Drugs /

vemurafenib

Back to Drugs List
Associated Genetic Biomarkers
Associated Diseases

Overview

Generic Name(s):
vemurafenib
Trade Name(s):
Zelboraf
NCI Definition [1]:
An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers.

Biomarker-Directed Therapies

Clinical Trials

View Clinical Trials for vemurafenib

Vemurafenib has been investigated in 34 clinical trials, of which 27 are open and 7 are closed. Of the trials investigating vemurafenib, 1 is early phase 1 (1 open), 6 are phase 1 (4 open), 3 are phase 1/phase 2 (3 open), and 24 are phase 2 (19 open).

BRAF Codon 600 Missense, BRAF V600E, and BRAF V600K are the most frequent biomarker inclusion criteria for vemurafenib clinical trials.

Melanoma, malignant solid tumor, and multiple myeloma are the most common diseases being investigated in vemurafenib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Vemurafenib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Vemurafenib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating vemurafenib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
plx-4032, vemurafenib (substance), vemurafenib, braf(v600e) kinase inhibitor ro5185426, braf(v600e) kinase inhibitor ro5185426, braf (v600e) kinase inhibitor ro5185426, plx4032, 1-propanesulfonamide, n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3-yl)carbonyl)-2,4-difluorophenyl)-, vemurafenib, ro5185426, plx 4032, rg7204, r05185426, Zelboraf, vemurafenib (product), rg 7204, ro 5185426
Drug Categories [2]:
BRAF inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
ARAF, BRAF, RAF1
NCIT ID [1]:
C64768
SNOMED ID [1]:
R-FB9DD

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.