Chemical: Drug
vemurafenib
PharmGKB contains no prescribing info for this . Contact us to report known genotype-based dosing guidelines, or if you are interested in developing guidelines.
Annotated Labels
- Annotation of FDA Label for vemurafenib and BRAF,NRAS
- Annotation of EMA Label for vemurafenib and BRAF
- Annotation of PMDA Label for vemurafenib and BRAF
- Annotation of HCSC Label for vemurafenib and BRAF
1. Annotation of FDA Label for vemurafenib and BRAF,NRAS
Summary
Vemurafenib is a kinase inhibitor used to treat patients with unresectable or metastatic melanoma ONLY in cases where the BRAF V600E mutation is found by an FDA-approved test. In vitro evidence points to BRAF wild-type cells proliferation with exposure to BRAF inhibitors. Therefore, testing is required. Additionally, the label notes progression of pre-existing chronic myelomonocytic leukemia with NRAS mutation in postmarketing experience.
There's more of this label. Read more.
2. Annotation of EMA Label for vemurafenib and BRAF
Summary
The EMA European Public Assessment Report (EPAR) for vemurafenib (Zelboraf) requires testing of tumours for the BRAF V600 mutation prior to initiating treatment.
There's more of this label. Read more.
3. Annotation of PMDA Label for vemurafenib and BRAF
Summary
The PMDA package insert for vemurafenib (ZELBORAF) states that it is indicated for patients with unresectable, refractory melanoma with BRAF gene mutation.
There's more of this label. Read more.
4. Annotation of HCSC Label for vemurafenib and BRAF
Summary
The product monograph for vemurafenib (ZELBORAF) states that it is indicated for the treatment of patients with BRAF V600 mutation-positive melanoma, and that it should not be used in patients with BRAF wild-type melanoma.
There's more of this label. Read more.
PharmGKB contains no Clinical Variants that meet the highest level of criteria.
Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.
The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.
The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.
The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.
Links in the "Gene" column lead to PharmGKB Gene Pages.
List of all variant annotations for vemurafenib
| Gene ? |
Variant?
(147) |
Alternate Names ? | Chemicals ? |
Alleles
?
(+ chr strand) |
Function ? |
Amino Acid?
Translation |
|
|---|---|---|---|---|---|---|---|
| rs113488022 | NC_000007.13:g.140453136A>C, NC_000007.13:g.140453136A>G, NC_000007.13:g.140453136A>T, NC_000007.14:g.140753336A>C, NC_000007.14:g.140753336A>G, NC_000007.14:g.140753336A>T, NG_007873.3:g.176429T>A, NG_007873.3:g.176429T>C, NG_007873.3:g.176429T>G, NM_004333.4:c.1799T>A, NM_004333.4:c.1799T>C, NM_004333.4:c.1799T>G, NP_004324.2:p.Val600Ala, NP_004324.2:p.Val600Glu, NP_004324.2:p.Val600Gly, XM_005250045.1:c.1799T>A, XM_005250045.1:c.1799T>C, XM_005250045.1:c.1799T>G, XM_005250046.1:c.1799T>A, XM_005250046.1:c.1799T>C, XM_005250046.1:c.1799T>G, XM_005250047.1:c.1799T>A, XM_005250047.1:c.1799T>C, XM_005250047.1:c.1799T>G, XM_011516529.1:c.1799T>A, XM_011516529.1:c.1799T>C, XM_011516529.1:c.1799T>G, XM_011516530.1:c.1695-3918T>A, XM_011516530.1:c.1695-3918T>C, XM_011516530.1:c.1695-3918T>G, XP_005250102.1:p.Val600Ala, XP_005250102.1:p.Val600Glu, XP_005250102.1:p.Val600Gly, XP_005250103.1:p.Val600Ala, XP_005250103.1:p.Val600Glu, XP_005250103.1:p.Val600Gly, XP_005250104.1:p.Val600Ala, XP_005250104.1:p.Val600Glu, XP_005250104.1:p.Val600Gly, XP_011514831.1:p.Val600Ala, XP_011514831.1:p.Val600Glu, XP_011514831.1:p.Val600Gly, XR_242190.1:n.1807T>A, XR_242190.1:n.1807T>C, XR_242190.1:n.1807T>G, XR_927520.1:n.1807T>A, XR_927520.1:n.1807T>C, XR_927520.1:n.1807T>G, XR_927521.1:n.1807T>A, XR_927521.1:n.1807T>C, XR_927521.1:n.1807T>G, XR_927522.1:n.1703-3918T>A, XR_927522.1:n.1703-3918T>C, XR_927522.1:n.1703-3918T>G, XR_927523.1:n.1703-3918T>A, XR_927523.1:n.1703-3918T>C, XR_927523.1:n.1703-3918T>G |
A > T
|
SNP |
V600E
|
Overview
- PLX4032
- Zelboraf
PharmGKB Accession Id
PA165946873
Type(s):
Drug
Description
Vemurafenib is a novel, oral small molecule designed to treat melanoma and other cancers harboring the oncogenic V600E BRAF mutation (rs113488022) [Article:22646766]. It can also inhibit non-mutant BRAF and RAF1 and showed activity against ACK1 (also known as TNK2), KHS1 (MAP4K5) and SRMS in vitro [Article:22646766].
Source: PharmGKB [Article:22646766]
Indication
Vemurafenib is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma with the BRAF V600E mutation.
Source: PharmGKB
Other Vocabularies
- ATC: Protein kinase inhibitors (L01XE)
- UMLS: Vemurafenib (C3192263)
- RxNorm: Vemurafenib (1147220)
- NDFRT: VEMURAFENIB (N0000183250)
Information pulled from DrugBank has not been reviewed by PharmGKB.
Chemical Properties
SMILES
CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F
Source: PubChem
InChI String
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
Source: PubChem
IUPAC Names
- N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
PharmGKB Curated Pathways
Pathways created internally by PharmGKB based primarily on literature evidence.
-
Vemurafenib Pathway, Pharmacodynamics
Simplified diagram of mechanism of action of vemurafenib and downstream signaling effects.
Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.
Curated Information ?
Drug Targets
| Gene | Description |
|---|---|
| BRAF | (source: PharmGKB ) |
Curated Information ?
| Evidence | Disease |
|---|---|
|
Melanoma |
