Drug intelligence / Profile preview

TRC102 + pemetrexed

Development stage
Phase 1
Lead developer
TRACON Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

TRC102 (methoxyamine) is a small-molecule inhibitor of base excision repair (BER) that potentiates the cytotoxicity of DNA-damaging chemotherapies, such as pemetrexed, by binding to chemotherapy-induced abasic sites in DNA and preventing their repair. This leads to accumulation of DNA damage and increased cancer cell death. Pemetrexed is an antifolate antineoplastic agent that inhibits enzymes involved in folate metabolism and DNA synthesis, thereby blocking cancer cell proliferation. The combination has been studied primarily for advanced solid tumors, including non-small cell lung cancer (NSCLC), malignant mesothelioma, and salivary gland tumors. Clinical trials have shown that the combination can be administered safely with evidence of antitumor activity[1][2][3].

Other names
pemetrexed disodium
02

Targets

AP site (Apurinic/apyrimidinic site)DHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)

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