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Nerlynx Dosage

Generic name: NERATINIB MALEATE 40mg
Dosage form: tablet

Medically reviewed on July 5, 2018.

Antidiarrheal Prophylaxis

Antidiarrheal prophylaxis is recommended during the first 2 cycles (56 days) of treatment and should be initiated with the first dose of NERLYNX [ see Dosage and Administration ( 2.3) and Warnings and Precautions ( 5.1) ].

Instruct patients to take loperamide as directed in Table 1, titrating to 1-2 bowel movements per day.

Table 1: Loperamide Prophylaxis
Time on NERLYNX Dose Frequency
Weeks 1-2 (days 1 - 14) 4 mg Three times daily
Weeks 3-8 (days 15 - 56) 4 mg Twice daily
Weeks 9-52 (days 57 – 365) 4 mg As needed (not to exceed 16 mg per day)

Additional antidiarrheal agents may be required to manage diarrhea in patients with loperamide-refractory diarrhea. NERLYNX dose interruptions and dose reductions may also be required to manage diarrhea [ see Dosage and Administration ( 2.3) ].

Recommended Dose and Schedule

The recommended dose of NERLYNX is 240 mg (six tablets) given orally once daily with food, continuously for one year.

Instruct patients to take NERLYNX at approximately the same time every day. NERLYNX tablets should be swallowed whole (tablets should not be chewed, crushed, or split prior to swallowing).

If a patient misses a dose, do not replace missed dose, and instruct the patient to resume NERLYNX with the next scheduled daily dose.

Dose Modifications

Dose Modifications for Adverse Reactions

NERLYNX dose modification is recommended based on individual safety and tolerability. Management of some adverse reactions may require dose interruption and/or dose reduction as shown in Table 2 to Table 5. Discontinue NERLYNX for patients who fail to recover to Grade 0-1 from treatment-related toxicity, for toxicities that result in a treatment delay > 3 weeks, or for patients that are unable to tolerate 120 mg daily. Additional clinical situations may result in dose adjustments as clinically indicated (e.g. intolerable toxicities, persistent Grade 2 adverse reactions, etc.).

Table 2: NERLYNX Dose Modifications for Adverse Reactions
Dose Level NERLYNX Dose
Recommended starting dose 240 mg daily
First dose reduction 200 mg daily
Second dose reduction 160 mg daily
Third dose reduction 120 mg daily
Table 3: NERLYNX Dose Modifications and Management – General Toxicities 1

1 Refer to Table 4 and Table 5 below for management of diarrhea and hepatotoxicity

2 Per CTCAE v4.0
Severity of Toxicity2 Action
Grade 3 Hold NERLYNX until recovery to Grade ≤ 1 or baseline within 3 weeks of stopping treatment. Then resume NERLYNX at the next lower dose level.
Grade 4 Discontinue NERLYNX permanently.

Dose Modifications for Diarrhea

Diarrhea management requires the correct use of antidiarrheal medication, dietary changes, and appropriate dose modifications of NERLYNX. Guidelines for adjusting doses of NERLYNX in the setting of diarrhea are shown in Table 4.

Table 4: Dose Modifications for Diarrhea
Severity of Diarrhea1 Action

1 Per CTCAE v4.0

2 Complicated features include dehydration, fever, hypotension, renal failure, or Grade 3 or 4 neutropenia

3 Despite being treated with optimal medical therapy
  • Grade 1 diarrhea [increase of < 4 stools per day over baseline]
  • Grade 2 diarrhea [increase of 4-6 stools per day over baseline] lasting < 5 days
  • Grade 3 diarrhea [increase of ≥ 7 stools per day over baseline; incontinence; hospitalization indicated; limiting self-care activities of daily living] lasting < 2 days
  • Adjust antidiarrheal treatment
  • Diet modifications
  • Fluid intake of ~2L should be maintained to avoid dehydration
  • Once event resolves to ≤ Grade 1 or baseline, start loperamide 4 mg with each subsequent NERLYNX administration.
  • Any grade with complicated features 2
  • Grade 2 diarrhea lasting five days or longer 3
  • Grade 3 diarrhea lasting longer than 2 days 3
  • Interrupt NERLYNX treatment
  • Diet modifications
  • Fluid intake of ~2L should be maintained to avoid dehydration
  • If diarrhea resolves to Grade 0-1 in one week or less, then resume NERLYNX treatment at the same dose.
  • If diarrhea resolves to Grade 0-1 in longer than one week, then resume NERLYNX treatment at reduced dose (see Table 2).
  • Once event resolves to ≤ Grade 1 or baseline, start loperamide 4 mg with each subsequent NERLYNX administration.
  • Grade 4 diarrhea [Life-threatening consequences; urgent intervention indicated]
  • Permanently discontinue NERLYNX treatment
  • Diarrhea recurs to Grade 2 or higher at 120 mg per day
  • Permanently discontinue NERLYNX treatment

Dose Modifications for Hepatic Impairment

Reduce the NERLYNX starting dose to 80 mg in patients with severe hepatic impairment (Child Pugh C). No dose modifications are recommended for patients with mild to moderate hepatic impairment (Child Pugh A or B) [ see Use in Specific Populations ( 8.6) and Clinical Pharmacology ( 12.3) ].

Dose Modifications for Hepatotoxicity

Guidelines for dose adjustment of NERLYNX in the event of liver toxicity are shown in Table 5. Patients who experience ≥ Grade 3 diarrhea requiring IV fluid treatment or any signs or symptoms of hepatotoxicity, such as worsening of fatigue, nausea, vomiting, right upper quadrant pain or tenderness, fever, rash, or eosinophilia, should be evaluated for changes in liver function tests. Fractionated bilirubin and prothrombin time should also be collected during hepatotoxicity evaluation [ see Warnings and Precautions ( 5.2) ].

Table 5: Dose Modifications for Hepatotoxicity
Severity of Hepatoxicity1 Action

1 Per CTCAE v4.0
  • Grade 3 ALT (>5-20x ULN)
    OR
  • Grade 3 bilirubin (>3-10x ULN)
  • Hold NERLYNX until recovery to ≤ Grade 1
  • Evaluate alternative causes
  • Resume NERLYNX at the next lower dose level if recovery to ≤ Grade 1 occurs within 3 weeks. If Grade 3 ALT or bilirubin occurs again despite one dose reduction, permanently discontinue NERLYNX
  • Grade 4 ALT (>20x ULN)
    OR
  • Grade 4 bilirubin (>10x ULN)
  • Permanently discontinue NERLYNX
  • Evaluate alternative causes

Concomitant Use with Gastric Acid Reducing Agents

Proton pump inhibitors (PPI): Avoid concomitant use with NERLYNX [ see Drug Interactions ( 7.1) ].

H2-receptor antagonists: Take NERLYNX at least 2 hours before the next dose of the H 2-receptor antagonist or 10 hours after the H2-receptor antagonist [ see Drug Interactions ( 7.1) ].

Antacids: Separate dosing of NERLYNX by 3 hours after antacids [ see Drug Interactions ( 7.1) ].

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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