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

General Information of Drug (ID: DM81UJW)

• Drug Name: LY-2590443 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Migraine	8A80	Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DM81UJW

Molecule-Related Drug Atlas

Drug(s) Targeting Substance-P receptor (TACR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aprepitant	DM053KT	Depression	6A70-6A7Z	Approved	[3]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[4]
Rolapitant	DM8XP26	Chemotherapy-induced nausea	MD90	Approved	[5]
Netupitant	DMEKAYI	Chemotherapy-induced nausea	MD90	Phase 3	[5]
Serlopitant	DM5VH6U	Prurigo nodularis	EC91.0	Phase 3	[6]
LY-686017	DM7WORZ	Atopic dermatitis	EA80	Phase 3	[7]
Elinzanetant	DMC6EFI	Hot flushes	GA30	Phase 3	[8]
CP-122721	DMSWLM5	Major depressive disorder	6A70.3	Phase 2	[9]
FR139317	DMEL5SV	Hypertension	BA00-BA04	Phase 2	[4]
VOFOPITANT HYDROCHLORIDE	DMQMYP5	Vomiting	MD90	Phase 2	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[2]

References

• [1] ClinicalTrials.gov (NCT00804973) Study in Subjects With Acute Migraines Headaches.. U.S. National Institutes of Health.
• [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: 360).
• [3] Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
• [4] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [5] Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
• [8] Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
• [9] A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
• [10] Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.