MIV-150 is a tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC50s = 1 nM in vitro).1 It has been shown to inactivate viruses that are resistant to other antiviral drugs, including non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, and protease inhibitors.1 Although MIV-150 possesses poor oral bioavailability, it demonstrates efficacy when formulated as a topical microbicide.2,3
1.Fernández-Romero, J.A., Thorn, M., Turville, S.G., et al.Carrageenan/MIV-150 (PC-815), a combination microbicideSex. Transm. Dis.34(1)9-14(2007) 2.Turville, S.G., Aravantinou, M., Miller, T., et al.Efficacy of Carraguardr-based microbicides in vivo despite variable in vitro activityPLoS One3(9)e3162(2008) 3.Singer, R., Derby, N., Rodriguez, A., et al.The nonnucleoside reverse transcriptase inhibitor MIV-150 in carrageenan gel prevents rectal transmission of simian/human immunodeficiency virus infection in macaquesJ. Virol.85(11)5504-5512(2011)