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AssigneeRevolution Medicines, Inc.
InventorsJohn E. Knox, Elena S. KOLTUN, Kyle SEAMON, Aidan TOMLINSON, David E. WILDES, James CREGG
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The present disclosure relates to therapies for treating cancer. In particular, the present disclosure relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a RAS(ON) GTP hydrolysis-promoting compound optionally in combination with an additional therapeutic agent (e.g., a RAS(OFF) inhibitor, RTK inhibitor, SHP2 inhibitor, or SOS1 inhibitor), pharmaceutical compositions comprising a therapeutically effective amounts of the inhibitor(s), kits comprising the compositions and methods of use therefor.
A method of treating cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a RAS(ON) GTP hydrolysis-promoting compound and a RAS(OFF) inhibitor, wherein the cancer does not comprise a RAS mutation at position 61.
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A method of increasing sensitivity of a cell to a RAS(OFF) inhibitor, the method comprising contacting the cell with an effective amount of a RAS(ON) GTP hydrolysis-promoting compound, wherein the RAS(ON) GTP hydrolysis-promoting compound synergistically increases the sensitivity of the cell to the RAS(OFF) inhibitor.
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A pharmaceutical composition comprising (i) a means for promoting RAS(ON) GTP hydrolysis, and (ii) a pharmaceutically acceptable excipient.
A pharmaceutical composition comprising (i) a means for altering the position of glutamine 61 of RAS(ON) towards the gamma phosphate of GTP bound to the RAS(ON) protein, thereby increasing the GTP hydrolysis rate relative to the hydrolysis rate of RAS(ON) in the absence of said means, and (ii) a pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.