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

A Study to Detect V-Raf Murine Sarcoma Viral Oncogene Homolog B1 (BRAF) V600 Mutation on Cell-Free Deoxyribonucleic Acid (cfDNA) From Plasma in Participants With Advanced Melanoma

Phase 2

Completed

Conditions: Metastatic Melanoma

Interventions: Drug: Cobimetinib
Drug: Vemurafenib

First Posted Date: 2016-05-11

Last Posted Date: 2019-08-28

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 40

Registration Number: NCT02768207

Locations: 🇧🇪
UZ Brussel, Brussel, Belgium
🇧🇪
UZ Antwerpen, Edegem, Belgium
🇧🇪
Jessa Zkh (Campus Virga Jesse), Hasselt, Belgium

and more 11 locations

XL888 + Vemurafenib + Cobimetinib for Unresectable BRAF Mutated Stage III/IV Melanoma

Phase 1

Active, not recruiting

Conditions: Melanoma
Skin Cancer

Interventions: Drug: XL888
Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2016-03-29

Last Posted Date: 2025-05-22

Lead Sponsor: H. Lee Moffitt Cancer Center and Research Institute

Target Recruit Count: 26

Registration Number: NCT02721459

Locations: 🇺🇸
H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, United States

TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer

Phase 2

Recruiting

Conditions: Lymphoma, Non-Hodgkin
Multiple Myeloma
Advanced Solid Tumors

Interventions: Drug: Sunitinib
Drug: Vemurafenib and Cobimetinib
Drug: Palbociclib
Drug: Nivolumab and Ipilimumab
Drug: Abemaciclib
Drug: Atezolizumab and PHESGO
Drug: Atezolizumab and Talazoparib
Drug: Futibatinib
Drug: Trastuzumab and Pertuzumab
Drug: Tucatinib plus Trastuzumab Subcutaneous (SC)
Drug: Talazoparib
Drug: Temsirolimus
Drug: Regorafenib
Drug: Olaparib
Drug: Pembrolizumab
Drug: Entrectinib
Drug: Larotrectinib

First Posted Date: 2016-02-26

Last Posted Date: 2025-05-06

Lead Sponsor: American Society of Clinical Oncology

Target Recruit Count: 4200

Registration Number: NCT02693535

Locations: 🇺🇸
University of Alabama at Birmingham Comprehensive Cancer Center, Birmingham, Alabama, United States
🇺🇸
Cancer Treatment Centers of America-Phoenix, Phoenix, Arizona, United States
🇺🇸
Sutter Auburn, Auburn, California, United States

and more 129 locations

Genomics-Based Target Therapy for Children With Relapsed or Refractory Malignancy

Phase 2

Conditions: Relapsed Pediatric Solid Tumor
Refractory Pediatric Solid Tumor
Relapsed Pediatric AML
Refractory Pediatric AML

Interventions: Procedure: CancerSCAN™
Drug: Ifosfamide
Drug: Carboplatin
Drug: Etoposide
Drug: Fludarabine
Drug: Cytarabine
Drug: Pazopanib
Drug: Sorafenib
Drug: Axitinib
Drug: Crizotinib
Drug: Dasatinib
Drug: Erlotinib
Drug: Everolimus
Drug: Imatinib
Drug: Ruxolitinib
Drug: Vandetanib
Drug: Vemurafenib
Drug: Trastuzumab

First Posted Date: 2015-12-23

Last Posted Date: 2020-03-19

Lead Sponsor: Samsung Medical Center

Target Recruit Count: 90

Registration Number: NCT02638428

Locations: 🇰🇷
Samsung Medical Center, Seoul, Korea, Republic of

A Study to Investigate the Effect of Itraconazole and Rifampin on Pharmacokinetics (PK) of Vemurafenib at Steady State

Phase 1

Completed

Conditions: Metastatic Melanoma, BRAF V600 Mutation Positive

Interventions: Drug: Itraconazole
Drug: Rifampin
Drug: Vemurafenib

First Posted Date: 2015-11-18

Last Posted Date: 2020-02-12

Lead Sponsor: Genentech, Inc.

Target Recruit Count: 32

Registration Number: NCT02608034

Locations: 🇮🇱
Hadassah Ein Karem Hospital; Oncology Dept, Jerusalem, Israel
🇰🇷
Samsung Medical Center; Gastroenterology, Seoul, Korea, Republic of
🇷🇺
FSBSI "N. N. Blokhin Russian Cancer Research Center", Moscow, Russian Federation

and more 8 locations

Clinical Trial to Evaluate the Efficacy of Vemurafenib in Combination With Cobimetinib (Continuous and Intermittent) in BRAFV600-mutation Positive Patients With Unresectable Locally Advanced or Metastatic Melanoma

Phase 2

Completed

Conditions: Melanoma

Interventions: Drug: vemurafenib and cobimetinib

First Posted Date: 2015-10-22

Last Posted Date: 2020-02-17

Lead Sponsor: Grupo Español Multidisciplinar de Melanoma

Target Recruit Count: 70

Registration Number: NCT02583516

Locations: 🇪🇸
Hospital Universitario 12 de Octubre, Madrid, Spain
🇪🇸
Hospital Universitario de Canarias, Tenerife, Spain
🇪🇸
Hospital Clínico Universitario de Salamanca, Salamanca, Spain

and more 15 locations

Enhancing Radioiodine Incorporation Into BRAF Mutant Thyroid Cancers With the Combination of Vemurafenib and KTN3379

Phase 1

Completed

Conditions: Thyroid Cancer

Interventions: Biological: KTN3379
Drug: vemurafenib

First Posted Date: 2015-05-28

Last Posted Date: 2017-09-05

Lead Sponsor: Celldex Therapeutics

Target Recruit Count: 7

Registration Number: NCT02456701

Locations: 🇺🇸
Memorial Sloan-Kettering Cancer Center, New York, New York, United States

Bioavailability Study of Vemurafenib in Participants With BRAF^V600 Mutation-Positive Malignancies

Phase 1

Completed

Conditions: Malignant Melanoma, Cancer

Interventions: Drug: Vemurafenib
Drug: 14C-Labeled Vemurafenib

First Posted Date: 2015-05-12

Last Posted Date: 2017-11-14

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 6

Registration Number: NCT02441465

Locations: 🇭🇺
Magyar Honvedseg Egeszsegugyi Kozpont, Budapest, Hungary

Trial of Vemurafenib and Cobimetinib in Patients With Advanced BRAFV600 Mutant Melanoma

Phase 3

Withdrawn

Conditions: Melanoma

Interventions: Drug: Cobimetinib
Drug: Vemurafenib

First Posted Date: 2015-04-28

Last Posted Date: 2016-11-15

Lead Sponsor: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins

Registration Number: NCT02427893

Locations: 🇺🇸
The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland, United States

Vemurafenib Plus Cobimetinib in Metastatic Melanoma

Phase 2

Terminated

Conditions: Metastatic Melanoma

Interventions: Drug: Vemurafenib plus cobimetinib
Device: Positron Emission Tomography
Procedure: Tissue sampling
Procedure: Blood sampling

First Posted Date: 2015-04-13

Last Posted Date: 2022-11-30

Lead Sponsor: Netherlands Working Group on Immunotherapy of Oncology

Target Recruit Count: 78

Registration Number: NCT02414750

Locations: 🇳🇱
University Medical Center St Radboud, Nijmegen, Netherlands
🇳🇱
The Netherlands Cancer Institute, Amsterdam, Netherlands
🇳🇱
VU medical center, Amsterdam, Netherlands

and more 7 locations

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