NERLYNX Film-coated tablet (2020)

Βιβλιογραφική αναφορά

Συγγραφείς

Puma Biotechnology, Inc.

Λέξεις κλειδιά

70437-240

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1. Indications and Usage

1.1 Extended Adjuvant Treatment of Early-Stage Breast Cancer NERLYNX as a single agent is indicated for the extended adjuvant treatment of adult patients with early-stage human epidermal growth factor ...

2. Dosage and Administration

2.1 Antidiarrheal Prophylaxis Administer antidiarrheal prophylaxis during the first 56 days of treatment and initiate with the first dose of NERLYNX [see Warnings and Precautions (5.1) and Adverse ...

3. Dosage Forms and Strengths

Tablets: 40 mg neratinib (equivalent to 48.31 mg of neratinib maleate). Film-coated, red, oval shaped and debossed with W104 on one side and plain on the other side.

4. Contraindications

None.

5. Warnings and Precautions

5.1 Diarrhea Severe diarrhea and sequelae, such as dehydration, hypotension, and renal failure occurred during treatment with NERLYNX. Diarrhea was reported in 95% of NERLYNX-treated patients in ExteNET, ...

6. Adverse Reactions

The following clinically significant adverse reactions are described elsewhere in the labeling: Diarrhea [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

7. Drug Interactions

7.1 Effect of Other Drugs on NERLYNX Table 10 includes drug interactions that affect the pharmacokinetics of neratinib. Table 10. Drug Interactions That Affect Neratinib: Gastric Acid Reducing Agents ...

8.1. Pregnancy

Risk Summary Based on findings from animal studies and the mechanism of action, NERLYNX can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1)]. There are ...

8.2. Lactation

Risk Summary No data are available regarding the presence of neratinib or its metabolites in human milk or its effects on the breastfed infant or on milk production. Because of the potential for serious ...

8.3. Females and Males of Reproductive Potential

Pregnancy Based on animal studies, NERLYNX can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1)]. Females of reproductive potential should have a pregnancy ...

8.4. Pediatric Use

The safety and efficacy of NERLYNX in pediatric patients has not been established.

8.5. Geriatric Use

In the ExteNET trial, in the NERLYNX arm; 1236 patients were <65 years, 172 patients were ≥65 years, of whom 25 patients were 75 years or older. There was a higher frequency of treatment discontinuations ...

8.6. Hepatic Impairment

No dose modifications are recommended for patients with mild to moderate hepatic impairment (Child Pugh A or B). Patients with severe, pre-existing hepatic impairment (Child Pugh Class C) experienced a ...

10. Overdosage

There is no specific antidote, and the benefit of hemodialysis in the treatment of NERLYNX overdose is unknown. In the event of an overdose, administration should be withheld and general supportive measures ...

11. Description

NERLYNX (neratinib) immediate release, film-coated tablets for oral administration contain 40 mg of neratinib, equivalent to 48.31 mg neratinib maleate. Neratinib is a member of the 4-anilino quinolidine ...

12.1. Mechanism of Action

Neratinib is an intracellular kinase inhibitor that irreversibly binds to epidermal growth factor receptor (EGFR), HER2, and HER4. In vitro, neratinib reduces EGFR and HER2 autophosphorylation, ...

12.2. Pharmacodynamics

Cardiac Electrophysiology The effect of NERLYNX on the QTc interval was evaluated in a randomized, placebo, and positive-controlled, double-blind, single-dose, crossover study in 60 healthy subjects. At ...

12.3. Pharmacokinetics

Neratinib exhibits a non-linear PK profile with less than dose proportional increase of AUC with the increasing daily dose over the range of 40 to 400 mg. Absorption The neratinib and major active metabolites ...

13.1. Carcinogensis, Mutagenesis, Impairment of Fertility

A two-year carcinogenicity study was conducted in rats at oral neratinib doses of 1, 3, and 10 mg/kg/day. Neratinib was not carcinogenic in male and female rats at exposure levels >25 times the AUC in ...

14. Clinical Studies

14.1 Extended Adjuvant Treatment of Early Stage Breast Cancer The safety and efficacy of NERLYNX were investigated in the ExteNET trial (NCT00878709), a multicenter, randomized, double-blind, placebo-controlled ...

16.1. How Supplied

NERLYNX 40 mg film-coated tablets are red, oval shaped and debossed with W104 on one side and plain on the other side. NERLYNX is available in: Bottles of 180 tablets: NDC 70437-240-18 Bottles of 126 tablets: ...

16.2. Storage and Handling

Store at controlled room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Patient Information). Diarrhea: Inform patients that NERLYNX has been associated with diarrhea, which may be severe in some ...