Adam Sikora

Drobnocząsteczkowe inhibitory kinaz w terapii celowanej czerniaka
2015-03-10

Small molecule kinase inhibitors in targeted therapy melanoma

Melanoma is a cancer that arises from melanocytes, specialized pigment cells that are found predominantly in the skin. The incidence of melanoma is rising steadily in western populations – the number of cases worldwide has dubled in past 20 years. In its early stages malignant melanoma can be cured by surgical resection, but once it has progressed to the metastatic stage it is extremely difficult to treat and does not respond to current therapies. The discovery of the genetic underpinnings of this historically refractory disease has exposed potential targets therapy, BRAF mutations being principal among them. In the least years following the discovery of BRAF mutations in 60–80% of advanced melanomas, only recently have potent shown efficacy and selective inhibitors of this intracellular signaling molecule shown efficacy from early clinical testing. Vemurafenib (PLX4032), dabrafenib (GSK2118436) and trametinib (GSK1120212), the orally available and well tolerated agents are on the verge of transforming the landscape of melanoma therapy based on the promising results of their repective phase I, II and III trials.

Keywords: melanoma, targeted therapy, vemurafenib, dabrafenib, trametinib.

© Farm Pol, 2015, 71(2): 87-91