We discover and develop important new medicines for cancer patients by translating frontier oncology targets.
Frontier oncology targets are proteins that drive the growth of cancers or that control immune responses that can defeat them. Frontier targets have not been drugged successfully before or have been inadequately served by previous drug discovery efforts. Our current discovery programs are focused in two areas, our Phosphatase and Beyond Rule of 5 (bRo5) Platforms.
Revolution Medicines has made a major commitment toward discovering and developing small molecule inhibitors of protein tyrosine phosphatases (PTPs), enzymes that regulate critical cellular proteins by selectively removing phosphate groups attached to certain tyrosine residues. We have two ongoing programs, each targeted at a tyrosine phosphatase enzyme, SHP2 and SHP1.
Some frontier targets are suitable to drug discovery focused on small molecule ligands whose size and physiochemical properties (“Rule of 5” or “Ro5”) are correlated with oral bioavailability, while other targets require larger and more complex ligands (“Beyond Rule of 5” or “bRo5”) that go beyond most traditional drug discovery platforms in pharmaceutical companies. Revolution Medicines has a major commitment to developing bRo5 small molecule drug candidates for targets like 4EBP1/mTORC1.
We have a robust pipeline of preclinical programs in the oncology and immuno-oncology space, and expect to enter clinical development with our lead SHP2 inhibitor in 2018.