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

General Information of Drug (ID: DM457B1)

Drug Name
FK-888 Drug Info
Synonyms
FK 888; FK-888; 138449-07-7; FK888; N(2)-(4-Hydroxy-1-(1-methyl-1H-indol-3-yl)carbonyl-L-prolyl)-N-methyl-N-phenylmethyl-3-(2-naphthyl)-L-alaninamide; SCHEMBL8079679; GTPL2114; AC1L332N; CHEMBL1416993; CHEBI:93463; DTXSID70160680; MolPort-023-276-412; HMS3269A13; ZINC3926844; PDSP2_000648; AKOS024457076; NCGC00159560-01; L-Alaninamide, trans-4-hydroxy-1-((1-methyl-1H-indol-3-yl)carbonyl)-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-; LS-193299; BRD-K83508485-001-01-9
Indication
Disease Entry ICD 11 Status REF
Migraine 8A80 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
107967
ChEBI ID
CHEBI:93463
CAS Number
CAS 138449-07-7
TTD Drug ID
DM457B1

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
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]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

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

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: 2114).
2 Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist, FK888. Br J Pharmacol. 1992 Nov;107(3):785-9.
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.