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

General Information of Drug (ID: DMGXENV)

Drug Name
Saxagliptin Drug Info
Synonyms
Onglyza; BMS 477118-11; BMS-477118; Kombiglyze XR (TN); OPC-262; Onglyza (TN); BMS-477118-11; (1S,5S)-2-[2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-amino(3-hydroxytricyclo[3.3
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Approved [1]
Cross-matching ID
PubChem CID
11243969
ChEBI ID
CHEBI:71272
CAS Number
CAS 361442-04-8
TTD Drug ID
DMGXENV
VARIDT Drug ID
DR00226
INTEDE Drug ID
DR1465
ACDINA Drug ID
D00616

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dipeptidyl peptidase 4 (DPP-4) TTDIGC1 DPP4_HUMAN Inhibitor [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 4C1 (SLCO4C1) DTY0QMU SO4C1_HUMAN Approved [3]
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Approved [4]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Approved [3]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [6]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [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
Dipeptidyl peptidase 4 (DPP-4) DTT DPP4 4.995 4.926 7.852 8.358
Organic anion transporting polypeptide 4C1 (SLCO4C1) DTP OATP4C1 4.133 4.508 5.612 3.7
Organic anion transporter 3 (SLC22A8) DTP OAT3 2.722 2.07 8.103 3.597
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Multidrug resistance-associated protein 1 (ABCC1) DTP MRP1 4.838 6.296 5.935 6.146
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
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 Type-2 diabetes
ICD Disease Classification 5A11
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Dipeptidyl peptidase 4 (DPP-4) DTT DPP4 9.54E-01 -0.27 -1.85
Organic anion transporting polypeptide 4C1 (SLCO4C1) DTP OATP4C1 9.91E-01 2.18E-01 6.01E-01
Organic anion transporter 3 (SLC22A8) DTP OAT3 6.49E-01 3.37E-03 6.66E-02
P-glycoprotein 1 (ABCB1) DTP P-GP 2.30E-01 3.06E-01 7.43E-01
Multidrug resistance-associated protein 1 (ABCC1) DTP MRP1 3.82E-01 1.16E-01 9.50E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 8.58E-01 -3.73E-03 -1.00E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.76E-01 -4.64E-01 -9.16E-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: 6316).
2 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
3 Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14.
4 Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88.
5 Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
6 Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol. 2011 Jul;72(1):92-102.