Despite the proven benefits of antibody-based therapies for HER2-amplified cancers, there remains an urgent need for novel therapeutic approaches to combat acquired and innate drug resistance. Here, O'Brien and colleagues demonstrate that tucatinib, a small molecule inhibitor of HER2, has selective activity in HER2-driven cancers. Tucatinib showed single agent and combined efficacy with trastuzumab and inhibitors of CDK4/6 in cell line xenograft models. The selective nature of tucatinib make it an ideal combination partner for HER2-based therapies. Data presented here provide insight into the optimal patient selection and combination strategies for the expanded clinical development of tucatinib.

Head and neck squamous cell carcinoma (HNSCC) is a common cancer with limited treatment options. Recent clinical trials in patients with HRAS-mutant HNSCC have shown the efficacy of tipifarnib, a farnesyl transferase inhibitor (FTI) that blocks a required posttranslational modification of HRAS and other proteins. Here, Javaid and colleagues have validated HRAS as...

You do not currently have access to this content.