Galidesivir

Galidesivir
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name (2S,3S,4R,5R)-2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3,4-diol;
CAS Number	222631-44-9 ;
PubChem CID	69211190;
ChemSpider	8620968;
UNII	OLF97F86A7;
Chemical and physical data
Formula	C11H15N5O3
Molar mass	265.268 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O[C@H]3[C@H](c2c1ncnc(N)c1[nH]c2)N[C@H](CO)[C@H]3O;
	InChI InChI=1S/C11H15N5O3/c12-11-8-6(14-3-15-11)4(1-13-8)7-10(19)9(18)5(2-17)16-7/h1,3,5,7,9-10,13,16-19H,2H2,(H2,12,14,15)/t5-,7+,9-,10+/m1/s1; Key:AMFDITJFBUXZQN-KUBHLMPHSA-N;

Galidesivir (BCX4430, Immucillin-A) is an antiviral drug, an adenosine analog^[1] (a type of nucleoside analog).^[2] It is developed by BioCryst Pharmaceuticals with funding from NIAID, originally intended as a treatment for hepatitis C, but subsequently developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease.

It also shows broad-spectrum antiviral effectiveness against a range of other RNA virus families, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses, flaviviruses and phleboviruses.^[3] BCX4430 has been demonstrated to protect against both Ebola and Marburg viruses in both rodents and monkeys, even when administered up to 48 hours after infection,^[1] and development for use in humans was then being fast-tracked due to concerns about the lack of treatment options for the 2013-2016 Ebola virus epidemic in West Africa.^[4]

BCX4430 later showed efficacy against Zika virus in a mouse model.^[5]

Galidesivir is one of several antiviral drugs being tested for coronavirus disease 2019.^[6]

On April 9th, BioCryst opened enrollment into a randomized, double-blind, placebo-controlled clinical trial to assess the safety, clinical impact and antiviral effects of galidesivir in patients with COVID-19. The trial (NCT03891420) is being funded by the National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health. https://clinicaltrials.gov/ct2/show/NCT03891420

References

^ ^a ^b Warren TK, Wells J, Panchal RG, Stuthman KS, Garza NL, Van Tongeren SA, et al. (April 2014). "Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430" (PDF). Nature. 508 (7496): 402–5. Bibcode:2014Natur.508..402W. doi:10.1038/nature13027. PMID 24590073.
^ Kamat SS, Burgos ES, Raushel FM (October 2013). "Potent inhibition of the C-P lyase nucleosidase PhnI by Immucillin-A triphosphate". Biochemistry. 52 (42): 7366–8. doi:10.1021/bi4013287. PMC 3838859. PMID 24111876.
^ Westover JB, et al. Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters. Antiviral Res. 2018 Aug;156:38-45. Westover, J. B.; Mathis, A.; Taylor, R.; Wandersee, L.; Bailey, K. W.; Sefing, E. J.; Hickerson, B. T.; Jung, K. H.; Sheridan, W. P.; Gowen, B. B. (2018). "Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters". Antiviral Research. 156: 38–45. doi:10.1016/j.antiviral.2018.05.013. PMC 6035881. PMID 29864447.
^ Rodgers, Paul (8 April 2014). "BioWar Lab Helping To Develop Treatment For Ebola". Forbes Magazine. {{cite web}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)
^ Julander JG, Siddharthan V, Evans J, Taylor R, Tolbert K, Apuli C, et al. (January 2017). "Efficacy of the broad-spectrum antiviral compound BCX4430 against Zika virus in cell culture and in a mouse model". Antiviral Research. 137: 14–22. doi:10.1016/j.antiviral.2016.11.003. PMC 5215849. PMID 27838352.
^ Praveen Duddu. Coronavirus outbreak: Vaccines/drugs in the pipeline for Covid-19. clinicaltrialsarena.com 19 February 2020.

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[pmid24590073-1] Warren TK, Wells J, Panchal RG, Stuthman KS, Garza NL, Van Tongeren SA, et al. (April 2014). "Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430" (PDF). Nature. 508 (7496): 402–5. Bibcode:2014Natur.508..402W. doi:10.1038/nature13027. PMID 24590073.

[pmid24111876-2] Kamat SS, Burgos ES, Raushel FM (October 2013). "Potent inhibition of the C-P lyase nucleosidase PhnI by Immucillin-A triphosphate". Biochemistry. 52 (42): 7366–8. doi:10.1021/bi4013287. PMC 3838859. PMID 24111876.

[3] Westover JB, et al. Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters. Antiviral Res. 2018 Aug;156:38-45. Westover, J. B.; Mathis, A.; Taylor, R.; Wandersee, L.; Bailey, K. W.; Sefing, E. J.; Hickerson, B. T.; Jung, K. H.; Sheridan, W. P.; Gowen, B. B. (2018). "Galidesivir limits Rift Valley fever virus infection and disease in Syrian golden hamsters". Antiviral Research. 156: 38–45. doi:10.1016/j.antiviral.2018.05.013. PMC 6035881. PMID 29864447.

[4] Rodgers, Paul (8 April 2014). "BioWar Lab Helping To Develop Treatment For Ebola". Forbes Magazine. {{cite web}}: Unknown parameter |name-list-format= ignored (|name-list-style= suggested) (help)

[pmid27838352-5] Julander JG, Siddharthan V, Evans J, Taylor R, Tolbert K, Apuli C, et al. (January 2017). "Efficacy of the broad-spectrum antiviral compound BCX4430 against Zika virus in cell culture and in a mouse model". Antiviral Research. 137: 14–22. doi:10.1016/j.antiviral.2016.11.003. PMC 5215849. PMID 27838352.

[clinicaltrialsarena-6] Praveen Duddu. Coronavirus outbreak: Vaccines/drugs in the pipeline for Covid-19. clinicaltrialsarena.com 19 February 2020.

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See also

References