Trametinib

Products Trametinib was approved in the form of film-coated tablets in the United States in 2013, in the EU in 2014, and in many countries in 2016 (Mekinist). Structure and properties Trametinib (C26H23FIN5O4, Mr = 615.4 g/mol) is a pyridine and a pyrimidine derivative. It is present in the drug product as trametinib dimethyl sulfoxide, … Trametinib

Kinase Inhibitors

Background Kinases (phosphotransferases) are a large family of enzymes involved in the transduction and amplification of signals on and in cells. They exert their effects by phosphorylating their substrates, that is, by adding a phosphate group to the molecules (Figure). Kinases have complicated names that are usually abbreviated: ALK, AXL, BCR-ABL, c-Kit, c-Met, ERBB, EGFR, … Kinase Inhibitors

Melanoma Causes and Treatment

Symptoms Melanomas are discolored, growing, skin lesions that arise from pigmented moles in about 30% of cases. They are found primarily on the skin, but can occur anywhere melanocytes are found, including the oral mucosa, respiratory tract, or eye, for example. In men they are most common on the upper body, in women on the … Melanoma Causes and Treatment

Vemurafenib

Products Vemurafenib was approved in 2011 in film-coated tablet form (Zelboraf). Structure and properties Vemurafenib (C23H18ClF2N3O3S, Mr = 489.9 g/mol) is a white, crystalline substance that is practically insoluble in water. Effects Vemurafenib (ATC L01XE15) has antitumor and antiproliferative properties. It reduces mortality and increases survival. The properties are based on inhibition of the mutant … Vemurafenib

Dabrafenib

Products Dabrafenib was approved in the US and EU in 2013 and in many countries in 2014 in hard capsule form (Tafinlar). Structure and properties Dabrafenib (C23H20F3N5O2S2, Mr = 519.6 g/mol) is present in drugs as dabrafenib mesilate, a white to slightly colored powder that is practically insoluble in water. It is a thiazole and … Dabrafenib