nolatrexed

Nolatrexed is a water-soluble, lipophilic quinazoline folate analog and a non-competitive inhibitor of thymidylate synthase. By occupying the folate binding site of thymidylate synthase, it inhibits the enzyme's activity and blocks thymine nucleotide synthesis. This leads to inhibition of DNA replication, DNA damage, S-phase cell cycle arrest, and caspase-dependent apoptosis in tumor cells[1][3][4]. Nolatrexed was developed as an antineoplastic agent for various solid tumors including liver cancer (hepatocellular carcinoma), head and neck cancer, colorectal cancer, lung cancer, pancreatic cancer, and prostate cancer[5]. It is orally active and not susceptible to certain resistance mechanisms that affect classical antifolate drugs due to its lipophilicity and lack of a glutamate moiety[8].

Brand names

ThymitaqOrataq

Other names

nolatrexed dihydrochloride