Introduction: Lorlatinib is a third-generation tyrosine kinase inhibitor approved for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer; cytochrome P450 (CYP) 3A plays an important role in the metabolism of lorlatinib. Conclusions: The addition of a single dose of lorlatinib to daily dosing with rifampin significantly reduced lorlatinib plasma exposure relative to a single dose of lorlatinib administered alone and was associated with severe but self-limiting transaminase elevations in all healthy participants. These observations support the contraindication in the product label against concomitant use of lorlatinib with all strong CYP3A inducers. READ ARTICLE
Advances in Therapy DOI:10.1007/s12325-019-01198-9
Authors: Joseph Chen, Huiping Xu, Sylvester Pawlak, Leonard P. James, Gerson Peltz, Kimberly Lee, Katherine Ginman, Michelle Bergeron & Yazdi K. Pithavala