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

General Information of Drug (ID: DMLY9F1)

• Drug Name: AZETIRELIN Drug Info
• Synonyms: Azetirelin; YM-14673 (dihydrate); Nalpha-[(S)-2-Azetidinone-4-carbonyl]-L-histidyl-L-prolinamide

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 65841
  CAS Number: CAS 95729-65-0
  TTD Drug ID: DMLY9F1
  INTEDE Drug ID: DR2422

Molecule-Related Drug Atlas

Drug(s) Targeting Thyrotropin-releasing hormone receptor (TRHR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
protirelin	DMGN5QD	Central nervous system disease	8A04-8D87	Approved	[5]
MONTIRELIN TETRAHYDRATE	DM31OGZ	Pain	MG30-MG3Z	Discontinued in Preregistration	[6]
Posatirelin	DML6EWH	Neurodegenerative disorder	8A20-8A23	Discontinued in Phase 3	[7]
JTP-2942	DM29C6S	Cognitive impairment	6D71	Discontinued in Phase 2	[8]
MK-771	DM4YQV0	Discovery agent	N.A.	Investigative	[9]
CORYMBONE B	DM463S2	Discovery agent	N.A.	Investigative	[10]
C4X-101	DM5971G	Endocrine disease	5B3Z	Investigative	[11]
MeTRH	DMGH8WV	Discovery agent	N.A.	Investigative	[12]

Drug(s) Metabolized By Tripeptidase (pepT)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Glypromate	DM0OX31	Neurological disorder	6B60	Phase 4	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Thyrotropin-releasing hormone receptor (TRHR)	TT4J8MF	TRFR_HUMAN	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Tripeptidase (pepT) Main DME	DEIZ2D9	PEPT_LACLL	Substrate	[3] , [4]

References

• [1] Developing a metagenomic view of xenobiotic metabolism. Pharmacol Res. 2013 March; 69(1): 21-31.
• [2] Intestinal absorption of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue. II. In situ and in vitro absorption characteristics of azetirelin from the rat intestine. Biol Pharm Bull. 1995 Jul;18(7):976-9.
• [3] Metabolism of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue, by intestinal microorganisms. Pharm Res. 1997 Aug;14(8):1004-7.
• [4] Intestinal absorption of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue. I. Possible factors for the low oral bioavailability in rats. Biol Pharm Bull. 1994 Sep;17(9):1256-61.
• [5] Company report (takeda)
• [6] Montirelin hydrate (NS-3), a TRH analog, improved the disturbance of consciousness caused by head concussion and pentobarbital in mice. Nihon Yakurigaku Zasshi. 1996 May;107(5):237-45.
• [7] TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin. Acta Pharm Hung. 2002;72(1):62-8.
• [8] Effect of JTP-2942, a novel thyrotropin-releasing hormone analogue, on pentobarbital-induced anesthesia in rats. Eur J Pharmacol. 1995 Mar 24;276(1-2):177-82.
• [9] TRH analog MK-771 reverses neurochemical and learning deficits in medial septal-lesioned rats. Peptides. 1989 Jan-Feb;10(1):121-4.
• [10] Corymbones A and B, phloroglucinols with thyrotropin releasing hormone receptor 2 binding affinity from the flowers of Corymbia peltata. J Nat Prod. 2008 May;71(5):881-3.
• [11] 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: 363).
• [12] Thyrotropin-releasing hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin actions in the CNS of mice. Neuropsychopharmacology. 2013 May;38(6):950-6.
• [13] Tripeptidase gene (pepT) of Lactococcus lactis: molecular cloning and nucleotide sequencing of pepT and construction of a chromosomal deletion mutant. J Bacteriol. 1994 May;176(10):2854-61.