General Information of Drug (ID: DM83JCK)

Drug Name
Iclepertin Drug Info
Synonyms
Iclepertin; 1421936-85-7; Iclepertin [INN]; UNII-M43ZDU10DD; M43ZDU10DD; Methanone, (5-(methylsulfonyl)-2-((1R)-2,2,2-trifluoro-1-methylethoxy)phenyl)((1R,5R)-1-(5-(trifluoromethyl)-3-isoxazolyl)-3-azabicyclo(3.1.0)hex-3-yl)-; BI-425809; Methanone, [5-(methylsulfonyl)-2-[(1R)-2,2,2-trifluoro-1-methylethoxy]phenyl][(1R,5R)-1-[5-(trifluoromethyl)-3-isoxazolyl]-3-azabicyclo[3.1.0]hex-3-yl]-; ICLEPERTIN [USAN]; SCHEMBL22621289; GTPL12110; MYHDQTVHHMSLEF-DDBGAENHSA-N; GLXC-25863; AKOS040755624; BI425809; MS-29509; BI 425809; HY-138935; CS-0173438; EN300-33036645; Z5066614506; (1R,5R)-3-(5-methanesulfonyl-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}benzoyl)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hexane; [5-(Methylsulfonyl)-2-[(1R)-2,2,2-trifluoro-1-methylethoxy]phenyl][(1R,5R)-1-[5-(trifluoromethyl)-3-isoxazolyl]-3-azabicyclo[3.1.0]hex-3-yl]methanone; [5-?(Methylsulfonyl)?-?2-?[(1R)?-?2,?2,?2-?trifluoro-?1-?methylethoxy]?phenyl]?[(1R,?5R)?-?1-?[5-?(trifluoromethyl)?-?3-?isoxazolyl]?-?3-?azabicyclo[3.1.0]?hex-?3-?yl]?-methanone; [5-methylsulfonyl-2-[(2R)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-[(1R,5R)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl]methanone
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Phase 3 [1]
Cross-matching ID
PubChem CID
155259577
TTD Drug ID
DM83JCK

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
R1678 DM4K9WH Schizophrenia 6A20 Phase 3 [3]
BI 425809 DMH3XDR Schizophrenia 6A20 Phase 3 [4]
AMG 747 DMWPGB8 Schizophrenia 6A20 Phase 2 [5]
ORG-25935 DMWN2EC Psychotic disorder 6A20-6A25 Phase 2 [6]
PF-3463275 DMO02LU Schizophrenia 6A20 Phase 2 [5]
GlyT1 PET radiotracers DMCKZUT Schizophrenia 6A20 Phase 1 [7]
ALX-5407 DMLJWPN Schizophrenia 6A20 Phase 1 [8]
JNJ-17305600 DMMI4XR Schizophrenia 6A20 Phase 1 [9]
DCCCyB DMQ8ACY Schizophrenia 6A20 Phase 1 [10]
MK-2637 DMUHOJP Schizophrenia 6A20 Phase 1 [11]
⏷ 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
Glycine transporter GlyT-1 (SLC6A9) TTHJTF7 SC6A9_HUMAN Inhibitor [2]

References

1 ClinicalTrials.gov (NCT05211947) An Open Label, Single Arm, Extension Trial to Examine Long-term Safety of Iclepertin Once Daily in Patients With Schizophrenia Who Have Completed Previous Iclepertin Phase III Trials (CONNEX-X). U.S.National Institutes of Health.
2 Effects of the Glycine Transporter-1 Inhibitor Iclepertin (BI 425809) on Sensory Processing, Neural Network Function, and Cognition in Animal Models Related to Schizophrenia. J Pharmacol Exp Ther. 2022 Aug;382(2):223-232.
3 Clinical pipeline report, company report or official report of Roche (2009).
4 Efficacy and safety of the novel glycine transporter inhibitor BI 425809 once daily in patients with schizophrenia: a double-blind, randomised, placebo-controlled phase 2 study. Lancet Psychiatry. 2021 Mar;8(3):191-201.
5 Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain. Nat Rev Drug Discov. 2013 Nov;12(11):866-85.
6 The selective glycine uptake inhibitor org 25935 as an adjunctive treatment to atypical antipsychotics in predominant persistent negative symptoms of schizophrenia: results from the GIANT trial. J Clin Psychopharmacol. 2014 Apr;34(2):190-8.
7 Glycine Transport Inhibitors for the Treatment of Schizophrenia. Open Med Chem J. 2010; 4: 10-19.
8 ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Mol Pharmacol. 2001 Dec;60(6):1414-20.
9 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: 935).
10 Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1. ACS Med Chem Lett. 2010 October 14; 1(7): 350-354.
11 Characterization of the novel GlyT1 PET tracer [18F]MK-6577 in humans. Synapse. 2015 Jan;69(1):33-40.