Thymidylate synthase inhibitor

Thymidylate synthase inhibitors are chemical agents which inhibit the enzyme thymidylate synthase and have potential as an anticancer chemotherapy.^[1] Five agents were in clinical trials in 2002: raltitrexed, pemetrexed, nolatrexed, ZD9331, and GS7904L.^[2]

Examples include

• Raltitrexed, used for colorectal cancer since 1998
• Fluorouracil, used for colorectal cancer^[3]
• BGC 945^[4]
• OSI-7904L^[5]

References

1. Jackman, A.L.; Calvert, A.H. (1995). "Folate-based thymidylate synthase inhibitors as anticancer drugs". Annals of Oncology. 6 (9): 871–881. PMID 8624289.
2. "Thymidylate synthase inhibitors as anticancer agents: from bench to bedside". Retrieved 2009-01-28.
3. Papamichael, D. (1999). "The use of thymidylate synthase inhibitors in the treatment of advanced colorectal cancer: current status". Oncologist. 4 (6): 478–87. PMID 10631692.
4. Gibbs, David D.; et al. (2005). "BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to α-folate receptor-overexpressing tumors". Cancer Research. 65 (24): 11721–11728. doi:10.1158/0008-5472.CAN-05-2034.
5. 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.