OSI-7904 is a noncompetitive liposomal thymidylate synthase inhibitor. OSI-7904 is a benzoquinazoline folate analog with antineoplastic activity. As a thymidylate synthase inhibitor, OSI-7904 noncompetitively binds to thymidylate synthase, resulting in inhibition of thymine nucleotide synthesis and DNA replication.[1]
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| Formula | C27H24N4O6 |
| Molar mass | 500.511 g·mol−1 |
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OSI-7904L is a liposome-encapsulated formulation of OSI-7904. Liposome encapsulation improves the efficacy and increases the half-life of OSI-7904.[1]
Its effect on solid tumors is currently under evaluation.[2][3][4]
References
edit- ^ a b "NCI Drug Dictionary: OSI-7904L". National Cancer Institute.
- ^ Ricart AD, Berlin JD, Papadopoulos KP, et al. (December 2008). "Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors" (PDF). Clin. Cancer Res. 14 (23): 7947–55. doi:10.1158/1078-0432.CCR-08-0864. PMID 19047127. S2CID 14215154.
- ^ "Phase I study of liposomal thymidylate synthase inhibitor (TSI) OSI-7904L in patients with advanced solid tumors. Proc Am Soc Clin Oncol 22: 2003 (abstr 561)".
- ^ Clamp AR (2008). "A phase I and pharmacokinetic study of OSI-7904L, a liposomal thymidylate synthase inhibitor in combination with oxaliplatin in patients with advanced colorectal cancer. Cancer Chemotherapy and Pharmacology April 2008, Volume 61, Issue 4, pp 579-585". Cancer Chemotherapy and Pharmacology. 61 (4): 579–585. doi:10.1007/s00280-007-0509-5. PMID 17520255. S2CID 26018991.
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