Alicaforsen

Title: Alicaforsen
CAS Registry Number: 185229-68-9
CAS Name: d[(R)-P-Thio](G-C-C-C-A-A-G-C-T-G-G-C-A-T-C-C-G-T-C-A)deoxyribonucleic acid
Literature References: Synthetic 20 base phosphorothioate antisense oligonucleotide designed to inhibit expression of intercellular adhesion molecule-1 (ICAM-1), a key mediator of inflammation. Prepn: C. F. Bennett, C. K. Mirabelli, WO 9405333; eidem, US 5514788 (1994, 1996 both to Isis). Purifn and scale up: R. R. Deshmukh et al., Nucleosides Nucleotides Nucleic Acids 20, 567 (2001). ICAM-1 inhibition in cell culture: C. F. Bennett et al., J. Immunol. 152, 3530 (1994). Clinical pharmacokinetics: J. M. Glover et al., J. Pharmacol. Exp. Ther. 282, 1173 (1997). ELISA determn in plasma: R. Z. Yu et al., Anal. Biochem. 304, 19 (2002). Clinical evaluation in Crohn's disease: B. R. Yacyshyn et al., Gut 51, 30 (2002); in ulcerative colitis: S. J. H. van Deventer et al., ibid. 53, 1646 (2004). Review of toxicology: S. P. Henry et al., Toxicol. Pathol. 27, 95-100 (1999); A. A. Levin, Biochim. Biophys. Acta 1489, 69-84 (1999); of pharmacology and clinical development: W. R. Shanahan, Jr., Expert Opin. Invest. Drugs 8, 1417-1429 (1999); C. F. Barish, Expert Opin. Biol. Ther. 5, 1387-1391 (2005).
Derivative Type: Sodium salt
CAS Registry Number: 331257-52-4
Manufacturers' Codes: ISIS-2302
Therap-Cat: Anti-inflammatory.
Keywords: Anti-inflammatory (Biological Response Modifier); Anti-inflammatory (Gastrointestinal).
Alinidine Aliskiren Alitretinoin Alizapride Alizarin

Alicaforsen is an inflammatory bowel disease drug candidate. It is an antisense therapeutic that targets the messenger RNA for the production of human ICAM-1 protein. It is being progressed through clinical development as a nightly enema.