Benznidazole is an orally bioavailable antiprotozoal agent.1 It is a 2-nitroimidazole prodrug that becomes active when the nitro group is reduced within the parasite.2 It inhibits the growth of the parasites T. cruzi, T. vaginalis, G. lamblia, and E. histolytica (IC50s = 8.1, 18.62, 22.58, and 4.27 μM, respectively).3,4 It also inhibits clonogenic growth of human C33A cervical and KNS42 glioblastoma cancer cells under hypoxic, but not normoxic, conditions when used at a concentration of 100 μM.5 Benznidazole (100 mg/kg per day) decreases T. cruzi blood parasitemia to below detectable levels in a mouse model of chronic stable Chagas disease.1 Formulations containing benznidazole have been used in the treatment of Chagas disease caused by T. cruzi.
1.Khare, S., Liu, W., Stinson, M., et al.Antitrypanosomal teatment with benznidazole is superior to posaconazole regimens in mouse models of Chagas diseaseAntimicrob. Agents Chemother.59(10)6385-6394(2015) 2.Trochine, A., Creek, D.J., Faral-Tello, P., et al.Benznidazole biotransformation and multiple targets in Trypanosoma cruzi revealed by metabolomicsPLoS Negl. Trop. Dis.8(5)e2844(2014) 3.Cogo, J., de Oliveira Caleare, A., Ueda-Nakamura, T., et al.Trypanocidal activity of guaianolide obtained from Tanacetum parthenium (L.) Schultz-Bip. and its combinational effect with benznidazolePhytomedicine20(1)59-66(2012) 4.Hernández-Nú?ez, E., Tlahuext, H., Moo-Puc, R., et al.Design, synthesis and biological evaluation of 2-(2-amino-5(6)-nitro-1H-benzimidazol-1-yl)-N-arylacetamides as antiprotozoal agentsMolecules22(4)E579(2017) 5.Li, Q., Lin, Q., and Yun, Z.Hypoxia-activated cytotoxicity of benznidazole against clonogenic tumor cellsCancer Biol. Ther.17(12)1266-1273(2016)