NCATS is evaluating GS-441524 as a potential treatment for SARS-CoV-2 infection.
Molecular Weight :
291.26
GS-441524: PK Property Summary
* IV dose: 5 mg/kg from mouse/rat; 2 mg/kg from dog/cyno
** PO dose: 10 mg/kg from mouse/rat; 5 mg/kg from dog/cyno
GS-441524 PK Property Overview
- Low to moderate clearance (CLp)
- Moderate volume of distribution (Vdss)
- Large variation in oral bioavailability (F), from 8.3% in cyno to 85% in dog
- GS-441524 for these studies was purchased from AK Scientific and characterized by NCATS
Calculated PK Properties
Calculated PK Properties
Calculated PK Properties
PK Study: Cynomolgus Macaque
Calculated PK Properties
Cynomolgus Macaque PK*
*Concentration at 48 hr was <LLOQ of 1 ng/mL
GS-441524: 7-Day Dose Range Finding Toxicology
Non-GLP Dose Range Finding Toxicology (DRF) studies in three species are complete.
These studies inform species selection and doses for GLP toxicology studies.
- PO, BID dosing
- Formulation: 5% ethanol, 30% PG, 45% PEG-400, 20% water, 1 equiv. HCl (rat); powder in capsule (dog); 0.5% CMC in water (cyno)
- GS-441524 purchased from Alichem and characterized by NCATS
- Preliminary data, final study reports pending
- GS-441524 well tolerated at the maximum feasible dose, supporting progression to GLP toxicology studies
GS-441524: GLP Toxicology
Rat and dog selected as GLP toxicology species.
GS-441524: Clinical Studies
GMP manufacturing activities are underway.
