pelitrexol

Pelitrexol is a water-soluble antifolate small molecule that acts as an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), the first folate-dependent enzyme in the de novo purine synthesis pathway. By inhibiting GARFT, pelitrexol reduces intracellular pools of purine nucleotides required for DNA replication and RNA transcription, leading to cell cycle arrest in S-phase and inhibition of tumor cell proliferation. This mechanism also results in reduced mTORC1 activity by impairing Rheb activation. Pelitrexol was developed as an antineoplastic agent and has been studied primarily for metastatic non-small cell lung cancer and colorectal cancer. Despite promising preclinical activity—including robust tumor growth suppression in NSCLC models—its clinical development was discontinued due to limited efficacy as a single agent[1][3][4][5][6][7].

Other names

446022-33-9DHT6E8M4KPDHT-6E8M4KPDHT 6E8M4KP