Vemurafenib
Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Also known as: PLX-4032, RG 7204, Ro 51-85426, RO 5185426, zelboraf
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Vemurafenib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2011. Its mechanism of action is classified as Cytochrome P450 1A2 Inhibitors, P-Glycoprotein Inhibitors and Protein Kinase Inhibitors. DrugCentral lists 24 molecular targets, including RET, Map2k4 and TNK2. Recorded indications include Erdheim-Chester Disease and Malignant Melanoma with BRAF V600E Mutation.
- Approval status: onp (first approved 2011 by the FDA).
- Drug class: Kinase Inhibitor.
- Mechanism of action: Cytochrome P450 1A2 Inhibitors; P-Glycoprotein Inhibitors; Protein Kinase Inhibitors.
- Molecular targets: RET, Map2k4, TNK2 and BRAF (24 listed in DrugCentral).
- Indications: Erdheim-Chester Disease and Malignant Melanoma with BRAF V600E Mutation.
- ATC code: L01EC01 (B-Raf serine-threonine kinase (BRAF) inhibitors).
- Molecular formula: C23H18ClF2N3O3S; molecular weight 489.92 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (2)
- Erdheim-Chester Disease
- Malignant Melanoma with BRAF V600E Mutation
Contraindications (16)
- Acute nephropathy
- Bradycardia
- Breastfeeding (mother)
- Congenital long QT syndrome
- Decompensated chronic heart failure
- Hyperbilirubinemia
- Hypocalcemia
- Hypokalemia
- Hypomagnesemia
- Iritis
- Liver function tests abnormal
- Pregnancy, function
- Prolonged QT interval
- Retinal Blood Vessel Occlusions
- Torsades de pointes
- Uveitis
Mechanism & targets
| Mechanism of action (MoA) | Cytochrome P450 1A2 Inhibitors; P-Glycoprotein Inhibitors; Protein Kinase Inhibitors |
|---|---|
| Established pharmacologic class | Kinase Inhibitor |
Molecular targets (24)
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 2011-08-17 | FDA | — | HOFFMANN LA ROCHE | Yes |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
L01EC01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › B-Raf serine-threonine kinase (BRAF) inhibitors |
Pharmacogenomics
Drug-label and guideline annotations from PharmGKB and CPIC.
- EMA label: BRAF · Testing Required
- FDA label: BRAF · Testing Required
- FDA label: HRAS, KRAS, NRAS
- HCSC label: BRAF · Testing Required
- PMDA label: BRAF · Testing Required
Reported adverse-event signals
Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.
| MedDRA term | LLR |
|---|---|
| Disease progression | 948.6 |
| Photosensitivity reaction | 940.9 |
| Rash | 773.9 |
| Metastases to central nervous system | 572.3 |
| Sunburn | 528.9 |
| Skin toxicity | 518.9 |
| Keratoacanthoma | 462.6 |
| Hyperkeratosis | 441.6 |
| Squamous cell carcinoma | 387.7 |
| Rash maculo-papular | 357.4 |
| Skin papilloma | 353.3 |
| Death | 265.7 |
Chemical structure
Full physicochemical, ADMET and 3D-structure analysis of Vemurafenib is on its molecule page.
| Molecular formula | C23H18ClF2N3O3S |
|---|---|
| Molecular weight | 489.92 g/mol |
| CAS number | 918504-65-1 |
| InChIKey | GPXBXXGIAQBQNI-UHFFFAOYSA-N |
| PubChem CID | 42611257 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Vemurafenib used for?
DrugCentral lists the following indications for Vemurafenib: Erdheim-Chester Disease and Malignant Melanoma with BRAF V600E Mutation.
How does Vemurafenib work?
Vemurafenib is classified as Cytochrome P450 1A2 Inhibitors, P-Glycoprotein Inhibitors and Protein Kinase Inhibitors; its molecular targets in DrugCentral include RET, Map2k4, TNK2 and BRAF (inhibitor).
When was Vemurafenib first approved?
Vemurafenib was first approved by the FDA in 2011.
What drug class does Vemurafenib belong to?
Vemurafenib is in the Kinase Inhibitor class.
What is the chemical formula of Vemurafenib?
Vemurafenib has the molecular formula C23H18ClF2N3O3S and a molecular weight of 489.92 g/mol.
Browse: all drugs starting with V · drug guides by category · protein targets A–Z.
Sources
- DrugCentral drug card 4185 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL1229517 — compound record and bioactivity
- PubChem CID 42611257 — chemical identifiers
- DrugBank DB08881 — drug record
- FDA UNII 207SMY3FQT — substance identity
- DailyMed: FDA labels for Vemurafenib — current prescribing information (label search)
- UniProt P07949 (RET) — target protein
- UniProt Q07912 (TNK2) — target protein
- UniProt P15056 (BRAF) — target protein
- UniProt Q9NYL2 (ZAK) — target protein
- UniProt P04049 (RAF1) — target protein
- UniProt P00533 (EGFR) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
- PharmGKB / CPIC — pharmacogenomic label annotations
How this page is built: methodology · editorial policy & corrections.
For research and educational use only — not medical advice. This page is compiled automatically from public databases. It is not written or reviewed by a clinician. Do not start, stop or change any treatment based on it; consult a qualified healthcare professional. Spotted an error? See our corrections policy or email hello@molforge.ai.