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

General Information of Drug (ID: DMJ0QOW)

Drug Name
Rilpivirine Drug Info
Synonyms
500287-72-9; TMC278; Edurant; TMC 278; UNII-FI96A8X663; R278474; TMC-278; 4-{[4-({4-[(E)-2-Cyanoethenyl]-2,6-Dimethylphenyl}amino)pyrimidin-2-Yl]amino}benzonitrile; CHEBI:68606; FI96A8X663; R 278474; 4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile; (E)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile; (E)-4-(4-(4-(2-cyanovinyl)-2,6-dimethylphenylamino)pyrimidin-2-ylamino)benzonitrile; W-202888; RPV; Mu O-conotoxin
Indication
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Approved [1]
Pain MG30-MG3Z Investigative [2]
Cross-matching ID
PubChem CID
6451164
ChEBI ID
CHEBI:68606
CAS Number
CAS 500287-72-9
TTD Drug ID
DMJ0QOW
INTEDE Drug ID
DR1424
ACDINA Drug ID
D00594

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Human immunodeficiency virus Reverse transcriptase (HIV RT) TT84ETX POL_HV1B1 Inhibitor [3]
Voltage-gated sodium channel alpha Nav1.8 (SCN10A) TT90XZ8 SCNAA_HUMAN Inhibitor [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [5]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [6]
UDP-glucuronosyltransferase 1A4 (UGT1A4) DELOY3P UD14_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
Voltage-gated sodium channel alpha Nav1.8 (SCN10A) DTT SCN10A 6.276 5.928 6.19 6.363
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
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 Human immunodeficiency virus infection
ICD Disease Classification 1C62
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Voltage-gated sodium channel alpha Nav1.8 (SCN10A) DTT SCN10A 9.89E-01 -0.16 -0.31
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 3.80E-01 -9.11E-03 -3.47E-02
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 1.65E-02 -4.37E-02 -7.84E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 6.90E-01 2.35E-02 7.88E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
2 Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian senso... J Biol Chem. 2004 Jun 11;279(24):25774-82.
3 Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416.
4 Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7.
5 Human biotransformation of the nonnucleoside reverse transcriptase inhibitor rilpivirine and a cross-species metabolism comparison. Antimicrob Agents Chemother. 2013 Oct;57(10):5067-79.
6 Population pharmacokinetics and pharmacogenetics analysis of rilpivirine in HIV-1-infected individuals. Antimicrob Agents Chemother. 2016 Dec 27;61(1).