grade 0 or 1 in longer than one week, then resume therapy at reduced dose; when event resolves to Grade 1 or less or baseline, start loperamide 4 mg with each dose of this drug.
-Grade 4 (life-threatening consequences; urgent intervention indicated): Permanently discontinue therapy.
Diarrhea that recurs to Grade 2 or higher at 120 mg per day: Permanently discontinue therapy.
GASTRIC ACID REDUCING AGENTS:
-Concomitant use of this drug with a proton pump inhibitor, H 2-receptor antagonist, or antacid may decrease neratinib plasma concentration. Decreased neratinib AUC may reduce its activity. Lansoprazole (PPI) resulted in a decrease of neratinib C max by 71% and AUC by 65%.
-PPIs: Avoid concomitant use.
-H2-receptor antagonists: Take neratinib at least 2 hours before the next dose of the H2-receptor antagonist or 10 hours after the H2-receptor antagonist.
-Antacids: Separate neratinib dosing by 3 hours after antacids.
STRONG AND MODERATE CYP450 3A4 INHIBITORS:
-Concomitant use of neratinib with a strong CYP450 3A4 inhibitor (ketoconazole) increased neratinib C max by 321% and AUC by 481%.
-Concomitant use of neratinib with other strong or moderate CYP450 3A4 inhibitors may increase neratinib concentrations.
-Increased neratinib concentrations may increase the risk of toxicity.
-Avoid concomitant use of neratinib with strong or moderate CYP450 3A4 inhibitors.
STRONG OR MODERATE CYP450 3A4 INDUCERS:
-Concomitant use of neratinib with a strong CYP450 3A4 inducer (rifampin) reduced neratinib C max by 76% and AUC by 87%.
-Concomitant use of neratinib with other strong or moderate CYP450 3A4 inducers may decrease neratinib concentrations.
-Decreased neratinib AUC may reduce its activity.
-Avoid concomitant use of neratinib with strong or moderate CYP450 3A4 inducers.
Safety and efficacy have not been established in patients younger than 18 years.
Consult WARNINGS section for additional precautions.
Data not available
-This drug should be taken with food at approximately the same time every day.
-Swallow tablets whole; do not chew, crush, or split tablets.
-Do not replace a missed dose; resume therapy with the next scheduled dose.
-Antidiarrheal prophylaxis with loperamide is recommended during the first 2 cycles (56 days) of therapy and should be initiated with the first dose and titrated to 1 to 2 bowel movements per day.
-Additional antidiarrheal agents may be needed to manage diarrhea in patients with loperamide-refractory diarrhea.
-Dose interruption or reduced doses of this drug may be required to manage diarrhea.
-Store at controlled room temperature: 20C to 25C (68F to 77 F); excursions permitted to 15C to 30C (59F to 86 F).
-Overdosage: No specific antidote; benefit of hemodialysis is unknown.
-Gastrointestinal: Diarrhea (throughout treatment); stool cultures (as clinically indicated)
-Hepatic: Total bilirubin, AST, ALT, alkaline phosphatase (prior to treatment initiation, monthly for the first 3 months of treatment, then every 3 months during treatment and as clinically indicated); fractionated bilirubin and prothrombin time (as clinically indicated)
-Avoid grapefruit products during therapy with this drug.
-This drug may cause side effects including fatigue and muscle spasms; avoid potentially dangerous activities such as driving and operating machinery until you know how this drug affects you.
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