Structural formula of Brigatinib/Brigatinib

Brigatinib/Brigatinib is a kinase inhibitor, its chemical name is 5-Chloro-N4-[2-(dimethylphosphoryl)phenyl]-N2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine. The molecular formula is C29H39ClN7O2P, which corresponds to a molecular weight of 584.10g/mol. Brigatinib hydrochloride is an off-white to beige/tan solid that is taken orally as film-coated tablets containing 180 mg, 90 mg or 30 mg of brigatinib.

Brigatinib is a second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) that is highly active against non-small cell lung cancer (NSCLC) harboring ALK translocations. Brigatinib was found to be very effective against different ALK resistance mutations that mediate the biological process of acquired resistance, especially G1269A ALK C1156Y, I1171S/T, V1180L, etc. Different clinical trials have evaluated the activity of brigatinib in crizotinib-resistant patients, confirming high activity and durable responses, not only in parenchymal disease but also in intracranial disease.

This original drug is marketed in China under the name brigatinib, and has entered the scope of Class B medical insurance. Specifications The price of 30mg*14 tablets*2 tablets per box may be around 8,000 yuan, which is relatively expensive. Currently, there are relatively cheap generic brigatinib drugs on the market overseas. Their drug ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of a box of 90mg*30 tablets produced by a Bangladesh pharmaceutical factory is around 2,000 yuan (the price may fluctuate due to exchange rates).