OSI-7904L is a novel noncompetitive liposomal thymidylate synthase inhibitor. OSI-7904 is a benzoquinazoline folate analogue 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. OSI-7904L is a liposome-encapsulated formulation of OSI-7904. Liposome encapsulation improves the efficacy and increases the half-life of OSI-7904. Its effect on solid tumours is currently under evaluation. References: Ricart AD, Berlin JD, Papadopoulos KP, Syed S, Drolet DW, Quaratino-Baker C, Horan J, Chick J, Vermeulen W, Tolcher AW, Rowinsky EK, Rothenberg ML. Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors. Clin Cancer Res. 2008 Dec 1;14(23):7947-55. PubMed PMID: 19047127.

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