Inhibition of trk kinase mediated tumor growth and disease progression
OwnerDaniel L. FLYNN, Michael D. KAUFMAN +1inventors
InventorsDaniel L. FLYNN, Michael D. KAUFMAN, Bryan D. SMITH
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Abstract
It has been shown that Compound 1 unexpectedly and potently inhibits TRK kinases, including all three forms of TRK: NTRK1, NTRK2, and NTRK3. Additionally it has been shown that Compound 1 potently inhibits oncogenic mutated forms of TRK kinases, including fusion proteins. By way of exemplification, Compound 1 potently inhibits the NTRK1 oncogenic fusion protein TPM3/NTRK1 in cellular assays. Compound 1 inhibits TRK kinase mediated tumor growth in vivo in a TPM3/NTRK1 xenograft model.
Claims27
A method of inhibiting TRK kinase mediated tumor growth, survival, or disease progression comprising administering to a subject in need thereof an effective amount of N-(4-(2-(cyclopropanecarboxamido)pyridin-4-yloxy)-2,5-difluorophenyl)-N′-(4)cyclopropane-1,1-dicarboxamide, or a pharmaceutically acceptable salt thereof.
A method of treating cancer in a subject in need thereof comprising comprising administering to the subject an effective amount of N-(4-(2-(cyclopropanecarboxamido)pyridin-4-yloxy)-2,5-difluorophenyl)-N′-(4)cyclopropane-1,1-dicarboxamide, or a pharmaceutically acceptable salt thereof, wherein the cancer is associated with overexpression of a TRK kinase, mutation of a TRK kinase, and/or a TRK kinase fusion protein.
Dependencies are inferred from the claim text.