vemurafenib (zelboraf) Report issue

Small molecule Orphan Drug FDA Approved FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem

Active Ingredient History

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  • Now
Vemurafenib (trade name Zelboraf) is a low molecular weight, orally available kinase inhibitor. It inhibits of some mutated forms of BRAF serinethreonine kinase, including BRAF V600E and is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5 and FGR at similar concentrations. Vemurafenib is not recommended for use in patients with wild-type BRAF melanoma. Zelboraf does not cure melanoma, but stops it's progression. Some 26% of patients in clinical trials developed a non melanoma form of skin cancer called cutaneous squamous cell carcinoma, which can usually be removed via relatively simple surgery. Other side effects include joint pain, rash, hair loss, fatigue, nausea, and skin sensitivity to sunlight. Patients taking Zelboraf must avoid sun exposure. It's not yet clear how long Zelboraf can increase melanoma survival.   NCATS

Chemistry

  • SMILES: CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(Cl)C=C4)=C(F)C=C1
  • InChIKey: GPXBXXGIAQBQNI-UHFFFAOYSA-N
  • Mol. Mass: 489.922
  • ALogP: 5.54
  • ChEMBL Molecule:
    vemurafenib  
More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

Australia

$23.9744

United States

$34.1213 - $45.2117
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

1-propanesulfonamide, n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3- yl)carbonyl)-2,4-difluorophenyl)- | braf(v600e) kinase inhibitor ro5185426 | n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3-yl)carbonyl)-2,4- difluorophenyl)propane-1-sulfonamide | plx4032 | plx 4032 | plx-4032 | r05185426 | rg7204 | rg 7204 | rg-7204 | ro5185426 | ro 5185426 | ro 51-85426 | ro-5185426 | vemurafenib | vermurafenib | zelboraf

Organizations (114)

Research & Development (114)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (57)

Approved Indications (2)


 

Carcinoma, Non-Small-Cell Lung

Melanoma

Experimental Indications - Clinical Trial Phases 1-4 (57)


 

Anemia (Phase 1)

Biliary Tract Neoplasms (Phase 2)

Brain Neoplasms (Phase 2)

Breast Neoplasms (Phase 2)

Carcinoma, Non-Small-Cell Lung (Phase 2/Phase 3)

Colorectal Neoplasms (Phase 3)

Craniopharyngioma (Phase 2)

Ependymoma (Phase 2)

Erdheim-Chester Disease (Phase 2/Phase 3)

Gastrointestinal Neoplasms (Phase 2)

Glioma (Phase 2/Phase 3)

Hepatoblastoma (Phase 2)

Histiocytosis (Phase 2)

Histiocytosis, Langerhans-Cell (Phase 2)

Hodgkin Disease (Phase 1)

Laryngeal Neoplasms (Phase 2/Phase 3)

Leukemia (Phase 2)

Leukemia, Hairy Cell (Phase 2)

Leukemia, Lymphocytic, Chronic, B-Cell (Phase 1)

Leukemia, Myelogenous, Chronic, BCR-ABL Positive (Phase 1)

Leukemia, Myeloid, Acute (Phase 2)

Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative (Phase 1)

Leukemia, Myeloid, Chronic-Phase (Phase 1)

Leukemia, Myelomonocytic, Chronic (Phase 1)

Lymphoma (Phase 1/Phase 2)

Lymphoma, Non-Hodgkin (Phase 2)

Lymphoma, Primary Cutaneous Anaplastic Large Cell (Phase 1)

Melanoma ()

Multiple Myeloma (Phase 2/Phase 3)

Mutation (Phase 2)

Myelodysplastic Syndromes (Phase 1)

Myeloproliferative Disorders (Phase 1)

Neoplasm Metastasis (Phase 2)

Neoplasms ()

Neoplasms, Germ Cell and Embryonal (Phase 2)

Neuroblastoma (Phase 2)

Neuroectodermal Tumors, Primitive, Peripheral (Phase 2)

Osteosarcoma (Phase 2)

Ovarian Neoplasms (Phase 2/Phase 3)

Pancreatic Neoplasms (Phase 2)

Precursor B-Cell Lymphoblastic Leukemia-Lymphoma (Phase 1)

Primary Myelofibrosis (Phase 1)

Prostatic Neoplasms (Phase 2)

Prostatic Neoplasms, Castration-Resistant (Phase 1)

Proto-Oncogene Proteins B-raf (Phase 1)

ras Proteins (Phase 1)

Rhabdoid Tumor (Phase 2)

Rhabdomyosarcoma (Phase 2)

Sarcoma (Phase 2)

Sarcoma, Clear Cell (Phase 2)

Sarcoma, Ewing (Phase 2)

Skin Neoplasms (Phase 1)

Thyroid Cancer, Papillary (Phase 2/Phase 3)

Thyroid Carcinoma, Anaplastic (Phase 2/Phase 3)

Thyroid Neoplasms (Phase 2)

Urinary Bladder Neoplasms (Phase 2)

Wilms Tumor (Phase 2)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 144
  • # of Trial Organizations: 114

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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