Mechanism of action The substance potently and selectively blocks two receptor tyrosine kinase enzymes: anaplastic lymphoma kinase (ALK) and the RET proto-oncogene. The active metabolite M4 has similar activity against ALK. Inhibition of ALK subsequently blocks cell signalling pathways, including STAT3 and the PI3K/AKT/mTOR pathway, and induces death (apoptosis) of tumour cells. Pharmacokinetics Proposed metabolism of<unk> .<unk>  itself and the active metabolite M4 are the main compounds found in the circulation, while the others are minor metabolites. When taken with a meal, the absolute bioavailability of the drug is 37%, and highest blood plasma concentrations are reached after four to six hours. Steady state conditions are reached within seven days. Plasma protein binding of<unk>  and M4 is over 99%. The enzyme mainly responsible for<unk>  metabolism is CYP3A4; other CYP enzymes and aldehyde dehydrogenases only play a small role.<unk>  and M4 account for 76% of the circulating substance, while the rest are minor metabolites. Plasma half-life of<unk>  is 32.5 hours, and that of M4 is 30.7 hours. 98% are excreted via the faeces, of which 84% are unchanged<unk>  and 6% are M4. Less than 1% are found in the urine.
Alectinib
Vatalanib
Brigatinib
Abrocitinib
Regorafenib
Sorafenib
Nintedanib
Gilteritinib