Nolatrexed dihydrochloride (AG 337) is an orally active, non-competitive, lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. It interacts at the folate cofactor binding site of the enzyme, increases sulfotransferases, and induces cell cycle arrest in the S phase of cancer cells. It also exhibits anticancer activity against cervical cancer.
- Orally active and non-competitive lipophilic inhibitor of thymidylate synthase.
- Interacts at the folate cofactor binding site of the enzyme.
- Increases sulfotransferases.
- Induces cell cycle arrest in S phase of cancer cells.
- Exhibits anticancer activity against cervical cancer.