RE: Patent application13 Dec 2022 17:15
Wow! Great find ES.
It seems to be a way of extending the circulating half-life of the pre|CISION prodrugs by linking 5140 to a serum protein OR... and this is where it gets very interesting... to a moiety that binds to a serum protein. All possibilities for that moiety are given of course (covering all bases) but amongst them are Affimers®. That would be TMAC™.
So the 'drug' is cytotoxic agent linked to 5140 linked to Affimer which binds to a serum protein which carries the drug around the body, avoiding the destruction in the liver because the liver lets serum proteins through unharmed - imagine the problems to you, me and all aninals with a liver if it didn't!
The only thing I don't understand is how, physically, the dipeptide linker (5140) is connected to both the cytotoxic agent and the Affimer when the dipeptide linker is the 'key' that fits into the FAP 'lock' in order for the FAP enzyme to cleave the prodrug off. Logic says that the Affirmer (big enough to bind to the serum protein) would need to be inside the lock space as well as the dipeptide. Probably explained within the many diagrams of chemical structures shown in the patent but not something I need to devote time to - what will be will be.
I'd just like to say that my total admiration goes to those folks who direct the research in order to define the extend and boundaries of the invention, who construct the patent specification, who write the patent application and who translate it into other languages, as well as the poor sods at the various patent offices who have to examine it for novelty.