General Information of Drug (ID: DM1JUS0)

Drug Name
FK-224 Drug Info
Synonyms FR-115224
Indication
Disease Entry ICD 11 Status REF
Asthma CA23 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
6437864
CAS Number
CAS 125787-94-2
TTD Drug ID
DM1JUS0

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
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)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ibodutant DMT67EH Irritable bowel syndrome DD91.0 Phase 3 [11]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [12]
Rambazole DMP2DNS Psoriasis vulgaris EA90 Phase 2 [13]
Nepadutant DMPMF6L Infantile colics DD93.1 Phase 1/2 [14]
Saredutant DMSRJY3 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [15]
CS-003 DM1AEVT Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [16]
DNK-333 DM4ZO01 Irritable bowel syndrome DD91.0 Discontinued in Phase 2 [17]
AVE-5883 DM3P84V Asthma CA23 Discontinued in Phase 1/2 [18]
UK-224671 DMDTRJB Urinary incontinence MF50.2 Discontinued in Phase 1 [19]
SR 144190 DMK4XT8 Acute or chronic pain MG30-MG31 Discontinued in Phase 1 [20]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Substance-K receptor (TACR2) TTYO0A3 NK2R_HUMAN Modulator [2]
Substance-P receptor (TACR1) TTZPO1L NK1R_HUMAN Modulator [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: 2103).
2 Effects of FK224, a novel compound NK1 and NK2 receptor antagonist, on airway constriction and airway edema induced by neurokinins and sensory nerv... J Pharmacol Exp Ther. 1992 Jul;262(1):403-8.
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.
11 Antagonist profile of ibodutant at the tachykinin NK2 receptor in guinea pig isolated bronchi. Eur J Pharmacol. 2013 Nov 15;720(1-3):180-5.
12 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
13 Pharmacology of an original and selective nonpeptide antagonist ligand for the human tachykinin NK2 receptor. Eur J Pharmacol. 2005 Jun 1;516(2):104-11.
14 Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
15 Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochem Pharmacol. 2009 May 1;77(9):1522-30.
16 Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
17 Dual tachykinin NK1/NK2 antagonist DNK333 inhibits neurokinin A-induced bronchoconstriction in asthma patients. Eur Respir J. 2004 Jan;23(1):76-81.
18 Effect of an NK1/NK2 receptor antagonist on airway responses and inflammation to allergen in asthma. Am J Respir Crit Care Med. 2007 Mar 1;175(5):450-7.
19 Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica. 2000 Jun;30(6):627-42.
20 Pharmacologic evaluation of neurokinin-2 receptor antagonists in the guinea pig respiratory tract. Am J Vet Res. 2004 Jul;65(7):984-91.