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

Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial)

Phase 2

Active, not recruiting

Conditions: Advanced Malignant Solid Neoplasm
Juvenile Xanthogranuloma
Langerhans Cell Histiocytosis
Malignant Glioma
Recurrent Childhood Rhabdomyosarcoma
Recurrent Ewing Sarcoma
Recurrent Osteosarcoma
Recurrent Primary Central Nervous System Neoplasm
Refractory Hepatoblastoma
Refractory Medulloblastoma

Interventions: Procedure: Biopsy Procedure
Procedure: Biospecimen Collection
Other: Laboratory Biomarker Analysis
Procedure: Bone Marrow Aspiration and Biopsy
Procedure: Mutation Carrier Screening
Procedure: Bone Scan
Drug: Larotrectinib Sulfate
Procedure: Computed Tomography
Drug: Olaparib
Drug: Palbociclib
Drug: Tazemetostat
Drug: Samotolisib
Drug: Selumetinib Sulfate
Drug: Ensartinib
Drug: Vemurafenib
Drug: Ulixertinib
Drug: Tipifarnib
Drug: Erdafitinib
Procedure: Magnetic Resonance Imaging
Other: Pharmacological Study
Drug: Selpercatinib
Procedure: Radionuclide Imaging
Procedure: Positron Emission Tomography
Procedure: X-Ray Imaging

First Posted Date: 2017-05-16

Last Posted Date: 2025-05-13

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 1376

Registration Number: NCT03155620

Locations: 🇺🇸
Children's Hospital of Alabama, Birmingham, Alabama, United States
🇺🇸
Providence Alaska Medical Center, Anchorage, Alaska, United States
🇺🇸
Banner Children's at Desert, Mesa, Arizona, United States

and more 169 locations

A Study of Adult Participants With BRAF V600 Mutation-Positive Advanced Melanoma Treated With Cobimetinib (Cotellic®) During the French Early Access Program (Temporary Authorization for Use [TAU])

Completed

Conditions: Melanoma

Interventions: Drug: Cobimetinib
Drug: Vemurafenib

First Posted Date: 2017-05-04

Last Posted Date: 2019-01-22

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 200

Registration Number: NCT03139513

Locations: 🇫🇷
CH Metropole de Savoie, CHAMBERY Cedex, France
🇫🇷
Hopital Louis Pasteur; Sce Dermatologie, Colmar, France
🇫🇷
Hopital Cochin; Dermatologie, Paris, France

and more 30 locations

LY3022855 With BRAF/MEK Inhibition in Patients With Melanoma

Phase 1

Completed

Conditions: Melanoma

Interventions: Drug: LY3022855
Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2017-04-05

Last Posted Date: 2024-07-17

Lead Sponsor: Dana-Farber Cancer Institute

Target Recruit Count: 5

Registration Number: NCT03101254

Locations: 🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States

PROCLAIM-CX-072: A Trial to Find Safe and Active Doses of an Investigational Drug CX-072 for Patients With Solid Tumors or Lymphomas

Phase 1

Completed

Conditions: Solid Tumor
Lymphoma

Interventions: Drug: CX-072
Drug: ipilimumab
Drug: vemurafenib

First Posted Date: 2017-01-06

Last Posted Date: 2022-02-09

Lead Sponsor: CytomX Therapeutics

Target Recruit Count: 300

Registration Number: NCT03013491

Locations: 🇬🇧
PROCLAIM Invetigative Site, Glasgow, United Kingdom
🇬🇧
PROCLAIM Investigative Site, Newcastle upon Tyne, United Kingdom
🇪🇸
PROCLAIM Investigative Ssite, Valencia, Spain

