![Full text] MEK inhibitors and their potential in the treatment of ...](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_vY2MjISv3Xzr7o3-FAW1H0Scu73po61prVRqFtk4dZ1jB9vN7iNaacc8X_OvNTJcggLUsqr5Y7EyjMw0LBV1JbZhPQWssRNfAEbOKl37K_ezMU_fjzI_NOASTNeNDbZT216rmIvuwnf0WI6Hk=s0-d "Full text] MEK inhibitors and their potential in the treatment of ...")
src: www.dovepress.com
A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers. (See MAPK/ERK pathway#Clinical significance.)
Hence MEK inhibitors have potential for treatment of some cancers, especially BRAF-mutated melanoma, and KRAS/BRAF mutated colorectal cancer.
Video MEK inhibitor
Approved for clinical use
- Trametinib (GSK1120212), FDA-approved to treat BRAF-mutated melanoma. Also studied in combination with BRAF inhibitor dabrafenib to treat BRAF-mutated melanoma.
- Cobimetinib or XL518, approved by US FDA in Nov 2015 for use in combination with vemurafenib (Zelboraf(R)), for treatment of advanced melanoma with a BRAF V600E or V600K mutation.
Maps MEK inhibitor
In clinical trials
- Binimetinib (MEK162), is currently in phase 3 clinical trials for ovarian cancer, BRAF mutant melanoma, and NRAS mutant melanoma.
- Selumetinib, had a phase 2 clinical trial for non-small cell lung cancer (NSCLC) which demonstrated an improvement in PFS, and is now in phase III development in KRAS mutation positive NSCLC (SELECT-1, NCT01933932). Other ph 3 clinical trials underway include uveal melanoma (failed), and differentiated thyroid carcinoma.
- PD-325901, for breast cancer, colon cancer, and melanoma A phase II trial for advanced non-small cell lung cancer "did not meet its primary efficacy end point".
src: c8.alamy.com
Others
- CI-1040, PD035901
- TAK-733, preclinical for multiple myeloma.
src: cancerdiscovery.aacrjournals.org
References
Source of the article : Wikipedia