SAMT-247

SAMT-247 is a microbicide that selectively inactivate the viral nucleocapsid protein NCp7, causing zinc ejection and preventing RNA encapsidation. SAMT-247 shows good antiviral activity.

SAMT-247 covalently modifies the Gag polyprotein^[2].
SAMT-247 shows antiviral activity with an EC₅₀ of 0.6 μM in CEM-SS cells infected with HIV-1_IIIB. SAMT-247 shows low cellular toxicity (TC₅₀ > 100 μM)^[2].

A 1% gel formulation of SAMT-247 protected five of six rhesus macaques from vaginal challenge with a CCR5 (R5) -tropic SHIV^[3].

References:
[1]. Helmold Hait S, et al. An SAMT-247 Microbicide Provides Potent Protection against Intravaginal Simian Immunodeficiency Virus Infection of Rhesus Macaques, whereas an Added Vaccine Component Elicits Mixed Outcomes. J Immunol. 2020 Jun 15;204(12):3315-3328.
[2]. Miller Jenkins LM, et al. Small-molecule inactivation of HIV-1 NCp7 by repetitive intracellular acyl transfer. Nat Chem Biol. 2010 Dec;6(12):887-9.
[3]. Cheng-Mayer C, et al. Delay of simian human immunodeficiency virus infection and control of viral replication in vaccinated macaques challenged in the presence of a topical microbicide. AIDS. 2011 Sep 24;25(15):1833-41.