Galidesivir (hydrochloride)

Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir hydrochloride inhibits some negative-sense RNA viruses with EC₅₀s ranging from ~3 to ~68 μM^[1][2][3]. IC50 & Target: RdRp inhibitor In Vitro: Cellular kinases phosphorylate Galidesivir (BCX4430) hydrochloride to a triphosphate that mimics ATP; viral RNA polymerases incorporate the drug's monophosphate nucleotide into the growing RNA chain, causing premature chain termination^[1].
Galidesivir hydrochloride effectively inhibits the infection of Vero cells with YFV. The EC₅₀ determined by the neutral red uptake assay is 8.3 μg/ml (24.5 μM)^[3]. In Vivo: Galidesivir (BCX4430) hydrochloride is active after intramuscular, intraperitoneal, and oral administration in a variety of experimental infections. In nonclinical studies involving lethal infections with Ebola virus, Marburg virus, Rift Valley fever virus, and Yellow Fever virus, Galidesivir hydrochloride has demonstrated pronounced efficacy^[1].
Galidesivir hydrochloride (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF)^[4].