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

General Information of Drug (ID: DMGJCDR)

• Drug Name: Teneligliptin Drug Info
• Synonyms: Teneligliptin; 760937-92-6; UNII-28ZHI4CF9C; Teneligliptin [INN]; 28ZHI4CF9C; Teneligliptin hydrobromide; CHEMBL2147777; MP-513; Teneligliptin (INN); [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone; C22H30N6OS; {(2s,4s)-4-[4-(3-Methyl-1-Phenyl-1h-Pyrazol-5-Yl)piperazin-1-Yl]pyrrolidin-2-Yl}(1,3-Thiazolidin-3-Yl)methanone; 906093-29-6; Teneli; SCHEMBL161778; GTPL9906; WGRQANOPCQRCME-PMACEKPBSA-N; CHEBI:136042; MolPort-039-139-824; MP513; ZINC36520254; BDBM50391565

Indication

Disease Entry	ICD 11	Status	REF
Type-2 diabetes	5A11	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 11949652
  ChEBI ID: CHEBI:136042
  CAS Number: CAS 760937-92-6
  TTD Drug ID: DMGJCDR
  INTEDE Drug ID: DR1809

Molecule-Related Drug Atlas

Drug(s) Targeting Dipeptidyl peptidase 4 (DPP-4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Saxagliptin	DMGXENV	Type-2 diabetes	5A11	Approved	[4]
Sitagliptin	DMGDKXN	Cystic fibrosis	CA25	Approved	[5]
Alogliptin	DM8WI3R	Type-2 diabetes	5A11	Approved	[6]
Linagliptin	DMWFJTR	Non-insulin dependent diabetes	5A11	Approved	[7]
Vildagliptin	DMYN59P	Type-2 diabetes	5A11	Approved	[8]
Dapagliflozin Propanediol; Saxagliptin Hydrochloride	DM34TXO	Type-2 diabetes	5A11	Approved	[9]
Anagliptin	DMJXIC9	Type-2 diabetes	5A11	Approved	[10]
SaxaDapa FDC	DMAPRWV	Diabetic complication	5A2Y	Phase 3	[11]
LC-150444	DM09RKB	Type-2 diabetes	5A11	Phase 3	[12]
Dutogliptin	DMM5VTA	Type-2 diabetes	5A11	Phase 3	[13]

Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[14]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[15]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[16]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[17]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[19]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[20]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[21]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[15]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dipeptidyl peptidase 4 (DPP-4)	TTDIGC1	DPP4_HUMAN	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[3]

References

• [1] ClinicalTrials.gov (NCT02449330) Teneligliptin on the Progressive Left Ventricular Diastolic Dysfunction With Type 2 Diabetes Mellitus Study.
• [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. (Target id: 1612).
• [3] Effect of glimepiride on the pharmacokinetics of teneligliptin in healthy Korean subjects. J Clin Pharm Ther. 2019 Oct;44(5):720-725.
• [4] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [5] Novel therapeutics for type 2 diabetes: incretin hormone mimetics (glucagon-like peptide-1 receptor agonists) and dipeptidyl peptidase-4 inhibitors. Pharmacol Ther. 2009 Oct;124(1):113-38.
• [6] Clinical pipeline report, company report or official report of Takeda (2009).
• [7] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [8] Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [10] Diabetes Treatment. Diabetes Care. 2009 March; 32(3): e25-e30.
• [11] Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for type 2 diabetes. Cardiol Rev. 2010 Jul-Aug;18(4):213-7.
• [12] Clinical pipeline report, company report or official report of ShangHai APIs Chemical.
• [13] Dutogliptin, a selective DPP4 inhibitor, improves glycaemic control in patients with type 2 diabetes: a 12-week, double-blind, randomized, placebo-controlled, multicentre trial. Diabetes Obes Metab. 2010 Apr;12(4):348-55.
• [14] Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
• [15] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [16] Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
• [17] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [18] Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
• [19] Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
• [20] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [21] The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
• [22] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.