ML29255 Neoadjuvant Vemurafenib and Cobimetinib Melanoma

Phase 2

Withdrawn

Conditions: Stage IIIB-C Melanoma

Interventions: Drug: Vemurafenib and Cobimetinib

First Posted Date: 2016-12-29

Last Posted Date: 2018-05-09

Lead Sponsor: Inova Health Care Services

Registration Number: NCT03005639

Locations: 🇺🇸
Inova Schar Cancer Institute, Fairfax, Virginia, United States

Induction Therapy With Vemurafenib and Cobimetinib to Optimize Nivolumab and Ipilimumab Therapy

Phase 2

Conditions: Melanoma, Malignant, of Soft Parts

Interventions: Drug: Vemurafenib and Cobimetinib

First Posted Date: 2016-11-18

Last Posted Date: 2020-06-05

Lead Sponsor: Radboud University Medical Center

Target Recruit Count: 200

Registration Number: NCT02968303

Locations: 🇳🇱
UMC Utrecht, Utrecht, Netherlands
🇳🇱
The Netherlands Cancer Institute, Amsterdam, Netherlands
🇳🇱
Radboudumc, Nijmegen, Netherlands

and more 10 locations

The Drug Rediscovery Protocol (DRUP Trial)

First Posted Date: 2016-10-05

Last Posted Date: 2024-01-24

Lead Sponsor: The Netherlands Cancer Institute

Target Recruit Count: 1550

Registration Number: NCT02925234

Locations: 🇳🇱
Meander medisch centrum, Amersfoort, Netherlands
🇳🇱
Netherlands Cancer Institute, Amsterdam, Netherlands
🇳🇱
Amsterdam UMC, locatie AMC, Amsterdam, Netherlands

and more 33 locations

A Study of Atezolizumab Plus Cobimetinib and Vemurafenib Versus Placebo Plus Cobimetinib and Vemurafenib in Previously Untreated BRAFv600 Mutation-Positive Patients With Metastatic or Unresectable Locally Advanced Melanoma

Phase 3

Completed

Conditions: Melanoma

Interventions: Drug: Atezolizumab Placebo
Drug: Atezolizumab
Drug: Cobimetinib
Drug: Vemurafenib
Drug: Vemurafenib Placebo

First Posted Date: 2016-09-21

Last Posted Date: 2024-09-30

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 514

Registration Number: NCT02908672

Locations: 🇺🇸
St. Luke's University Health network, Bethlehem, Pennsylvania, United States
🇫🇷
Institut Gustave Roussy; Dermatologie, Villejuif, France
🇩🇪
Universitätsklinikum Regensburg; Klinik und Poliklinik für Dermatologie, Regensburg, Germany

and more 113 locations

Evaluating the Efficacy and Safety of a Sequencing Schedule of Cobimetinib Plus Vemurafenib Followed by Immunotherapy With an Anti- PD-L1 Antibody in Patients With Unresectable or Metastatic BRAF V600 Mutant Melanoma

Phase 2

Completed

Conditions: Malignant Melanoma

Interventions: Drug: Vemurafenib
Drug: Cobimetinib
Drug: Atezolizumab

First Posted Date: 2016-09-15

Last Posted Date: 2025-04-09

Lead Sponsor: University Hospital, Essen

Target Recruit Count: 186

Registration Number: NCT02902029

Locations: 🇩🇪
HELIOS Klinikum Erfurt, Erfurt, Thuringia, Germany
🇩🇪
Charité-Universitätsmedizin Berlin, Berlin, Germany
🇩🇪
Elbe Kliniken Stade - Buxtehude, Buxtehude, Germany

and more 24 locations

Dose-seeking Study of Pembrolizumab Plus Vemurafenib and Cobimetinib Advanced Melanoma

Phase 1

Terminated

Conditions: Melanoma

Interventions: Drug: Pembrolizumab
Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2016-06-29

Last Posted Date: 2022-01-03

Lead Sponsor: Yana Najjar

Target Recruit Count: 9

Registration Number: NCT02818023

Locations: 🇺🇸
UPMC Cancer Center Hillman Cancer Center, Pittsburgh, Pennsylvania, United States

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