OSI-7904L

OSI-7904L is a novel 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]

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 tumours is currently under evaluation.[2][3][4]

References

  1. ↑ 1.0 1.1 "NCI Drug Dictionary: OSI-7904L". National Cancer Institute.
  2. ↑ 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". Clin. Cancer Res. 14 (23): 7947–55. doi:10.1158/1078-0432.CCR-08-0864. PMID 19047127.
  3. ↑ "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)".
  4. ↑ "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".