Our drug discovery and development activities are focused on inhibiting frontier oncology targets that play key roles within notorious growth and survival pathways, with particular emphasis on the RAS signaling pathway.   

These critical pathways are among the most frequently exploited in human cancers, whereby mutations in key nodes lead to excessive or aberrant signaling and cell growth. For example, many tumors of different types exhibit excessive activation of the RAS signaling cascade as a result of mutations in RTKs, RAS, NF1 or RAF. Mutations in RAS proteins alone account for approximately 30% of all human cancers in the US, many of which are fatal.

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Despite the critical roles that the RAS and associated signaling pathways play in tumor development and survival, development of drugs for targets within these pathways has proven challenging. Several of these proteins possess particular structural properties, such as flat surfaces and a lack of typical binding pockets, that make them hard to target pharmacologically.

At Revolution Medicines, we are actively advancing therapeutic programs against the following RAS Companion Inhibitors: SHP2, mTORC1/4EBP1 and SOS1; and against RAS(ON) Inhibitors. Our proprietary innovation engine is allowing us to create small molecule candidates designed to inhibit these targets, which were previously viewed as difficult-to-drug or entirely “undruggable.”


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