Galidesivir  (Synonyms: BCX4430; Immucillin-A)

Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir 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 inhibits some negative-sense RNA viruses with EC₅₀s ranging from ~3 to ~68 μM^[1][2][3].

RdRp

Cellular kinases phosphorylate Galidesivir (BCX4430) 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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Galidesivir (BCX4430) 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 has demonstrated pronounced efficacy^[1].
Galidesivir (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF)^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

265.27

Solid

C₁₁H₁₅N₅O₃

249503-25-1

O[[email protected]]1[[email protected]](C2=CNC3=C2N=CN=C3N)N[[email protected]](CO)[[email protected]]1O

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• [1]. Taylor R, et al. BCX4430 - A broad-spectrum antiviral adenosine nucleoside analog under development for the treatment of Ebola virus disease. J Infect Public Health. 2016;9(3):220-226.  [Content Brief]

  [2]. Elfiky AA, et al. ICN-1229, Remdesivir, PSI-7977, Galidesivir, and GS 1278 against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study. Life Sci. 2020 Mar 25:117592.  [Content Brief]

  [3]. Warren TK, et al. Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430. Nature. 2014;508(7496):402-405.  [Content Brief]

  [4]. Julander JG, et al. BCX4430, a novel nucleoside analog, effectively treats yellow fever in a Hamster model. Antimicrob Agents Chemother. 2014;58(11):6607-6614.  [Content Brief]