OSI-7904 explained

Legal Status:	Investigational
Iupac Name:	(2S)-2-[6-[(3-Methyl-1-oxo-2''H''-benzo[''f'']quinazolin-9-yl)methylamino]-3-oxo-1H-isoindol-2-yl]pentanedioic acid
Cas Number:	139987-54-5
Pubchem:	135403832
Unii:	ON177ZCE7M
C:	27
H:	24
N:	4
O:	6
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-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-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]}

Notes and References

1. Web site: NCI Drug Dictionary: OSI-7904L. National Cancer Institute.
2. Ricart AD, Berlin JD, Papadopoulos KP, etal . 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 . December 2008 . 19047127 . 10.1158/1078-0432.CCR-08-0864 . 14215154 . free .
3. Web site: 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 . 10.1007/s00280-007-0509-5 . 17520255. 61. 4. Cancer Chemotherapy and Pharmacology. 579–585. Clamp AR. 2008. 26018991 .