This morning I woke up to the news in an email alert that one of my client companies, sanofi-aventis, has been busy on the licensing front again after their recent deal with BiPar. This time they have licensed two compounds from Exelixis, which are PI3-kinase inhibitors, XL-147 and XL-765. You can read more about the deal itself on Mike Huckman's CNBC blog. Regular readers of this blog will recall some previous posts on PI3-kinase inhibition such as here and here.
It's an interesting and relatively 'hot' pathway with the advent of mTOR inhibitors and the role of AKT-PI3-Kinase pathway in potentially reducing drug resistance and limiting the feedback loop seen with mTOR.
The deal with a big Pharma suitor was inevitable after Exelixis signalled their intentions last December during the end of year pipeline update, according to my notes made at the time. The slight development lead in this area turned into a profitable deal for Exelixis.
At the recent AACR meeting in Denver, I noticed there were several others not far behind and some phase I data is expected to be presented next week at ASCO by Semafore on their PI3-kinase inhibitor, SF1126.
According to one of the abstracts:
"SF1126 is composed of the pan PI3K inhibitor LY294002 conjugated to an RGD targeting peptide. It is designed to increased solubility and binding to integrins expressed on tumor vasculature. This targeted prodrug enhances tumor delivery of the active inhibitor, improving antitumor efficacy and tolerability in xenograft models."
Other companies with receptor tyrosine kinase inhibitors (RTKIs) in phase I development include Novartis, who have two PI3-kinase inhibitors BEZ235 and BGT226, Genentech with GDC-0941 and Merck, who have an AKT inhibitor, MK-2206. There are also others in preclinical development. The number of mTOR inhibitors in R&D is now too numerous to mention in addition to the three already available commercially (sirolimus, temsirolimus and everolimus).
In the final analysis though, this looks a very good deal for Exelixis, who get another couple of their portfolio licensed out and relatively low risk for sanofi-aventis but neither PI3-K inhibitor will address the urgent shortfall they face when both Taxotere and Eloxatin go off patent in the very near future. Some late phase II/III compounds are still a glaring gap in the French company's pipeline.