Vemurafenib

Generic Name: Vemurafenib

Brand Names: Zelboraf

Drug Type: Small Molecule

Chemical Formula: C_₂₃H_₁₈ClF_₂N_₃O_₃S

CAS Number: 918504-65-1

Unique Ingredient Identifier: 207SMY3FQT

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

An Open-Label Study of Zelboraf (Vemurafenib) in Patients With Braf V600 Mutation Positive Metastatic Melanoma

Phase 4

Completed

Conditions: Malignant Melanoma

Interventions: Drug: Zelboraf

First Posted Date: 2013-07-12

Last Posted Date: 2020-01-07

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 60

Registration Number: NCT01898585

Locations: 🇿🇦
Groote Schuur Hospital ( Uni of Capetown ); Oncology Dept, Cape Town, South Africa
🇿🇦
Medical Oncology Centre of Rosebank; Oncology, Johannesburg, South Africa
🇿🇦
Mary Potter Oncology Centre, Groenkloof, South Africa

and more 5 locations

A Phase I Trial of Vemurafenib and Hydroxychloroquine in Patients With Advanced BRAF Mutant Melanoma

Phase 1

Completed

Conditions: Melanoma

First Posted Date: 2013-07-11

Last Posted Date: 2020-05-29

Lead Sponsor: Abramson Cancer Center at Penn Medicine

Target Recruit Count: 8

Registration Number: NCT01897116

Locations: 🇺🇸
Abramson Cancer Center of the University of Pennsylvania, Philadelphia, Pennsylvania, United States

Treatment of a Resistant Disease Using Decitabine Combined With Vemurafenib Plus Cobimetinib

Phase 1

Terminated

Conditions: Melanoma
BRAF-mutated Metastatic Melanoma
Metastatic Melanoma
V600EBRAF-mutated Metastatic Melanoma

Interventions: Drug: Vemurafenib + Cobimetinib, Decitabine

First Posted Date: 2013-06-12

Last Posted Date: 2018-09-19

Lead Sponsor: Mohammed M Milhem

Target Recruit Count: 18

Registration Number: NCT01876641

Locations: 🇺🇸
University of Iowa Hospitals & Clinics, Iowa City, Iowa, United States

A Study of the Effect of Vemurafenib on the Pharmacokinetics of Acenocoumarol in Patients With BRAFV600 Mutation-Positive Metastatic Malignancy

Phase 1

Completed

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: acenocoumarol
Drug: vemurafenib

First Posted Date: 2013-05-13

Last Posted Date: 2016-11-02

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 9

Registration Number: NCT01851824

A Study of the Effect of Vemurafenib on the Pharmacokinetics of Phenprocoumon in Patients With BRAFV600 Mutation-Positive Metastatic Malignancy

Phase 1

Completed

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: phenprocoumon
Drug: vemurafenib

First Posted Date: 2013-05-08

Last Posted Date: 2016-11-02

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 2

Registration Number: NCT01849666

Radiation Use During Vemurafenib Treatment

Phase 1

Withdrawn

Conditions: BRAFV600 Mutation
Stage IV Melanoma

Interventions: Radiation: Radiation therapy
Drug: Vemurafenib

First Posted Date: 2013-05-01

Last Posted Date: 2017-05-24

Lead Sponsor: University of Utah

Registration Number: NCT01843738

Locations: 🇺🇸
Huntsman Cancer Institute, Salt Lake City, Utah, United States

A Study on the Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine in Patients With BRAFV600 Mutation-Positive Metastatic Malignancies

Phase 1

Completed

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: Tizanidine
Drug: Vemurafenib

First Posted Date: 2013-05-01

Last Posted Date: 2017-03-20

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 18

Registration Number: NCT01844674

Locations: 🇨🇾
Bank of Cyprus Oncology Center, Nicosia, Cyprus
🇨🇦
CSSS champlain - Charles-Le Moyne, Greenfield Park, Quebec, Canada
🇺🇸
Karmanos Cancer Center, Detroit, Michigan, United States

and more 9 locations

Study of an Oral Cdk Inhibitor Administered With an Oral BRAF Inhibitor in Patients With Advanced or Inoperable Malignant Melanoma With BRAF Mutation

Phase 1

Suspended

Conditions: Advanced or Inoperable Malignant Melanoma With BRAF Mutation

Interventions: Drug: P1446A-05
Drug: Vemurafenib (Zelboraf®)

First Posted Date: 2013-04-26

Last Posted Date: 2014-09-04

Lead Sponsor: Piramal Enterprises Limited

Target Recruit Count: 100

Registration Number: NCT01841463

Locations: 🇺🇸
The University of Texas, MD Anderson Cancer Center, Houston, Texas, United States
🇺🇸
University of Colorado Anschutz Medical Campus, Aurora, Colorado, United States
🇺🇸
UCSF Medical Center at Mount Zion, South San Francisco, California, United States

and more 1 locations

Cabozantinib-S-Malate and Vemurafenib in Treating Patients With Solid Tumors or Melanoma That is Metastatic or That Cannot Be Removed By Surgery

Phase 1

Terminated

Conditions: Stage IIIA Melanoma
Stage IIIC Melanoma
Recurrent Melanoma
Stage IIIB Melanoma
Stage IV Melanoma
Unspecified Adult Solid Tumor, Protocol Specific

Interventions: Drug: cabozantinib-s-malate
Drug: vemurafenib
Other: laboratory biomarker analysis
Other: pharmacological study

First Posted Date: 2013-04-18

Last Posted Date: 2014-09-25

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 5

Registration Number: NCT01835184

Locations: 🇺🇸
Dana-Farber Cancer Institute, Boston, Massachusetts, United States
🇺🇸
Emory University/Winship Cancer Institute, Atlanta, Georgia, United States
🇺🇸
Virginia Commonwealth University, Richmond, Virginia, United States

A Phase 1b Open Label, Dose Escalation Study of PLX3397 in Combination With Vemurafenib in V600-mutated BRAF Melanoma

Phase 1

Terminated

Conditions: V600-mutated BRAF Unresectable Melanoma
V600-mutated BRAF Metastatic Melanoma
Stage III or Stage IV Metastatic Melanoma That Has Not Been Previously Treated With a Selective BRAF Inhibitor

Interventions: Drug: PLX3397
Drug: vemurafenib

First Posted Date: 2013-04-08

Last Posted Date: 2020-05-28

Lead Sponsor: Daiichi Sankyo

Target Recruit Count: 13

Registration Number: NCT01826448

Locations: 🇺🇸
University of Colorado, Denver, Aurora, Colorado, United States
🇺🇸
Vanderbilt University, Nashville, Tennessee, United States
🇺🇸
Seattle Cancer Care Alliance, Seattle, Washington, United States

and more 3 locations

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