Product Information
Registration Status: ActiveSIN15219P
COTELLIC FILM-COATED TABLET 20mg is approved to be sold in Singapore with effective from 2017-04-21. It is marketed by ROCHE SINGAPORE PTE LTD, with the registration number of SIN15219P.
This product contains Cobimetinib 20mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by F. Hoffmann-La Roche Ltd in SWITZERLAND, andDelpharm Milano S.r.l. (Primary & Secondary Packager) in ITALY.
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
Cobimetinib is an orally active, potent and highly selective small molecule inhibiting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), and central components of the RAS/RAF/MEK/ERK signal transduction pathway. It has been approved in Switzerland and the US, in combination with vemurafenib for the treatment of patients with unresectable or metastatic BRAF V600 mutation-positive melanoma.
Indication
For the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation. Cobimetinib is used in combination with vemurafenib, a BRAF inhibitor.
Mechanism of Action
MEK inhibitor Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Cobimetinib and vemurafenib target two different kinases in the RAS/RAF/MEK/ERK pathway.
Pharmacokinetics
- Absorption
- The bioavailability of cobimetinib is 46%, the AUC and Cmax is unaffected by food.
- Distribution
- 806L in cancer patients based on a population PK analysis.
- Metabolism
- Cobimetinib is mainly metabolized via CYP3A oxidation and UGT2B7 glucuronidation with no major metabolites formed.
- Elimination
Clearance
13.9L/h
Toxicity
The most common adverse effects (>20%) for cobimetinib are diarrhea, photosensitivity reactions, nausea, fever and vomiting.
Active Ingredient/Synonyms
Cobimetinib | Cobimetinib |
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.