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
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
Trade Name
FDA
EMA
Zelboraf
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Vemurafenib
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| ZELBORAF | Roche | N-202429 RX | 2011-08-17 | 1 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| zelboraf | New Drug Application | 2018-12-13 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| melanoma | — | D008545 | — |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
VEMURAFENIB, ZELBORAF, HOFFMANN LA ROCHE | |||
| 2024-11-06 | ODE-158 | ||
HCPCS
No data
Clinical
Clinical Trials
143 clinical trials
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Mock data
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Colorectal neoplasms | D015179 | 5 | 4 | — | — | — | 8 | ||
| Non-hodgkin lymphoma | D008228 | C85.9 | 1 | 4 | — | — | — | 5 | |
| Thyroid neoplasms | D013964 | EFO_0003841 | 2 | 2 | — | — | 1 | 5 | |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 1 | 2 | — | — | — | 3 |
| Multiple myeloma | D009101 | C90.0 | 1 | 2 | — | — | — | 3 | |
| Langerhans-cell histiocytosis | D006646 | C96.6 | — | 3 | — | — | — | 3 | |
| Hairy cell leukemia | D007943 | C91.4 | — | 3 | — | — | — | 3 | |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 1 | 1 | — | — | — | 2 |
| Sarcoma | D012509 | — | 2 | — | — | — | 2 | ||
| Neuroblastoma | D009447 | EFO_0000621 | — | 2 | — | — | — | 2 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Myelodysplastic syndromes | D009190 | D46 | 1 | — | — | — | — | 1 | |
| Myeloid leukemia acute | D015470 | C92.0 | 1 | — | — | — | — | 1 | |
| Prostatic neoplasms | D011471 | C61 | 1 | — | — | — | — | 1 | |
| Castration-resistant prostatic neoplasms | D064129 | 1 | — | — | — | — | 1 | ||
| Primary myelofibrosis | D055728 | D47.4 | 1 | — | — | — | — | 1 | |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | C91.0 | 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 | |
| Anemia | D000740 | EFO_0004272 | D64.9 | 1 | — | — | — | — | 1 |
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Indications Without Phase
No data
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 | 3OG7 |
| CAS-ID | 918504-65-1 |
| RxCUI | 1147220 |
| 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
RAF1
RAF1
Organism
Homo sapiens
Gene name
RAF1
Gene synonyms
RAF
NCBI Gene ID
Protein name
RAF proto-oncogene serine/threonine-protein kinase
Protein synonyms
C-Raf proto-oncogene, serine/threonine kinase, cRaf, Oncogene RAF1, Proto-oncogene c-RAF, raf proto-oncogene serine/threonine protein kinase, Raf-1, v-raf-1 murine leukemia viral oncogene homolog 1, v-raf-1 murine leukemia viral oncogene-like protein 1
Uniprot ID
Mouse ortholog
Raf1 (110157)
RAF proto-oncogene serine/threonine-protein kinase (Q9QUU8)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
0 adverse events reported
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