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

General Information of Drug (ID: DMM74PK)

Drug Name
Atrasentan Drug Info
Synonyms
Xinlay; Atrasentan [INN]; A 127722; A 147627; ABT 627; A-127722; A-147627; ABT-627; Xinlay (TN); A-127722.5; (+)-A 127722; (+)-A-127722; (11C)ABT-627; (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid; 2-(4-methoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(((dibutylamino)carbonyl)methyl)pyrrolidine-3-carboxylic acid; 2R-(4-methoxyphenyl)-4S(1,3-benzodioxol-5-yl)-1-(N,N-di(n-butyl)aminocarbonyl-methyl)-pyrrolidine-3R-carboxylic acid
Indication
Disease Entry ICD 11 Status REF
Diabetic nephropathy GB61.Z Phase 3 [1]
Prostate cancer 2C82.0 Withdrawn from market [2] , [3]
Cross-matching ID
PubChem CID
159594
ChEBI ID
CHEBI:135810
CAS Number
CAS 173937-91-2
TTD Drug ID
DMM74PK
VARIDT Drug ID
DR01433
INTEDE Drug ID
DR1899

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Antagonist [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Phase 3 [5]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Phase 3 [6]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Phase 3 [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 3 [7]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Endothelin A receptor (EDNRA) DTT EDNRA 3.776 4.505 5.121 3.536
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
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 Diabetic nephropathy
ICD Disease Classification GB61.Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Endothelin A receptor (EDNRA) DTT EDNRA 5.13E-01 -0.82 -0.79
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 5.69E-01 -2.39E-02 -2.71E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 7.67E-01 0.00E+00 0.00E+00
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 7.18E-01 -5.08E-02 -4.53E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 -2.60E-02 -3.37E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 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: 3487).
3 Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
4 Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
5 Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther. 2006 Mar;79(3):186-96.
6 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
7 Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther. 2006 Mar;79(3):186-96.