Which generation of targeted drug is trametinib?

Trametinib (Trametinib) is a potent small molecule inhibitor of MEK kinase. It is a second generation allosteric non-competitive inhibitor of ATP with nanomolar activity against purified MEK 1 and MEK 2 kinases. Preclinical studies demonstrated potent inhibition of p-ERK 1/2, which correlated with potent cell growth inhibition in tumor cell lines harboring mutated B-RAF or Ras. Through this mechanism, trametinib induces cell cycle arrest.

Trametinib is the first MEK1/2 inhibitor approved by the U.S. Food and Drug Administration (FDA). It was approved in May 2013 for the treatment of BRAF V600E/K melanoma. Trametinib treatment entered clinical evaluation after it showed significant tumor growth inhibition in a number of preclinical human tumor xenograft models. In a phase I dose-escalation trial in 206 patients with advanced solid tumors, the once-daily 2 mg dosing regimen of trametinib was found to be tolerable and recommended for use in the phase II study. Rash and diarrhea were the most common adverse events.

The original drug of Trametinib has been launched in China and is included in the scope of medical insurance, but it may only be available to patients who meet the indications. The price of 2 mg*30 tablets is more than RMB 10,000. The original drug of Trametinib sold overseas, with the price of 2 mg*30 tablets, is more than RMB 7,000 (the price may fluctuate due to exchange rates). There are also generic trametinib drugs produced in other countries overseas, and their drug ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of a 2mg*30 tablet of a generic drug produced by a Laos pharmaceutical factory is more than 2,000 yuan (the price may fluctuate due to the exchange rate).