Than melanomas Alternatively Nnte it targeted a receptor kinase upstream Rts signing Alsen of the Ras / Raf / MEK / ERK cascade. It is important to study the effects of sorafenib combination with a MEK Bicalutamide Casodex inhibitor examined to melanoma, and some other types of cancer. Sorafenib k can Specifically expressing VEGF and other membrane receptors on certain cancer cells, w While the MEK inhibitor is exactly to the cascade Raf / MEK / ERK, eliminate the Unweighted Activated similar oncogene or other BRAF signaling molecules upstream mutant. To improve the effectiveness of sorafenib in the treatment of melanoma, is combined with standard chemotherapeutics. Sorafenib, unlike other new kinase inhibitors targeting the kinase mutant compared to WT, binds both WT and mutant V600E B Raf proteins And delayed Siege growth of melanoma xenografts nozzles at M.
Show other, newly developed inhibitors of Raf kinase can gr Ere selectivity t compared with the mutant compared with WT Raf proteins. Treatment of malignant melanoma is pancreas, heart lon, lung, breast, and HCC with Selumetinib Selumetinib has undergone an inhibitor of MEK1 orally, the active phase II clinical development. It is one of the inhibitors of MEK1 in the first randomized phase II to evaluate. Selumetinib showed significant tumor suppressor activity T pr Clinical models of cancer, including melanoma, pancreatic, heart lon, lung, liver and breast cancer. Effects can be enhanced Selumetinib fa Significantly, when the tumor is a mutation that activates the Raf / MEK / ERK. Selumetinib very promising in the treatment of pancreatic cancer, the h Frequently.
Mutations that can lead to Ras downstream Raf / activation of the MEK / ERK Because of the h Ufigen detection of pancreatic cancer at an advanced stage, it may be necessary, combined with an inhibitor of signal transduction herk Mmlicher chemotherapy after surgical removal of pancreatic cancer, when m Possible. Selumetinib has undergone several Phase I and II clinical trials. A Phase I study to evaluate the safety, reps Compatibility and pharmacokinetics of selumetinib patients with various solid tumors was performed. Phase II trials have compared: The efficacy of temozolomide against selumetinib patients with inoperable stage 3 or 4 melanoma patients the efficacy and safety of selumetinib over capecitabine pancreatic cancer advanced or metastatic non for gemcitabine therapy, the efficacy and safety compared with selumetinib in patients with NSCLC who have not responded to one or two chemotherapy pemetrexed have responded well.
efficacy and safety against selumetinib capectiabine patients with colorectal cancer who have not responded to one or two prior chemotherapy The first clinical trials were not strong support for the use of MEK inhibitors as monotherapy in patients with cancer. No provision for pre-existing activation of the Raf / MEK before screening / ERK The properly S identification of cancer patients activation of the Raf / MEK / ERK may be necessary to prescribe MEK inhibitors as part of their therapy, as we already mentioned Have hnt that MEK inhibitors are cytostatic rather than cytotoxic.