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

The Effects of Vemurafenib + Cobimetinib on Immunity in Patients With Melanoma

Phase 2

Terminated

Conditions: Melanoma

Interventions: Drug: Vemurafenib
Drug: Cobimetinib

First Posted Date: 2013-03-18

Last Posted Date: 2019-02-26

Lead Sponsor: Georgetown University

Target Recruit Count: 5

Registration Number: NCT01813214

Locations: 🇺🇸
Georgetown Lombardi Comprehsnive Cancer Center, Washington, District of Columbia, United States
🇺🇸
University of Virginia Health System, Charlottesville, Virginia, United States
🇺🇸
Massachusetts General Hospital, Boston, Massachusetts, United States

and more 1 locations

Vemurafenib, Cetuximab, and Irinotecan Hydrochloride in Treating Patients With Solid Tumors That Are Metastatic or That Cannot Be Removed by Surgery

Phase 1

Active, not recruiting

Conditions: Unresectable Solid Neoplasm
Metastatic Malignant Solid Neoplasm
Stage IV Colorectal Cancer AJCC v7
Stage IVA Colorectal Cancer AJCC v7
BRAF NP_004324.2:p.V600X
Stage IVB Colorectal Cancer AJCC v7
KRAS wt Allele

Interventions: Biological: Cetuximab
Drug: Irinotecan Hydrochloride
Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Vemurafenib

First Posted Date: 2013-02-08

Last Posted Date: 2025-03-30

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 33

Registration Number: NCT01787500

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States

Phase 2 Study of Neoadjuvant Vemurafenib in Melanoma Patients With Untreated Brain Metastases

Phase 2

Completed

Conditions: Melanoma

Interventions: Drug: Vemurafenib

First Posted Date: 2013-01-31

Last Posted Date: 2017-03-10

Lead Sponsor: Yale University

Target Recruit Count: 2

Registration Number: NCT01781026

Locations: 🇺🇸
Smilow Cancer Hospital at Yale New Haven, New Haven, Connecticut, United States

A Study of The Impact of Severe Hepatic Impairment on the Pharmacokinetics and Safety of Vemurafenib in BRAF V600 Mutation-Positive Cancer Participants

Phase 1

Completed

Conditions: Neoplasms

Interventions: Drug: Vemurafenib

First Posted Date: 2013-01-14

Last Posted Date: 2018-02-13

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 8

Registration Number: NCT01767623

Locations: 🇺🇸
California Cancer Associates for Research & Excellence, Inc., Encinitas, California, United States
🇬🇧
Velindre Cancer Centre, Cardiff, United Kingdom
🇦🇺
Peninsula and South Eastern Haematology and Oncology Grou, Frankston, Victoria, Australia

and more 5 locations

A Pharmacokinetics Study to Investigate the Effect of Vemurafenib on Digoxin in Patients With BRAFV600 Mutation-Positive Metastatic Melanoma

Phase 1

Completed

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: Digoxin
Drug: Vemurafenib

First Posted Date: 2013-01-10

Last Posted Date: 2015-09-23

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 29

Registration Number: NCT01765569

A Pharmacokinetics (PK) Study to Investigate the Effect of Rifampin on PK of Vemurafenib (Zelboraf)

Phase 1

Completed

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: Rifampin
Drug: Vemurafenib

First Posted Date: 2013-01-10

Last Posted Date: 2016-12-15

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 27

Registration Number: NCT01765543

A Pharmacokinetics Study to Investigate the Effect of Ketoconazole on Vemurafenib in Patients With BRAFV600 Mutation-Positive Metastatic Melanoma

Phase 1

Withdrawn

Conditions: Malignant Melanoma, Neoplasms

Interventions: Drug: ketoconazole
Drug: vemurafenib

First Posted Date: 2013-01-10

Last Posted Date: 2016-11-02

Lead Sponsor: Hoffmann-La Roche

Registration Number: NCT01765556

Combined BRAF-Targeted Therapy & Immunotherapy for Melanoma

Phase 2

Terminated

Conditions: Melanoma

Interventions: Drug: Aldesleukin
Drug: Vemurafenib

First Posted Date: 2012-12-21

Last Posted Date: 2017-04-12

Lead Sponsor: Massachusetts General Hospital

Target Recruit Count: 6

Registration Number: NCT01754376

Locations: 🇺🇸
Massachusetts General Hospital, Boston, Massachusetts, United States
🇺🇸
Beth Israel Deaconess Medical Center, Boston, Massachusetts, United States

Vemurafenib in Children With Recurrent/Refractory BRAF Gene V600E (BRAFV600E)-Mutant Gliomas

Early Phase 1

Active, not recruiting

Conditions: Pediatric Recurrent/Refractory BRAFV600E-mutant Gliomas

Interventions: Drug: Vemurafenib

First Posted Date: 2012-12-12

Last Posted Date: 2025-01-23

Lead Sponsor: University of California, San Francisco

Target Recruit Count: 40

Registration Number: NCT01748149

Locations: 🇺🇸
Children's Hospital Los Angeles, Los Angeles, California, United States
🇺🇸
Mattel Children's Hospital UCLA, Los Angeles, California, United States
🇺🇸
Dana-Farber Cancer Institute, Boston, Massachusetts, United States

and more 18 locations

An Extension (Rollover) Study of Vemurafenib in Participants With BRAF V600 Mutation-Positive Malignancies Previously Enrolled in an Antecedent Vemurafenib Protocol

Phase 4

Completed

Conditions: Neoplasms

Interventions: Drug: Vemurafenib

First Posted Date: 2012-12-03

Last Posted Date: 2021-01-07

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 215

Registration Number: NCT01739764

Locations: 🇺🇸
Siouxland Regional Cancer Center d/b/a June E. Nylen Cancer Center, Sioux City, Iowa, United States
🇺🇸
Evelyn H. Lauder Center, New York, New York, United States
🇺🇸
University of Pennsylvania Health System, Philadelphia, Pennsylvania, United States

and more 80 locations

Drug Development Updates

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