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

General Information of Drug (ID: DMH3XDR)

• Drug Name: BI 425809 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Schizophrenia	6A20	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 155259577
  TTD Drug ID: DMH3XDR

Molecule-Related Drug Atlas

Drug(s) Targeting Glycine transporter GlyT-1 (SLC6A9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
R1678	DM4K9WH	Schizophrenia	6A20	Phase 3	[3]
Iclepertin	DM83JCK	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]

Molecular Interaction Atlas of This Drug

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 (NCT04846868) Clinical Trial of BI 425809 Effect on Cognition and Functional Capacity in Schizophrenia (CONNEX-1). U.S. National Institutes of Health.
• [2] 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.
• [3] Clinical pipeline report, company report or official report of Roche (2009).
• [4] 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.
• [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.