Alectinib is another selective ALK inhibitor that is able to overcome resistance
mutations from prior crizotinib exposure [38].
Chemische Eigenschaften
White to Off-White Solid
Indications
Alectinib (Alecensa(R), Roche) was approved first in Japan in 2014 and then by US FDA in 2015 as a second-generation ALK inhibitor for NSCLC treatment on patients who have progressed or do not tolerate crizotinib. Developed through a structure-based drug design approach, alectinib is a benzocarbazolone derivative that has shown potent inhibitory activity against ALK (IC50 value of 1.9 nM) and gatekeeper mutant L1196M ALK (IC50 value of 1.6 nM). Alectinib is effective with crizotinib-resistant ALK mutations on L1196M, F1174L, R1275Q, and C1156Y. In addition, an array of small-molecule inhibitors are currently being evaluated by several clinical trials for ALK-driven tumors.
Definition
ChEBI: An organic heterotetracyclic compound that is 6,6-dimethyl-5,6-dihydro-11H-benzo[b]carbazol-11-one carrying additional cyano, 4-(morpholin-4-yl)piperidin-1-yl and ethyl substituents at positions 3, 8 and 9 respectively. Used (as the hydr
chloride salt) for the treatment of patients with anaplastic lymphoma kinase-positive, metastatic non-small cell lung cancer.
Trademarks
Alecensa?
Alectinib Upstream-Materialien And Downstream Produkte