OSI-7904

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]

OSI-7904
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • (2S)-2-[6-[(3-Methyl-1-oxo-2H-benzo[f]quinazolin-9-yl)methylamino]-3-oxo-1H-isoindol-2-yl]pentanedioic acid
CAS Number
PubChem CID
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H24N4O6
Molar mass500.511 g·mol−1
3D model (JSmol)
SMILES
  • CC1=NC2=C(C3=C(C=CC(=C3)CNC4=CC5=C(C=C4)C(=O)N(C5)[C@@H](CCC(=O)O)C(=O)O)C=C2)C(=O)N1

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
  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" (PDF). Clin. Cancer Res. 14 (23): 7947–55. doi:10.1158/1078-0432.CCR-08-0864. PMID 19047127. S2CID 14215154.
  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. 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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