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

General Information of Drug (ID: DM2IJWG)

• Drug Name: GFB-887 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Diabetic nephropathy	GB61.Z	Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DM2IJWG

Molecule-Related Drug Atlas

Drug(s) Targeting Short transient receptor potential channel 5 (TRPC5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BI 1358894	DM740BS	Depression	6A70-6A7Z	Phase 2	[3]
2-APB	DM9AKVR	Discovery agent	N.A.	Investigative	[4]
daidzein	DMRFTJX	Discovery agent	N.A.	Investigative	[5]
lysophosphatidylcholine	DMOGFVH	Discovery agent	N.A.	Investigative	[5]
KB-R7943	DMMD5W3	Discovery agent	N.A.	Investigative	[6]
BTP2	DMNM63G	Discovery agent	N.A.	Investigative	[5]
bromoenol lactone	DMKQ0CA	Discovery agent	N.A.	Investigative	[7]
ML204	DM15YL0	Discovery agent	N.A.	Investigative	[8]
(-)-englerin A	DMPQBWY	Discovery agent	N.A.	Investigative	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Short transient receptor potential channel 5 (TRPC5)	TT32NQ1	TRPC5_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT04387448) A Phase 2a Multiple Ascending, Placebo-Controlled Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of GFB-887, a TRPC5 Channel Inhibitor, in Patients With Diabetic Nephropathy, Focal Segmental Glomerulosclerosis, and Treatment-Resistant Minimal Change Disease. U.S.National Institutes of Health.
• [2] Safety and Efficacy of GFB-887, a TRPC5 Channel Inhibitor, in Patients With Focal Segmental Glomerulosclerosis, Treatment-Resistant Minimal Change Disease, or Diabetic Nephropathy: TRACTION-2 Trial Design. Kidney Int Rep. 2021 Jul 23;6(10):2575-2584.
• [3] Clinical pipeline report, company report or official report of Boehringer Ingelheim.
• [4] Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol. 2005 Jun;145(4):405-14.
• [5] 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: 490).
• [6] The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels. Biochem Biophys Res Commun. 2007 Sep 14;361(1):230-6.
• [7] Bromoenol lactone inhibits voltage-gated Ca2+ and transient receptor potential canonical channels. J Pharmacol Exp Ther. 2011 Nov;339(2):329-40.
• [8] Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46.
• [9] (-)-Englerin is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.