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GS-441524
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GS-441524
GS-441524 is a nucleoside analogue antiviral drug which was developed by Gilead Sciences. It is the main plasma metabolite of the antiviral prodrug remdesivir, and has a half-life of around 24 hours in human patients. Remdesivir and GS-441524 were both found to be effective in vitro against feline coronavirus strains responsible for feline infectious peritonitis (FIP), a lethal systemic disease affecting domestic cats. Remdesivir was never tested in cats (though some vets now offer it), but GS-441524 has been found to be effective treatment for FIP.
It is widely used despite no official FDA approval due to Gilead's refusal to license this drug for veterinary use. In several countries oral GS-441524 tablets (and injectable remdesivir) became legally available to vets for the treatment of FIP in cats, for example Australia, the Netherlands, and the United Kingdom.
Besides remdesivir, other prodrugs include obeldesivir (Gilead Sciences, Phase III) and deuremidevir (Vigonvita/Junshi, conditional approval in China).
Since untreated feline infectious peritonitis (FIP) is fatal in almost all cases and in most countries there are no approved treatments available, GS-441524 has reportedly been sold illegally worldwide on the black market and used by pet owners to treat affected cats, although Gilead Sciences has refused to license the drug for veterinary use. Its efficacy for this purpose has been conclusively demonstrated in multiple trials, including field trials, and even in more complicated forms of FIP such as those with multisystemic or neurological involvement. In naturally infected cats, a recovery rate of over 80% has been observed with GS-441524 treatment in several studies and in treatment programs in countries where the drug is legalised.
As of 2023, oral GS-441524 tablets or capsules (and injectable remdesivir) became legally available to vets for the treatment of FIP in cats in Australia, the Netherlands, and the United Kingdom. As of June 2024, the medication is available in the U.S.
GS-441524 is either similar to or more potent than remdesivir against SARS-CoV-2 in cell culture, with some researchers arguing that GS-441524 would be better than remdesivir for the treatment of COVID-19. Specific advantages cited include ease of synthesis, lower kidney and hepatotoxicity, as well as potential for oral delivery (which is precluded of remdesivir because of poor hepatic stability and first pass metabolism). The public health advocacy group, Public Citizen, in an open letter urged the DHHS and Gilead to investigate GS-441524 for the treatment of COVID-19, suggesting that Gilead was not doing so for financial motives related to the longer intellectual property lifespan of Remdesivir, whose patents expire no sooner than 2035. Direct efficacy against SARS-CoV-2 was demonstrated in a mouse model of COVID-19.
GS-441524 has been directly administered in a healthy human, with highest plasma concentrations of 12 uM reached, which is >10 times the concentration required for activity against SARS-CoV-2 in culture.
GS-441524 is sold as a research chemical in very high purity (>99% by NMR and HPLC) by a number of suppliers. Such sales for research purposes do not constitute patent infringements which was affirmed by a U.S. Supreme Court decision. However, despite the high purity, under FDA regulations, such chemicals are not allowed for clinical trials since their manufacture is not performed under FDA cGMP certified conditions.
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GS-441524
GS-441524 is a nucleoside analogue antiviral drug which was developed by Gilead Sciences. It is the main plasma metabolite of the antiviral prodrug remdesivir, and has a half-life of around 24 hours in human patients. Remdesivir and GS-441524 were both found to be effective in vitro against feline coronavirus strains responsible for feline infectious peritonitis (FIP), a lethal systemic disease affecting domestic cats. Remdesivir was never tested in cats (though some vets now offer it), but GS-441524 has been found to be effective treatment for FIP.
It is widely used despite no official FDA approval due to Gilead's refusal to license this drug for veterinary use. In several countries oral GS-441524 tablets (and injectable remdesivir) became legally available to vets for the treatment of FIP in cats, for example Australia, the Netherlands, and the United Kingdom.
Besides remdesivir, other prodrugs include obeldesivir (Gilead Sciences, Phase III) and deuremidevir (Vigonvita/Junshi, conditional approval in China).
Since untreated feline infectious peritonitis (FIP) is fatal in almost all cases and in most countries there are no approved treatments available, GS-441524 has reportedly been sold illegally worldwide on the black market and used by pet owners to treat affected cats, although Gilead Sciences has refused to license the drug for veterinary use. Its efficacy for this purpose has been conclusively demonstrated in multiple trials, including field trials, and even in more complicated forms of FIP such as those with multisystemic or neurological involvement. In naturally infected cats, a recovery rate of over 80% has been observed with GS-441524 treatment in several studies and in treatment programs in countries where the drug is legalised.
As of 2023, oral GS-441524 tablets or capsules (and injectable remdesivir) became legally available to vets for the treatment of FIP in cats in Australia, the Netherlands, and the United Kingdom. As of June 2024, the medication is available in the U.S.
GS-441524 is either similar to or more potent than remdesivir against SARS-CoV-2 in cell culture, with some researchers arguing that GS-441524 would be better than remdesivir for the treatment of COVID-19. Specific advantages cited include ease of synthesis, lower kidney and hepatotoxicity, as well as potential for oral delivery (which is precluded of remdesivir because of poor hepatic stability and first pass metabolism). The public health advocacy group, Public Citizen, in an open letter urged the DHHS and Gilead to investigate GS-441524 for the treatment of COVID-19, suggesting that Gilead was not doing so for financial motives related to the longer intellectual property lifespan of Remdesivir, whose patents expire no sooner than 2035. Direct efficacy against SARS-CoV-2 was demonstrated in a mouse model of COVID-19.
GS-441524 has been directly administered in a healthy human, with highest plasma concentrations of 12 uM reached, which is >10 times the concentration required for activity against SARS-CoV-2 in culture.
GS-441524 is sold as a research chemical in very high purity (>99% by NMR and HPLC) by a number of suppliers. Such sales for research purposes do not constitute patent infringements which was affirmed by a U.S. Supreme Court decision. However, despite the high purity, under FDA regulations, such chemicals are not allowed for clinical trials since their manufacture is not performed under FDA cGMP certified conditions.
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