GS-441524 for COVID19 not pursued by GILEAD

Categories:
Collaborating on patent analysis and opposition/invalidation filing
Country:
United States of America
Name:
Florian Muller

GS-441524 is a nucleoside, which forms the pharmacophore of Remdesivir. Remdesivir was developed because GS-441524 phosphorylation, according to GILEAD, does not occur in human cells (as referenced in the articles below, this is contradicted by published data). GS-441524 is likely to be a better COVID19 drug because 1) much simpler to mass produce 2) more even distribution across organs without the dose-limiting toxicities associated with Remdesivir's selectivity for liver cells 3) greater water solubility allowing easy formulation for inhalation (high drug delivery to lung). However, GILEAD owns patent rights to GS-441524 (2009) and Remdesivir (2017); The 2009 patent of GS-441524 may be invalid due to prior art: as we have seen in the GILEAD vs MERK trial (which Merk initially won), there is a large amount of prior art in the nucleoside space that may invalidate the GS-441524 patent.

https://www.statnews.com/2020/05/14/gilead-should-ditch-remdesivir-and-focus-on-its-simpler-safer-ancestor/

https://www.vettimes.co.uk/news/vet-science-being-ignored-in-quest-for-covid-19-drug/

Expertise is sought in reviewing the 2009 patent covering GS-441524 to find potentially invalidating prior art either in the patent or public domain literature.

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