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[News event]: Pfizer announced today that it will acquire a partial interest in the estrogen receptor PROTAC drug ARV-471 developed by Arvinas, a pioneer in protein degradation, with a down payment of 650 million and a stock subscription of 350 million, plus 1.
4 billion potential mileage
.
The two will be jointly responsible for the clinical development of the drug, and the profit will be divided by 5/5.
[Drug Source Analysis]: Avinas is the pioneer of PROTAC technology, created by the famous scientist Craig Crews
.
Crews invented the proteomic inhibitor Carfilzomib (Kyprolis®) and founded Proteolix to develop this drug
There are several practical problems to achieve this goal systematically
.
First, although dual-target drug design has a long history, its successful cases are very limited
However, the dose-effect relationship of PROTAC is also completely different from traditional inhibitors.
In theory, a PROTAC drug molecule can completely degrade the target protein if it is sufficiently efficient
.
Because this is a catalytic process, PROTAC does not need to sit in the target binding cavity to complete the inhibitory function, and then leave to degrade the next protein molecule
As PROTAC like ARV-471 has a certain clinical effect and does not have too serious platform-related side effects, protein degradation has quickly become a major frontier of small molecule drugs
.
However, it is difficult to judge the success or failure of new drugs in the early stage.
