Drug Information

Drug (ID: DG01090) and It's Reported Resistant Information

• Name: Sitagliptin
• Synonyms: Sitagliptin; 486460-32-6; Januvia; Xelevia; MK-0431; (R)-3-AMINO-1-(3-(TRIFLUOROMETHYL)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL)-4-(2,4,5-TRIFLUOROPHENYL)BUTAN-1-ONE; UNII-QFP0P1DV7Z; Tesavel; LEZ763; QFP0P1DV7Z; (3R)-3-AMINO-1-[3-(TRIFLUOROMETHYL)-5H,6H,7H,8H-[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7-YL]-4-(2,4,5-TRIFLUOROPHENYL)BUTAN-1-ONE; (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; (2R)-4-OXO-4-[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE; 790712-60-6; CHEBI:40237; Sitagliptan; MK0431; Sitagliptin (Prop.INN); sitagliptina; sitagliptine; sitagliptinum; SR-05000001748; HSDB 7516; LEZ 763; (2R)-4-OXO-4-[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-A MINE; Sitagliptin (13); (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; Sitagliptin; MK0431; 1169707-31-6; EC 690-730-1; CHEMBL1422; SCHEMBL17783; BSPBio_002262; Triazolopiperazine Analogue 1; (3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; MLS006011959; Sitagliptin [USAN:INN:BAN]; GTPL6286; BDBM11162; C16H15F6N5O; AMY6930; DTXSID70197572; LEZ-763; 1x70; HMS2093F20; ACT02665; EX-A2816; Sitagliptin (Metformin,MK-0431); WHO 8692; ZINC1489478; MFCD09838015; NSC813215; AKOS015888724; CCG-268731; DB01261; MCULE-2101761133; NSC-813215; NCGC00178734-03; NCGC00178734-06; NCGC00178734-13; 7-((3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)buyl)-5,6,7,8-tetrahydro-3-trifluoromethyl)-1,4-triazolo(4,3-a); AS-19118; HY-13749; SMR002546724; SBI-0206871.P001; Sitagliptin 100 microg/mL in Acetonitrile; S5079; X4663; A14377; A25516; D08516; AB01563393_01; AR-270/43507782; Q419832; Q-101366; Q-201711; SR-05000001748-1; BRD-K19416115-001-01-2; BRD-K19416115-001-03-8; Z1541638523; (1R)-3-oxo-3-[3-(trifluoroethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorobenzyl)propylamine; (2r)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a] pyrazin-7(8h)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine; (2r)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl]-1-(2,4,5-trifluorophenyl)butan-2-a; (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-alpha]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine; (3r)-3-amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-5h-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; (3R)-3-amino-1-[3-(trifluoromethyl)-5H,6H,7H,8H-[1,2,4]triazolo[3,4-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one hydrochloride; (R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine; 1,2,4-Triazolo(4,3-a)pyrazine, 7-((3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-5,6,7,8-tetrahydor-3-(trifluoromethyl)-; 1,2,4-Triazolo[4,3-a]pyrazine,7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-; 3-oxo-1-(2,4,5-trifluorobenzyl)-3-(3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)propylamine; 7-[(3r)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine
• Indication:
  In total 4 Indication(s)
  Type-2 diabetes [ICD-11: 5A11]; Approved; [1]
  Type-2 diabetes [ICD-11: 5A11]; Phase 3; [1]
  Type-2 diabetes [ICD-11: 5A11]; Phase 3; [1]
  Peripheral arterial disease [ICD-11: BD4Z]; Phase 1; [1]
• Target: .; NOUNIPROTAC; [1]
• Formula: C16H15F6N5O
• IsoSMILES: C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N
• InChI: 1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1
• InChIKey: MFFMDFFZMYYVKS-SECBINFHSA-N
• PubChem CID: 4369359
• TTD Drug ID: D05RTM
• VARIDT ID: DR00254
• INTEDE ID: DR1490
• DrugBank ID: DB01261

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-05: Endocrine/nutritional/metabolic diseases

Insulin-resistance syndrome [ICD-11: 5A44]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Dipeptidyl peptidase 4 (DPP4) [1]

• Molecule Alteration: Function; Inhibition
• Sensitive Disease: Insulin-resistance syndrome [ICD-11: 5A44.0]
• Experimental Note: Identified from the Human Clinical Data
• Mechanism Description: Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is currently indicated as an adjunctive treatment to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (DM). Sitagliptin is used to help mitigate insulin resistance after burn injury.

References

• Ref 1: Evaluation of the use of sitagliptin for insulin resistance in burn patients .Int J Burns Trauma. 2020 Oct 15;10(5):237-245. eCollection 2020.