Nifurtimox-d4 is intended for use as an internal standard for the quantification of nifurtimox by GC- or LC-MS. Nifurtimox is an antiprotozoal agent.1 It is active against TaluahuÉn, LQ, and Brener strains of T. cruzi epimastigotes (IC50s = 9.91, 12.28, and 10.44 μM, respectively). Nifurtimox interferes with cellular oxygen metabolism and induces parasitic cell death through the production of highly toxic oxygen reactive metabolites, including superoxide anions, hydroxyl radicals, and hydrogen peroxide. It also inhibits clonogenic growth of HCT116, H838, C33A, LN18, KNS42, MDA-MB-231, and FaDu human cancer cells under hypoxic conditions.2 Formulations containing nifurtimox have been used in the treatment of Chaga's disease.3
|1. Maya, J.D., Bollo, S., Nu•ez-Vergara, L.J., et al. Trypanosoma cruzi: Effect and mode of action of nitroimidazole and nitrofuran derivatives. Biochem. Pharmacol. 65(6), 999-1006 (2003).|2. Li, Q., Lin, Q., Kim, H., et al. The anti-protozoan drug nifurtimox preferentially inhibits clonogenic tumor cells under hypoxic conditions. Am. J. Cancer Res. 7(5), 1084-1095 (2017).|3. Pinazo, M.-J., Guerrero, L., Posada, E., et al. Benznidazole-related adverse drug reactions and their relationship to serum drug concentrations in patients with chronic chagas disease. Antimicrob. Agents Chemother. 57(1), 390-395 (2013).