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 | 2024-07-05 |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
VEMURAFENIB, ZELBORAF, HOFFMANN LA ROCHE | |||
| 2024-11-06 | ODE-158 | ||
HCPCS
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Clinical
Clinical Trials
170 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 | — | — | 5 | 7 | 3 | — | — | 13 |
| Thyroid neoplasms | D013964 | EFO_0003841 | — | 2 | 5 | 1 | — | 2 | 9 |
| Carcinoma | D002277 | — | C80.0 | 2 | 4 | 1 | — | 1 | 7 |
| Multiple myeloma | D009101 | — | C90.0 | 2 | 5 | 1 | — | 1 | 7 |
| Thyroid diseases | D013959 | HP_0000820 | E00-E07 | 2 | 4 | 1 | — | 1 | 7 |
| Non-small-cell lung carcinoma | D002289 | — | — | — | 6 | 2 | — | — | 6 |
| Hematologic neoplasms | D019337 | — | — | 1 | 4 | 2 | — | — | 5 |
| Glioma | D005910 | EFO_0000520 | — | 1 | 3 | 1 | — | — | 4 |
| Papillary thyroid cancer | D000077273 | — | — | 1 | 3 | 1 | — | — | 4 |
| Cutaneous malignant melanoma | D000096142 | — | — | — | 2 | 1 | — | — | 3 |
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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 | — | 3 | 5 | — | — | — | 8 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 1 | 6 | — | — | — | 7 |
| Recurrence | D012008 | — | — | 4 | 2 | — | — | — | 6 |
| Leukemia | D007938 | — | C95 | 1 | 4 | — | — | — | 5 |
| Non-hodgkin lymphoma | D008228 | — | C85.9 | 1 | 4 | — | — | — | 5 |
| Histiocytosis | D015614 | HP_0100727 | — | — | 5 | — | — | — | 5 |
| Lymphoma | D008223 | — | C85.9 | 2 | 3 | — | — | — | 4 |
| Plasma cell neoplasms | D054219 | — | — | 2 | 2 | — | — | 1 | 4 |
| Hairy cell leukemia | D007943 | — | C91.4 | — | 4 | — | — | — | 4 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 2 | 1 | — | — | — | 3 |
Show 37 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Prostatic neoplasms | D011471 | — | C61 | 2 | — | — | — | 1 | 3 |
| Myelodysplastic syndromes | D009190 | — | D46 | 1 | — | — | — | — | 1 |
| Myeloid leukemia acute | D015470 | — | C92.0 | 1 | — | — | — | — | 1 |
| Castration-resistant prostatic neoplasms | D064129 | — | — | 1 | — | — | — | — | 1 |
| Myeloproliferative disorders | D009196 | — | D47.1 | 1 | — | — | — | — | 1 |
| Primary myelofibrosis | D055728 | — | D47.4 | 1 | — | — | — | — | 1 |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | — | — | 1 | — | — | — | — | 1 |
| B-cell chronic lymphocytic leukemia | D015451 | — | C91.1 | 1 | — | — | — | — | 1 |
| Bcr-abl positive chronic myelogenous leukemia | D015464 | EFO_0000340 | — | 1 | — | — | — | — | 1 |
| Myelomonocytic leukemia chronic | D015477 | — | C93.1 | 1 | — | — | — | — | 1 |
Show 14 more
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Phototoxic dermatitis | D017484 | — | — | — | — | — | — | 1 | 1 |
| Renal cell carcinoma | D002292 | EFO_0000376 | — | — | — | — | — | 1 | 1 |
| Hepatocellular carcinoma | D006528 | — | C22.0 | — | — | — | — | 1 | 1 |
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | — | — | — | — | 1 | 1 |
| Colonic neoplasms | D003110 | — | C18 | — | — | — | — | 1 | 1 |
| Molecular targeted therapy | D058990 | — | — | — | — | — | — | 1 | 1 |
| Feasibility studies | D005240 | — | — | — | — | — | — | 1 | 1 |
| Healthy volunteers/patients | — | — | — | — | — | — | — | 1 | 1 |
| Contraceptive effectiveness | D000073516 | — | — | — | — | — | — | 1 | 1 |
| Uveal neoplasms | D014604 | EFO_1001230 | — | — | — | — | — | 1 | 1 |
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
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Financial
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Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
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12,330 adverse events reported
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