Zelboraf(vemurafenib)
Zelboraf (vemurafenib) is a small molecule pharmaceutical. Vemurafenib was first approved as Zelboraf on 2011-08-17. It is used to treat melanoma in the USA. It has been approved in Europe to treat melanoma. The pharmaceutical is active against serine/threonine-protein kinase B-raf. In addition, it is known to target RAF proto-oncogene serine/threonine-protein kinase.
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Commercial
Trade Name
FDA
EMA
Zelboraf
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| zelboraf | New Drug Application | 2024-11-08 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
VEMURAFENIB, ZELBORAF, HOFFMANN LA ROCHE | |||
| 2024-11-06 | ODE-158 | ||
HCPCS
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Clinical
Clinical Trials
171 clinical trials
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Colorectal neoplasms | D015179 | — | — | 1 | 3 | 1 | — | — | 4 |
| Multiple myeloma | D009101 | — | C90.0 | — | 3 | 1 | — | — | 3 |
| Non-small-cell lung carcinoma | D002289 | — | — | — | 3 | 2 | — | — | 3 |
| Hematologic neoplasms | D019337 | — | — | — | 3 | 2 | — | — | 3 |
| Neoplasms by histologic type | D009370 | — | — | — | 2 | 2 | — | — | 2 |
| Neoplasms by site | D009371 | — | — | — | 2 | 2 | — | — | 2 |
| Lymphoproliferative disorders | D008232 | Orphanet_2442 | D47.9 | — | 1 | 1 | — | — | 1 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | — | 1 | 1 | — | — | 1 |
| Glioma | D005910 | EFO_0000520 | — | — | 1 | 1 | — | — | 1 |
| Anaplastic thyroid carcinoma | D065646 | — | — | — | 1 | 1 | — | — | 1 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasm metastasis | D009362 | EFO_0009708 | — | — | 1 | — | — | 1 | 2 |
| Non-hodgkin lymphoma | D008228 | — | C85.9 | — | 1 | — | — | — | 1 |
| Unknown primary neoplasms | D009382 | — | — | — | 1 | — | — | — | 1 |
| Genomic instability | D042822 | — | — | — | 1 | — | — | — | 1 |
| Plasma cell neoplasms | D054219 | — | — | — | 1 | — | — | — | 1 |
| Cutaneous malignant melanoma | D000096142 | — | — | — | 1 | — | — | — | 1 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | — | 1 | — | — | — | 1 |
Indications Phases 1
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Indications Without Phase
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Vemurafenib |
| INN | vemurafenib |
| Description | Vemurafenib is a pyrrolopyridine that is 1H-pyrrolo[2,3-b]pyridine which is substituted at position 5 by a p-chlorophenyl group and at positions 3 by a 3-amino-2,6-difluorobenzoyl group, the amino group of which has undergone formal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases. It has a role as an antineoplastic agent and a B-Raf inhibitor. It is a pyrrolopyridine, a sulfonamide, a member of monochlorobenzenes, a difluorobenzene and an aromatic ketone. |
| Classification | Small molecule |
| Drug class | rapidly accelerated fibrosarcoma (RAF) kinase inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(Cl)cc4)cc23)c1F |
Identifiers
| PDB | — |
| CAS-ID | 918504-65-1 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1229517 |
| ChEBI ID | 63637 |
| PubChem CID | 42611257 |
| DrugBank | DB08881 |
| UNII ID | 207SMY3FQT (ChemIDplus, GSRS) |
Target
Agency Approved
BRAF
BRAF
Organism
Homo sapiens
Gene name
BRAF
Gene synonyms
BRAF1, RAFB1
NCBI Gene ID
Protein name
serine/threonine-protein kinase B-raf
Protein synonyms
94 kDa B-raf protein, B-Raf proto-oncogene serine/threonine-protein kinase (p94), B-Raf serine/threonine-protein, murine sarcoma viral (v-raf) oncogene homolog B1, p94, Proto-oncogene B-Raf, v-raf murine sarcoma viral oncogene homolog B, v-Raf murine sarcoma viral oncogene homolog B1
Uniprot ID
Mouse ortholog
Braf (109880)
serine/threonine-protein kinase B-raf (P28028)
Alternate
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Variants
No data
Financial
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Trends
PubMed Central
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Safety
Black-box Warning
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Adverse Events
Top Adverse Reactions
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12,869 adverse events reported
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