PROTAC -- new class of drug - first trial for prostate cancer

[George71]

"Gold rush

Following the 2015 flurry of small-molecule PROTACs, Deshaies, who had left the field, penned an opinion piece declaring that PROTACs had the potential to become a major new class of drug, possibly surpassing two of the hottest drug-development areas of all time — protein kinase inhibitors and monoclonal antibodies13. “The gold rush is on!” Deshaies wrote at the time.

Since then, he says, it has only intensified. He joined Amgen in 2017 and now oversees the company’s work in the area.

The Arvinas trial, expected to begin by mid-2019, will include 28–36 men with metastatic prostate cancer and will last around 9 months, says Taylor. It is usual for any new class of drug to go after a well-known target, where the biology and toxicology are well-understood, and Arvinas’s first candidate is no exception. It degrades the androgen receptor, a protein that is already targeted by a handful of approved drugs. The company hopes that by degrading rather than inhibiting the receptor, its PROTAC will be able to treat people who have become resistant to or see no benefit from existing drugs. And if the candidate succeeds, the field will finally have the clinical data that everyone is looking for. Arvinas will have shown that a PROTAC can be a drug."

nature.com/articles/d41586-...

[NPfisherman]

Great find, my man... a new class of drugs....doesn't block AR but degrades...if my thought process is correct, then wild/mutated AR would be degraded and an end to resistance...can it be?? The science is coming !!!!

Fish

[NPfisherman]

More info on Arvinas....

fiercebiotech.com/biotech/a...

They even have a second generation candidate to target AR-V7....If Pfizer put 830 million plus an "undisclosed amount", then someone sees potential here...trial by mid 2019....outstanding...

Fish

[Jbooml]

My God....my hopes are being fulfilled before my tearing eyes...an AR toxin...i wonder if they've refined it to look at missignalling active sites....that i thought would be the perfect solution to metastatic drift...i'm on cloud 9

thank you george for this incredibly wonderful information....now lets hope it works safely.

[p3d1]

Great find, this would seem to have great potential as another tool to fight with. Thank you George71 for posting this.,

[p3d1]

More information found here ir.arvinas.com/events-and-p...

[ElemanJ]

Good News. Considering the ongoing Trials FDA has given a fast track designation for PROTAC for treatment of CRPCa.

[TJGuy]

Any new news on Protac, post last comment 1 year old.

[George71 in reply to TJGuy]

"Arvinas is currently evaluating ARV-110 in a Phase 1 study for men with castration-resistant metastatic prostate cancer (mCRPC) who have progressed on standards of care."

arvinas.com/pipeline-progra...

"In a patient-derived xenograft (PDX) model derived from a patient not treated with, but insensitive to enzalutamide, orally delivered ARV-110 significantly inhibited the growth of enzalutamide-insensitive tumors (tumor growth inhibition: 100%)."

they list the trial as NCT03888612

for those who are mCRPC and have progressed on standard of care therapies.

It may work for everyone upfront -- who can tell.

clinicaltrials.gov/ct2/resu...

[George71 in reply to TJGuy]

Contact: Mary Garfield 475-234-5736 [e-mail]

Contact: Jennifer Ranciato 475-234-5700 [e-mail]