ensartinib + pralsetinib

Ensartinib + pralsetinib is a combination of two small molecule tyrosine kinase inhibitors used in the treatment of non-small cell lung cancer (NSCLC) with concurrent ALK rearrangement and RET rearrangement. Ensartinib is an oral inhibitor primarily targeting anaplastic lymphoma kinase (ALK), but also exhibits activity against other kinases such as MET. Pralsetinib is a selective inhibitor of the RET receptor tyrosine kinase. This dual-targeted approach addresses resistance mechanisms in NSCLC where both ALK and RET alterations are present. The combination has shown clinical benefit in case reports for patients who developed resistance to single-agent ALK inhibitors due to acquired RET rearrangements[1]. Both drugs are approved individually for specific indications in NSCLC.