Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM62UG5)

Drug Name
Vemurafenib Drug Info
Synonyms PLX4032; RG7204; RO5185426; Zelboraf (TN); Vemurafenib (BRAF inhibitor)
Indication
Disease Entry ICD 11 Status REF
Melanoma 2C30 Approved [1]
Cross-matching ID
PubChem CID
42611257
ChEBI ID
CHEBI:63637
CAS Number
CAS 918504-65-1
TTD Drug ID
DM62UG5
VARIDT Drug ID
DR00711
INTEDE Drug ID
DR1677
ACDINA Drug ID
D00723

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Serine/threonine-protein kinase B-raf (BRAF) TTWCGQT BRAF_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [3]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [3]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Serine/threonine-protein kinase B-raf (BRAF) DTT BRAF 6.409 7.097 6.062 6.049
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Melanoma
ICD Disease Classification 2C30
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Serine/threonine-protein kinase B-raf (BRAF) DTT BRAF 3.00E-01 0.1 0.2
P-glycoprotein 1 (ABCB1) DTP P-GP 9.48E-02 1.45E-01 2.92E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 7.57E-04 7.55E-03 3.42E-02
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 5.98E-03 9.85E-03 5.46E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.75E-01 3.78E-02 1.44E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5893).
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
4 Differential effects of the oncogenic BRAF inhibitor PLX4032 (vemurafenib) and its progenitor PLX4720 on ABCB1 function. J Pharm Pharm Sci. 2014;17(1):154-68.
5 Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43.