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

General Information of Drug (ID: DMB9861)

Drug Name
Rilapladib Drug Info
Indication
Disease Entry ICD 11 Status REF
Arteriosclerosis BD40 Phase 1 [1] , [2]
Cardiovascular disease BA00-BE2Z Phase 1 [2]
Cross-matching ID
PubChem CID
9918381
CAS Number
CAS 412950-08-4
TTD Drug ID
DMB9861

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Phospholipase A2 (PLA2G1B) TT9V5JH PA21B_HUMAN Modulator [3]
Platelet-activating factor acetylhydrolase (PLA2G7) TTDNFMT PAFA_HUMAN Inhibitor [4] , [5]
Thymidine kinase 1 (TK1) TTP3QRF KITH_HUMAN Inhibitor [6]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Thymidine kinase 1 (TK1) DTT TK1 5.524 5.296 5.963 6.272
Platelet-activating factor acetylhydrolase (PLA2G7) DTT PLA2G7 5.609 5.198 3.818 4.385
Phospholipase A2 (PLA2G1B) DTT PLA2G1B 5.385 3.733 4.178 5.278
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 Arteriosclerosis
ICD Disease Classification BD40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Platelet-activating factor acetylhydrolase (PLA2G7) DTT PLA2G7 5.33E-03 0.09 0.23
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: 7376).
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018454)
3 Effect of treatment for 12 weeks with rilapladib, a lipoprotein-associated phospholipase A2 inhibitor, on arterial inflammation as assessed with 18F-fluorodeoxyglucose-positron emission tomography imaging.J Am Coll Cardiol.2014 Jan 7-14;63(1):86-8.
4 Phospholipase A2 inhibitors. Curr Opin Lipidol. 2009 Aug;20(4):327-32.
5 THERAPEUTICS: Rilapladib
6 Trichomonas vaginalis thymidine kinase: purification, characterization and search for inhibitors. Biochem J. 1998 Aug 15;334 ( Pt 1):15-22.