Suramin is a polysulfonated naphthylurea with antiviral, antiparasitic, and anticancer activities.1 It is negatively charged at physiological pH and therefore binds to various intracellular targets including, but not limited to, ryanodine receptor 1 (IC50 = 4.9 ?M), G protein-coupled receptors, P2 purinergic receptors, PDGF, PKC, transferrin, DNA and RNA polymerases, sirtuins, and various cytokines.1,2,3 It reduces Zika virus infectivity in Vero cells (IC50 = ~2.5-5 ?g/ml).4 In vivo, suramin induces cell cycle arrest at the G2/M phase and apoptosis in L. donovani promastigotes in vitro and reduces hepatic parasitic burden in a mouse model of L. donovani-induced visceral leishmaniasis.5 Suramin (60 mg/kg) reduces tumor volume in patient-derived xenograft (PDX) mouse models of malignant mesothelioma.6 Formulations containing suramin have been used in the treatment of African sleeping sickness.
1.Wiedemar, N., Hauser, D.A., and M?ser, P.100 years of suraminAntimicrob. Agents Chemother.64(3)e01168-01119(2020) 2.Klinger, M., Bofill-Cardona, E., Mayer, B., et al.Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sitesBiochem. J.355(3)827-833(2001) 3.Charlton, S.J., Brown, C.A., Weisman, G.A., et al.PPADS and suramin as antagonists at cloned P2Y- and P2U- purinoceptorsBr. J. Pharmacol.118(3)704-710(1996) 4.Tan, C.W., Sam, I.-C., Chong, W.L., et al.Polysulfonate suramin inhibits Zika virus infectionAntiviral Res.143186-194(2017) 5.Khanra, S., Juin, S.K., Jawed, J.J., et al.In vivo experiments demonstrate the potent antileishmanial efficacy of repurposed suramin in visceral leishmaniasisPLoS Negl. Trop. Dis.14(8)e0008575(2020) 6.Chahinian, A.P., Mandeli, J.P., Gluck, H., et al.Effectiveness of cisplatin, paclitaxel, and suramin against human malignant mesothelioma xenografts in athymic nude miceJ. Surg. Oncol.67(2)104-111(1998)