Lorlatinib (PF-06463922, Pfizer Oncology, Groton, CT, USA) is an oral TKI that
targets both ALK and ROS1 with high affinity and good CNS penetration [91].
Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2. Potent MEK inhibitor.
Lorlatinib is the sole third-generation ALK inhibitor at this time; it is approved for
ALK-positive NSCLC patients who progressed on at least two ALK inhibitors with
one being crizotinib or who progressed on alectinib or ceritinib if either is used in
the frontline setting.
[1] iverson c, larson g, lai c, et al. rdea119/bay 869766: a potent, selective, allosteric inhibitor of mek1/2 for the treatment of cancer. cancer research, 2009, 69(17): 6839-6847.
