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Pharmacological effects of Lorlatinib tablets
In cell line models, lorlatinib was demonstrated to have subnanomolar potency against wild-type ALK while retaining potency against multiple acquired crizotinib-resistant ALK mutants, including G1202R. In a cell viability assay comparing lorlatinib with crizotinib, ceritinib, alectinib, and ensatinib, lorlatinib was shown to be the most potent inhibitor against wild-type ALK as well as TKI-resistant ALK mutants, including G1202R, and was independent of EML4-ALK variants and other fusions of ALK, indicating that only lorlatinib is able to inhibit ALK G1202R mutants.
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