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.
体外研究
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.
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).
体内研究
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.
Galidesivir hydrochloride (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF).
Animal Model:
Female Syrian golden hamsters (hamsters infected with YF virus)
Dosage:
4 mg/kg of body weight
Administration:
I.p.; twice daily for 7 days
Result:
Significantly improved the survival of hamsters infected with YFV.
分子式
C11H15N5O3.HCl
分子量
301.73
CAS号
222631-44-9
中文名称
加利司韦盐酸盐;加利地韦盐酸盐
运输条件
Room temperature in continental US; may vary elsewhere.