Background: Anaplastic lymphoma kinase (ALK) gene rearrangements are oncogenic drivers in non-small-cell lung cancer (NSCLC). TSR-011 is a dual ALK and tropomyosin-related kinase (TRK) inhibitor, active against ALK inhibitor resistant tumours in preclinical studies. Here, we report the safety, tolerability and recommended phase 2 dose (RP2D) of TSR-011 in patients with relapsed or refractory ALK- and TRK-positive advanced cancers. Conclusions: At the RP2D (40 mg Q8h), TSR-011 demonstrated a favourable safety profile with acceptable QTc changes. Limited clinical activity was observed. Based on the competitive ALK inhibitor landscape and benefit/risk considerations, further TSR-011 development was discontinued. READ ARTICLE
British Journal of Cancer DOI:10.1038/s41416-019-0503-9
Authors: Chia-Chi Lin, Hendrik-Tobias Arkenau, Sharon Lu, Jasgit Sachdev, Javier de Castro Carpeño, Monica Mita, Rafal Dziadziuszko, Wu-Chou Su, Dmitri Bobilev, Lorraine Hughes, Jian Chan, Zhi-Yi Zhang, Glen J. Weiss