Lexipafant

Lexipafant
Identifiers
	IUPAC name ethyl (2S)-4-methyl-2-[methyl-[4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]phenyl]sulfonylamino]pentanoate;
CAS Number	139133-26-9;
PubChem CID	9804204;
ChemSpider	7979964;
UNII	H14917M9YW;
ChEMBL	ChEMBL322832;
Chemical and physical data
Formula	C23H30N4O4S
Molar mass	458.58 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCOC(=O)C(CC(C)C)N(C)S(=O)(=O)C1=CC=C(C=C1)CN2C(=NC3=C2C=CN=C3)C;
	InChI InChI=1S/C23H30N4O4S/c1-6-31-23(28)22(13-16(2)3)26(5)32(29,30)19-9-7-18(8-10-19)15-27-17(4)25-20-14-24-12-11-21(20)27/h7-12,14,16,22H,6,13,15H2,1-5H3/t22-/m0/s1; Key:AQRXDPFOYJSPMP-QFIPXVFZSA-N;

Lexipafant (BB-882, Zacutex) is a drug which acts as a potent and selective inhibitor of the phospholipid mediator platelet-activating factor (PAF). It was developed in the 1990s by British Biotech with several potential applications, including HIV-associated neurocognitive disorder and acute pancreatitis. Initial results were encouraging and it progressed as far as Phase III clinical trials, but final analysis of trial results showed that it failed to improve survival rates in pancreatitis despite some symptomatic improvement, and it was ultimately discontinued from development as a medicine, though it continues to be used as a model PAF inhibitor for pharmacology research.[1][2][3][4]

References

Kingsnorth AN (1996). "Platelet-activating factor". Scandinavian Journal of Gastroenterology. Supplement. 219: 28–31. doi:10.3109/00365529609104996. PMID 8865468.
McKay C, Curran FJ, Sharples CE, Young CA, Baxter JN, Imrie CW (1996). "The Use of Lexipafant in the Treatment of Acute Pancreatitis". Platelet-Activating Factor and Related Lipid Mediators 2. Advances in Experimental Medicine and Biology. Vol. 416. pp. 365–370. doi:10.1007/978-1-4899-0179-8_59. ISBN 978-1-4899-0181-1. PMID 9131175.
Johnson CD, Kingsnorth AN, Imrie CW, McMahon MJ, Neoptolemos JP, McKay C, et al. (January 2001). "Double blind, randomised, placebo controlled study of a platelet activating factor antagonist, lexipafant, in the treatment and prevention of organ failure in predicted severe acute pancreatitis". Gut. 48 (1): 62–69. doi:10.1136/gut.48.1.62. PMC 1728186. PMID 11115824.
Abu-Zidan FM, Windsor JA (2002). "Lexipafant and acute pancreatitis: a critical appraisal of the clinical trials". The European Journal of Surgery = Acta Chirurgica. 168 (4): 215–219. doi:10.1080/11024150260102816. PMID 12440758.

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[1] Kingsnorth AN (1996). "Platelet-activating factor". Scandinavian Journal of Gastroenterology. Supplement. 219: 28–31. doi:10.3109/00365529609104996. PMID 8865468.

[2] McKay C, Curran FJ, Sharples CE, Young CA, Baxter JN, Imrie CW (1996). "The Use of Lexipafant in the Treatment of Acute Pancreatitis". Platelet-Activating Factor and Related Lipid Mediators 2. Advances in Experimental Medicine and Biology. Vol. 416. pp. 365–370. doi:10.1007/978-1-4899-0179-8_59. ISBN 978-1-4899-0181-1. PMID 9131175.

[3] Johnson CD, Kingsnorth AN, Imrie CW, McMahon MJ, Neoptolemos JP, McKay C, et al. (January 2001). "Double blind, randomised, placebo controlled study of a platelet activating factor antagonist, lexipafant, in the treatment and prevention of organ failure in predicted severe acute pancreatitis". Gut. 48 (1): 62–69. doi:10.1136/gut.48.1.62. PMC 1728186. PMID 11115824.

[4] Abu-Zidan FM, Windsor JA (2002). "Lexipafant and acute pancreatitis: a critical appraisal of the clinical trials". The European Journal of Surgery = Acta Chirurgica. 168 (4): 215–219. doi:10.1080/11024150260102816. PMID 12440758.