Trovirdine

Trovirdine (LY300046) is a selective non-nucleoside HIV-1 reverse transcriptase inhibitor, with an IC₅₀ value of 0.012 μM against the wild-type enzyme. Trovirdine inhibits the replication of both wild-type and mutant HIV-1, and exerts synergistic or additive effects when combined with some antiviral drugs. Trovirdine is applicable to research related to HIV-1 infection^[1]. In Vitro:Trovirdine potently inhibits the activity of wild-type HIV-1 reverse transcriptase with an IC₅₀ of 0.012 μM; it also inhibits the replication of wild-type HIV-1 in MT-4 cells with an IC₅₀ of 0.013 μM^[1].
Trovirdine exhibits IC₅₀ values of 0.34 μM and 0.33 μM against HIV‑1 RT Tyr181→Cys and HIV‑1 RT Leu100→Ile mutants with 28‑fold and 27‑fold resistance respectively. In MT‑4 cells, Trovirdine shows IC₅₀ values of 3.90 μM, 24.5 μM and 1.90 μM for HIV‑1 Ile100, Asn103 and Cys181 mutant strains, with resistance factors >300‑fold, >1×10³‑fold and >140‑fold correspondingly^[1].

Trovirdine inhibits the activity of wild-type HIV‑1 reverse transcriptase (measured by the dCTP incorporation assay) with an IC₅₀ of 0.03 μM; it also inhibits the activities of the HIV‑1 RT Tyr181→Cys mutant and HIV‑1 RT Leu100→Ile mutant, with corresponding IC₅₀ values of 0.53 μM and 0.34 μM, respectively^[1].

Trovirdine (6 days) inhibits the replication of wild-type HIV-1 as well as HIV-1 Ile100, Asn103, and Cys181 mutants in MT-4 cells in the context of combination testing with ddI, with corresponding IC₅₀ values of 0.019 μM, 4.0 μM, 13.7 μM, and 0.87 μM^[1].