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

General Information of Drug (ID: DM1OSUR)

• Drug Name: CP-195543 Drug Info
• Synonyms: LB4 antagonist (RA), Pfizer; LB4 antagonist (inflammation), Pfizer; Leukotriene B4 antagonist (inflammation), Pfizer; Leukotriene B4 antagonist (rheumatoid arthritis), Pfizer

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 9823886
  CAS Number: CAS 204981-48-6
  TTD Drug ID: DM1OSUR

Molecule-Related Drug Atlas

Drug(s) Targeting Leukotriene B4 receptor 1 (LTB4R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LTB4	DME26RS	Human immunodeficiency virus infection	1C62	Phase 2	[3]
Amelubant	DMUMCB9	Pulmonary disease	1B10-1F85	Phase 2	[4]
Biomed 101	DMQ9KZW	Kidney cancer	2C90.0	Phase 1	[5]
LY293111	DM03FHA	Pancreatic cancer	2C10	Discontinued in Phase 2	[6]
SB-201993	DMIF4VJ	Psoriasis vulgaris	EA90	Discontinued in Phase 2	[7]
CI-949	DMN4QSW	Asthma	CA23	Discontinued in Phase 2	[8]
LTB 019	DM6G0PN	Asthma	CA23	Discontinued in Phase 2	[9]
LY-223982	DMWB7DO	Asthma	CA23	Discontinued in Phase 2	[10]
CP-105696	DM1C4IN	Inflammatory bowel disease	DD72	Discontinued in Phase 1	[11]
TAK-683	DMRD8HK	Prostate cancer	2C82.0	Discontinued in Phase 1	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene B4 receptor 1 (LTB4R)	TTN53ZF	LT4R1_HUMAN	Antagonist	[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: 6155).
• [2] The synthesis of CP-195543, an LTB4 antagonist for the treatment of inflammatory diseases. Curr Opin Drug Discov Devel. 1999 Nov;2(6):550-6.
• [3] LTB4 promotes insulin resistance in obese mice by acting on macrophages, hepatocytes and myocytes. Nat Med. 2015 Mar;21(3):239-47.
• [4] Leukotriene receptor antagonists in children with cystic fibrosis lung disease : anti-inflammatory and clinical effects. Paediatr Drugs. 2005;7(6):353-63.
• [5] Biomed 101, a leukotriene B4 inhibitor, may decrease IL-2 toxicity. 2003 ASCO Annual Meeting. 2003.
• [6] The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer. PPAR Res. 2008;2008:827096.
• [7] (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist w... J Med Chem. 1996 Sep 13;39(19):3837-41.
• [8] Inhibition of histamine, leukotriene C4/D4, and thromboxane B2 release from human leukocytes and human chopped lung mast cells by the allergic mediator release inhibitor, CI-949. J Allergy Clin Immunol. 1990 Dec;86(6 Pt 1):902-8.
• [9] Effect of the oral leukotriene B4 receptor antagonist LTB019 on inflammatory sputum markers in patients with chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2008;21(2):409-17.
• [10] Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14.
• [11] 3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor, Bioorg. Med. Chem. Lett. 7(17):2307-2312 (1997).
• [12] A second leukotriene B(4) receptor, BLT2. A new therapeutic target in inflammation and immunological disorders. J Exp Med. 2000 Aug 7;192(3):421-32.