5 results about "Trametinib" patented technology

The invention discloses an MEK / HDAC double-target inhibitor as well as a synthesis method and application thereof, and belongs to the technical field of medicines. Through molecular docking and in-vitro thermodynamic migration experiments, the applicant finds that the inhibitor not only can stabilize MEK and HDAC proteins, but also can be specifically combined with the MEK and HDAC proteins in an intracellular environment; protein immunoblotting experiments find that the inhibitor can inhibit reactivation of ERK, overcomes the limitation of a single-target inhibitor in curative effect and activity, and significantly improves the drug resistance problem of trametinib in ovarian cancer treatment and various EGFR-TKI treatment in non-small cell lung cancer treatment; furthermore, an in-vitro anti-tumor activity experiment shows that the IC50 value of the MEK / HDAC inhibitor on tumor cells from human ovarian cancer and various lung cancers is 0.07-10 mu M, and the MEK / HDAC inhibitor has a wide and remarkable proliferation inhibition effect.

Compounds of formula (I) [Formula 1] A pharmaceutical combination comprising: (a) a Raf inhibitor that is TIFF2026503267000030.tif4686 or a pharmaceutically acceptable salt thereof; (b) a KRAS G12C inhibitor T; and / or (c) trametinib.

A method of treating and / or preventing a skin toxicity associated with the administration of a therapeutic treatment comprising trametinib, naporafenib, or a combination thereof in a subject in need thereof; the method comprising pre-emptively administering to the subject an effective amount of a rash treatment.

Disclosed herein is a method of treating melanoma in a subject, the method comprising administering (a) naporafenib and (b) a MEK inhibitor such as trametinib, wherein the melanoma comprises a cell that has: 1) a wild-type NRAS genotype and 2) a wild-type BRAF or a wild-type BRAF genotype.