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10-Propargyl-5,8-dideazafolic acid
- Development stage
- Preclinical
- Lead developer
- The Institute of Cancer Research
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
10-Propargyl-5,8-dideazafolic acid (CB3717) is a small molecule antifolate compound that acts as a potent inhibitor of thymidylate synthase. By inhibiting this enzyme, it disrupts the synthesis of thymidine monophosphate (dTMP), an essential precursor for DNA biosynthesis. This mechanism targets folate-dependent biological pathways and has been investigated primarily in the context of cancer therapy due to its ability to inhibit cell proliferation. The drug is considered experimental and has been studied for its effects on leukemia cell lines resistant to other antifolates such as methotrexate and trimetrexate[2][4][5][6][7].
- Other names
- 10-propargyl-5,8-dideazafolic acidN10-propargyl-5,8-dideazafolic acid
02
Targets
TS (Thymidylate synthase)
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