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

BRAF Inhibitor, Vemurafenib, in Patients With Relapsed or Refractory Hairy Cell Leukemia

Phase 2

Completed

Conditions: Hairy Cell Leukemia

Interventions: Drug: Vemurafenib

First Posted Date: 2012-10-22

Last Posted Date: 2024-08-20

Lead Sponsor: Memorial Sloan Kettering Cancer Center

Target Recruit Count: 36

Registration Number: NCT01711632

Locations: 🇺🇸
Scripps Clinic, La Jolla, California, United States
🇺🇸
Northwestern University, Evanston, Illinois, United States
🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States

and more 2 locations

Vemurafenib Neoadjuvant Trial in Locally Advanced Thyroid Cancer

Phase 2

Active, not recruiting

Conditions: Thyroid Cancer

Interventions: Drug: Vemurafenib (All Groups)
Drug: Vemurafenib (Post Surgery) - Group A + C
Other: Post Surgery - Group B

First Posted Date: 2012-10-18

Last Posted Date: 2025-05-11

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 24

Registration Number: NCT01709292

Locations: 🇺🇸
University of Texas MD Anderson Cancer Center, Houston, Texas, United States

A Study Comparing Vemurafenib Versus Vemurafenib Plus Cobimetinib in Participants With Metastatic Melanoma

Phase 3

Completed

Conditions: Malignant Melanoma

Interventions: Drug: Placebo
Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2012-09-21

Last Posted Date: 2022-05-02

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 495

Registration Number: NCT01689519

Locations: 🇧🇪
UZ Antwerpen, Edegem, Belgium
🇬🇧
Velindre Cancer Centre, Cardiff, United Kingdom
🇦🇺
Lismore Base Hospital; Cancer Care & Haematology Unit, Lismore, New South Wales, Australia

and more 153 locations

HD IL-2 + Vemurafenib in Patients With BRAF Mutation Positive Metastatic Melanoma

Phase 4

Terminated

Conditions: Metastatic Melanoma

Interventions: Drug: vemurafenib + HD IL-2

First Posted Date: 2012-09-11

Last Posted Date: 2021-02-01

Lead Sponsor: Clinigen, Inc.

Target Recruit Count: 53

Registration Number: NCT01683188

Locations: 🇺🇸
Emory University School of Medicine, Atlanta, Georgia, United States
🇺🇸
Luther General Cancer Care Institute, Park Ridge, Illinois, United States
🇺🇸
UPMC Cancer Centers, Pittsburgh, Pennsylvania, United States

and more 18 locations

A Phase I/Ib Trial for the Evaluation of SAR260301 in Monotherapy or in Combination With Vemurafenib in Patients With Various Advanced Cancer

Phase 1

Completed

Conditions: Neoplasm Malignant

Interventions: Drug: SAR260301
Drug: Vemurafenib

First Posted Date: 2012-08-28

Last Posted Date: 2015-04-10

Lead Sponsor: Sanofi

Target Recruit Count: 75

Registration Number: NCT01673737

Locations: 🇺🇸
Investigational Site Number 840001, Boston, Massachusetts, United States
🇺🇸
Investigational Site Number 840002, Houston, Texas, United States
🇺🇸
Investigational Site Number 840101, Boston, Massachusetts, United States

and more 1 locations

A Study of Vemurafenib Adjuvant Therapy in Participants With Surgically Resected Cutaneous BRAF-Mutant Melanoma

Phase 3

Completed

Conditions: Melanoma

Interventions: Drug: Vemurafenib
Drug: Placebo

First Posted Date: 2012-08-17

Last Posted Date: 2019-07-23

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 498

Registration Number: NCT01667419

Locations: 🇷🇺
Krasnodar City Oncology Center, Krasnodar, Russian Federation
🇷🇸
Military Medical Academy, Belgrade, Serbia
🇿🇦
Mary Potter Oncology Centre, Groenkloof, South Africa

and more 203 locations

Vemurafenib With Lymphodepletion Plus Adoptive Cell Transfer & High Dose IL-2 Metastatic Melanoma

Phase 2

Active, not recruiting

Conditions: Metastatic Melanoma

Interventions: Drug: High Dose Interleukin-2 (IL-2)
Procedure: ACT with TIL Infusion
Drug: Vemurafenib
Drug: Lymphodepletion

First Posted Date: 2012-08-07

Last Posted Date: 2025-05-22

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

Target Recruit Count: 17

Registration Number: NCT01659151

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

Study of XL888 With Vemurafenib for Patients With Unresectable BRAF Mutated Stage III/IV Melanoma

Phase 1

Completed

Conditions: Melanoma

Interventions: Drug: XL888
Drug: Vemurafenib

First Posted Date: 2012-08-06

Last Posted Date: 2023-01-19

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

Target Recruit Count: 21

Registration Number: NCT01657591

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

A Phase 1b Study of Atezolizumab in Combination With Vemurafenib or Vemurafenib Plus Cobimetinib in Participants With BRAFV600-Mutation Positive Metastatic Melanoma

Phase 1

Completed

Conditions: Malignant Melanoma

Interventions: Drug: Atezolizumab
Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2012-08-03

Last Posted Date: 2020-07-21

Lead Sponsor: Genentech, Inc.

Target Recruit Count: 67

Registration Number: NCT01656642

Locations: 🇺🇸
MD Anderson Cancer Center, Houston, Texas, United States
🇺🇸
UCLA, Los Angeles, California, United States
🇺🇸
The Angeles Clinic and Research Institute - W LA Office, Los Angeles, California, United States

and more 5 locations

A Phase I/II Trial of Vemurafenib and Metformin to Melanoma Patients

Phase 1

Recruiting

Conditions: Melanoma

Interventions: Drug: Vemurafenib
Drug: Metformin

First Posted Date: 2012-07-12

Last Posted Date: 2021-10-29

Lead Sponsor: University of Louisville

Target Recruit Count: 55

Registration Number: NCT01638676

Locations: 🇺🇸
James Graham Brown Cancer Center-University of Louisville, Louisville, Kentucky, United States

Drug Development Updates

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