Thread by @victoriacyanide

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

A series of patents were recently published by Vertex on the same series of the inhibitors (Dec. 8, 2022)

These all have the same priority/filing/publish dates

Earliest priority traces back to June 4, 2021: ~1 mo. earlier than 1st trial reg (July 19, 2021) 3/8

The most telling/interesting of this series are:

WO 2022/256708 A1 (solid dosage forms & dosing regimens)

WO 2022/256660 A1 (process chemistry) 4/8
worldwide.espacenet.com/patent/search?…
worldwide.espacenet.com/patent/search?…

Both patents describe the same compound💡 5/8

The biggest giveaways are in the solid dosage forms & dosing patent, which includes trial designs for peripherial diabetic neuropathy & bunionectomy as examples.

Treatment arms & dosing checks out

It becomes readily apparent that compound 1 = VX-548
6/8
clinicaltrials.gov/ct2/show/NCT05…

Example 4 on bunionectomy seals the deal. Crazy sig fig match! 7/8
investors.vrtx.com/news-releases/…
clinicaltrials.gov/ct2/show/NCT04…

Thread that inspired this thread + summary of the non-opiod pain landscape 8/8

https://twitter.com/cispt2/status/1619506107764068352?s=20