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

General Information of Drug (ID: DMUX8JZ)

• Drug Name: Nivocasan Drug Info
• Synonyms: GS-9450; LB-84451

Indication

Disease Entry	ICD 11	Status	REF
Fibrosis	GA14-GC01	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11633038
  CAS Number: CAS 908253-63-4
  TTD Drug ID: DMUX8JZ

Molecule-Related Drug Atlas

Drug(s) Targeting Caspase-1 (CASP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AC-201	DMB0TNL	Type-2 diabetes	5A11	Phase 2	[2]
Belnacasan	DM2Q50G	Epilepsy	8A60-8A68	Phase 2	[3]
PRALNACASAN	DM73UTG	Rheumatoid arthritis	FA20	Phase 2	[4]
Ac-YVAD-FMK	DM7K256	Allergic contact dermatitis	EK00	Patented	[5]
Ac-YVAD-cmk	DMA1RVN	Allergic contact dermatitis	EK00	Patented	[5]
VE-16084	DMHG70W	Rheumatoid arthritis	FA20	Terminated	[6]
L-709049	DMQZW6D	N. A.	N. A.	Terminated	[7]
SDZ-224-015	DMY1KE8	Rheumatoid arthritis	FA20	Terminated	[8]
M826	DM9NPE4	Discovery agent	N.A.	Investigative	[9]
YVAD	DM24LNB	Discovery agent	N.A.	Investigative	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Caspase-1 (CASP1)	TTCQIBE	CASP1_HUMAN	Modulator	[1]

References

• [1] Combined effects of an antioxidant and caspase inhibitor on the reversal of hepatic fibrosis in rats. Apoptosis. 2013 Dec;18(12):1481-91.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] (S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydr... J Pharmacol Exp Ther. 2007 May;321(2):509-16.
• [4] Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis. Osteoarthritis Cartilage. 2003 Oct;11(10):738-46.
• [5] Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59.
• [6] Interleukin-1 beta converting enzyme inhibition blocks progression of type II collagen-induced arthritis in mice. Cytokine. 1996 May;8(5):377-86.
• [7] Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). Bioorg Med Chem Lett. 2010 Sep 1;20(17):5184-90.
• [8] Reduction of inflammation and pyrexia in the rat by oral administration of SDZ 224-015, an inhibitor of the interleukin-1 beta converting enzyme. Br J Pharmacol. 1995 Jun;115(4):601-6.
• [9] Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80.
• [10] Mice deficient in interleukin-1beta converting enzyme resist anorexia induced by central lipopolysaccharide. Am J Physiol. 1999 Nov;277(5 Pt 2):R1435-43.