Phosphonate chemist by habit, scientist by choice, Molecular Sherlock by chance. MD/PhD student @utswmstp. Views are mine. #GS441524
Apr 12, 2023 • 13 tweets • 6 min read
NEW OBELDESIVIR (OBV; GS-5245) DATA! $GILD
Ph1 PK/PD from @GileadSciences' @ECCMID poster.
OBV = OBVIOUS! 🙊😂 #GS441524 #GS5245
Key points in thread 🧵 1/13
https://t.co/zOpymoJLicaskgileadmedical.com/conferences/co…
First, this was a healthy volunteer PK study. Impt to point this out bc it was strange that 25% of pts in PBO grp had grade 2 AE 🧐.
Also, note the dosing grps. They tested QD & BID regimens. The ph3 dose is 350 mg BID but this wasnt actually tested here...2/13
"Phase I trial, which involved 70 healthy adults, showed that obeldesivir reached sufficient concentrations in the blood and supports taking it without regard to food"
Since obeldesivir, figuring out the structure of undisclosed cmpds in the clinic has become my new hobby 🤠
So I'll periodically post structures of other cmpds here
I'll start w #VX548, a Nav1.8 inhibitor for treating pain by @VertexPharma $VRTX. Inspired by @cispt2 1/8
VX-548 is currently in ph3 for the tx of acute pain. From trials registry, the earliest trial date is on July 19, 2021. 2/8
First-in-Woman Safety, Tolerability, and Pharmacokinetics of Orally Administered #GS441524: A Broad-Spectrum Antiviral Treatment for #COVID19. A 🧵1/7 osf.io/am5s8/
Part 1 of the study: 750 mg GS-441524 was orally administered as a solution QD for 7 days. D1-5 were performed in the fasted state. D6-7 in the fed state. There was a slight food effect that seemed to hamper drug absorption. Cmax ~2.4-3 uM. AUC ~26-33 uM. 2/7
May 14, 2020 • 10 tweets • 8 min read
Fun fact: #remdesivir is almost certainly not the species that reaches #COVID19 patients' lungs! Its nucleoside #GS441524 is. Wrote this piece for @statnews explaining this! @GileadSciences consider aerosolizing GS-441524 prophylaxis. Pls read and RT! 1/x
bit.ly/3dIc0Au
I've been reading a lot of general audience/science articles on #remdesivir. Many of these articles seem to confuse nucleoSIDES with nucleoTIDES. Here's the difference, feat. important figures. 2/x