Can Remdesivir and its Parent Nucleoside GS-441524 be Potential Oral Drugs? An in vitro and in vivo DMPK Assessment

Can Remdesivir and its Parent Nucleoside GS-441524 be Potential Oral Drugs? An in vitro and in vivo DMPK Assessment

Innovative Grade US Origin Mouse CD1 Plasma and Pooled Human Plasma Apheresis Derived from Innovative Research were used in the following study:

 

Can Remdesivir and its Parent Nucleoside GS-441524 be Potential Oral Drugs? An in vitro and in vivo DMPK Assessment

Jiashu Xie, Zhengqiang Wang

Acta Pharmaceutica Sinica B
March 5, 2021

To date, the only FDA-approved drug for treating COVID-19 is Remdesivir (RDV), which can only be administered intravenously. RDV is a ProTide drug derived from nucleoside GS-441524, and the potency of RDV is dependent on intracellular conversion into GS-441524 triphosphate.

In vitro studies of RDV in human liver cells showed low stability on its own, indicating poor potential for oral use. However, it was observed that the stability levels were boosted when in the presence of cobicistat. Further, in vivo studies in human and mouse plasma showed promising levels of conversion to GS-441524 triphosphate when administered orally, indicating that RDV could potentially be taken as an oral drug.

 

Related products available from Innovative Research also include:

Innovative Grade US Origin Mouse CD1 Whole Blood

Pooled Human Serum Off The Clot

Pooled Human AB Serum Plasma Derived