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

General Information of Drug (ID: DM5FABJ)

Drug Name
LAROPIPRANT Drug Info
Synonyms
Laropiprant; 571170-77-9; MK 0524; Cardaptive; MK-0524; UNII-G7N11T8O78; CHEMBL426559; G7N11T8O78; 2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid; 2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methanesulfonyl-1H,2H,3H,4H-cyclopenta[b]indol-3-yl]acetic acid; Tedaptive; Laropiprant [USAN:INN:BAN]; [14C]-Laropiprant; Laropiprant/MK-0524; Laropiprant (INN/USAN); Laropiprant (MK-0524); SCHEMBL991107; AMOT0189; GTPL3356; KS-00000XIE; CTK8F0660; MK-0524B
Indication
Disease Entry ICD 11 Status REF
Coronary heart disease BA80.Z Phase 4 [1]
Arteriosclerosis BD40 Discontinued in Phase 3 [2]
Cross-matching ID
PubChem CID
9867642
ChEBI ID
CHEBI:135942
CAS Number
CAS 571170-77-9
TTD Drug ID
DM5FABJ

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
HMG-CoA reductase (HMGCR) TTPADOQ HMDH_HUMAN Inhibitor [3]
Prostacyclin receptor (PTGIR) TTOFYT1 PI2R_HUMAN Inhibitor [4]
Prostaglandin D2 receptor (PTGDR) TTNVEIR PD2R_HUMAN Inhibitor [4]
Prostaglandin D2 receptor 2 (PTGDR2) TTQDMX5 PD2R2_HUMAN Inhibitor [4]
Prostaglandin E2 receptor EP2 (PTGER2) TT1ZAVI PE2R2_HUMAN Inhibitor [4]
Prostaglandin F2-alpha receptor (PTGFR) TTT2ZAR PF2R_HUMAN Inhibitor [4]
Thromboxane A2 receptor (TBXA2R) TT2O84V TA2R_HUMAN Inhibitor [4]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Prostaglandin F2-alpha receptor (PTGFR) DTT PTGFR 0.379 2.744 3.609 1.138
Prostaglandin D2 receptor 2 (PTGDR2) DTT PTGDR2 4.436 5.954 4.217 4.641
HMG-CoA reductase (HMGCR) DTT HMGCR 6.357 6.256 5.17 6.85
Prostacyclin receptor (PTGIR) DTT PTGIR 6.384 3.7 4.684 4.603
Prostaglandin D2 receptor (PTGDR) DTT PTGDR 1.609 4.087 1.433 1.963
Thromboxane A2 receptor (TBXA2R) DTT TBXA2R 6.075 5.925 6.729 6.096
Prostaglandin E2 receptor EP2 (PTGER2) DTT PTGER2 4.75 5.888 5.066 4.466
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 Coronary heart disease
ICD Disease Classification BA80.Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Prostaglandin F2-alpha receptor (PTGFR) DTT PTGFR 8.25E-02 -0.05 -0.14
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 ClinicalTrials.gov (NCT01126073) A Double Blind, Randomized Study to Compare Influence of Niacin/Laropiprant on Functional and Morphological Characteristics of Arterial Wall and Parameters of Inflammation in Subjects With Coronary Heart Disease Already Treated With a Statin in Miran Sebestjen, University Medical Centre Ljubljana.
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023729)
3 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
4 Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.