Tivatinib (ARQ-197)

[donocco]

Elizabeth

If you think of it like the alphabet it becomes less formidble. To say P13K to AKT to MTor is just like saying A B C.

Your idea of a P13K inhibitor makes a lot of sense. There is one in the pipeline called Buparlisib or BMK-120.
There is another problem though. The signal transduction (P13K to AKT etc doesnt just go downstream. It also goes upstream.

Usually AKT activates Mtor, but MTor has 2 forms 1 and 2. Drugs like affinitor inhibit form 1 and dont have that strong an effect on MTOR-C2 or form 2. MTor-C2 can act upstream and activate AKT. So even blocking P13K isnt the whole answer. We need Mtor inhibitors that are effective against both forms of M-Tor.

Paul