Product Information
Registration Status: ActiveSIN15861P
NERLYNX FILM-COATED TABLETS 40 MG is approved to be sold in Singapore with effective from 2019-11-25. It is marketed by SPECIALISED THERAPEUTICS ASIA PTE LTD, with the registration number of SIN15861P.
This product contains Neratinib 40 mg in the form of TABLET, FILM COATED. It is approved for ORAL use.
This product is manufactured by Excella GmbH & Co. KG in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Neratinib was approved in July 2017 for use as an extended adjuvant therapy in Human Epidermal Growth Factor Receptor 2 (HER2) positive breast cancer. Approval was granted to Puma Biotechnology Inc. for the tradename Nerlynx. Neratinib is currently under investigation for use in many other forms of cancer.
Indication
For use as an extended adjuvant treatment in adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy [FDA Label].
Mechanism of Action
Neratinib binds to and irreversibly inhibits EGFR, HER2, and HER4 [FDA Label]. This prevents auotphoshorylation of tyrosine residues on the receptor and reduces oncogenic signalling through the mitogen-activated protein kinase and Akt pathways.
Pharmacokinetics
- Absorption
- Neratinib and its major active metabolites M3. M6, and M7 have a Tmax of 2-8 h [FDA Label]. Administration with a high fat meal increases Cmax by 1.7-fold and total exposure by 2.2-fold. Administration with a standard meal increases Cmax by 1.2-fold and total exposure by 1.1-fold. Administration with gastric acid reducing agents such as proton pump inhibitors reduces Cmax by 71% and total exposure by 65%.
- Distribution
- The apparent volume of distribution at steady state is 6433 L [FDA Label].
- Metabolism
- Neratinib is mainly undergoes metabolism via CYP3A4 [FDA Label]. It is also metabolized by flavin-containing monooxygenase to a lesser extent. The systemic exposures of neratinib's active metabolites M3, M6, M7, and M11 are 15%, 33%, 22%, and 4%.
- Elimination
Clearance
The total clearance during multiple doses is 216 L/h for after the first dose and 281 L/h during steady state [FDA Label].
Toxicity
Use of neratinib may produce diarrhea and hepatotoxicity as clinically significant adverse effects [FDA Label]. Serious adverse reactions in the neratinib arm of the clinical trials included diarrhea (1.6%), vomiting (0.9%), dehydration (0.6%), cellulitis (0.4%), renal failure (0.4%), erysipelas (0.4%), alanine aminotransferase increase (0.3%), aspartate aminotransferase increase (0.3%), nausea (0.3%), fatigue (0.2%), and abdominal pain (0.2%).
Active Ingredient/Synonyms
Neratinib | Neratinib |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.