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Vemurafenib

Generic Name
Vemurafenib
Brand Names
Zelboraf
Drug Type
Small Molecule
Chemical Formula
C23H18ClF2N3O3S
CAS Number
918504-65-1
Unique Ingredient Identifier
207SMY3FQT

Overview

Vemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E. It exerts its function by binding to the ATP-binding domain of the mutant BRAF. Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program.

Background

Vemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E. It exerts its function by binding to the ATP-binding domain of the mutant BRAF. Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program.

Indication

Vemurafenib is approved since 2011 for the treatment of metastatic melanoma with a mutation on BRAF in the valine located in the exon 15 at codon 600, this mutation is denominated as V600E. The V600E mutation, a substitution of glutamic acid for valine, accounts for 54% of the cases of cutaneous melanoma. Vemurafenib approval was extended in 2017, for its use as a treatment of adult patients with Erdheim-Chester Disease whose cancer cells present BRAF V600 mutation. Erdheim-Chester disease is an extremely rare histiocyte cell disorder that affects large bones, large vessels, central nervous system, as well as, skin and lungs. It is reported an association of Erdheim-Chester disease and V600E mutation.

Associated Conditions

  • Metastatic Melanoma
  • Refractory Lung Non-Small Cell Carcinoma
  • Unresectable Melanoma
  • Refractory Erdheim-Chester disease

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2024/11/18
Phase 2
Not yet recruiting
Peking University Shenzhen Hospital
2024/08/20
Phase 2
Recruiting
2024/06/04
Phase 2
Recruiting
City of Hope Medical Center
2023/03/14
Phase 2
Recruiting
2023/02/10
Phase 2
Recruiting
2022/09/02
N/A
Recruiting
2022/03/02
Phase 2
Recruiting
2022/03/02
N/A
Completed
2022/02/14
Early Phase 1
Withdrawn
2022/02/10
Phase 2
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Genentech, Inc.
50242-090
ORAL
240 mg in 1 1
11/27/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
2/17/2012

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
Zelboraf Tablet 240mg
SIN14308P
TABLET, FILM COATED
240mg
2/4/2013

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Vemurafenib film-coated tablets
国药准字HJ20170124
化学药品
片剂
1/17/2022

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
ZELBORAF vemurafenib 240 mg film coated tablet blister pack
183674
Medicine
A
5/10/2012
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