Title: Oblimersen Sodium
CAS Registry Number: 190977-41-4
CAS Name: d(P-thio)(T-C-T-C-C-C-A-G-C-G-T-G-C-G-C-C-A-T)DNA
Additional Names: augmerosen
Manufacturers' Codes: G-3139
Trademarks: Genasense (Genta)
Literature References: Synthetic 18 base phosphorothioate antisense oligonucleotide (AS ON); designed to bind to human bcl-2 oncogene, resulting in the down-regulation of an apoptosis-inhibiting protein Bcl-2. Prepn: J. C. Reed, WO 9508350 (1995); idem, US 5831066 (1998 to Univ. of Penn.). LC/MS determn in plasma and urine: G. Dai et al., J. Chromatogr. B 825, 201 (2005). Pharmacokinetics: F. I. Raynaud et al., J. Pharmacol. Exp. Ther. 281, 420 (1997). Mechanism of action study: L. Benimetskaya et al., Oligonucleotides 15, 206 (2005). Clinical evaluations in malignant melanoma: B. Jansen et al., Lancet 356, 1728 (2000); in non-Hodgkin's lymphoma: J. S. Waters et al., J. Clin. Oncol. 18, 1812 (2000); in prostate cancer: K. N. Chi et al., Clin. Cancer Res. 7, 3920 (2001). Review of pharmacology, preclinical and clinical development: R. J. Klasa et al., Antisense Nucleic Acid Drug Dev. 12, 193-213 (2002). Review of therapeutic potential in lung cancer: R. S. Herbst, S. R. Frankel, Clin. Cancer Res. 10, 4245s-4248s (2004); in prostate cancer: K. N. Chi, World J. Urol. 23, 33-37 (2005).
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Oligonucleotides. |