Progress and challenges in RET-targeted cancer therapy
Xueqing Hu , Ujjwol Khatri , Tao Shen , and Jie Wu, at University of Oklahoma Health Sciences Center, USA, provides a comprehensive review of the role of the RET (REarranged during Transfection) receptor tyrosine kinase in cancer development and the advancements in RET-targeted cancer therapies. RET, a transmembrane receptor tyrosine kinase, plays a crucial role in various cellular processes, including embryogenesis and cell development. However, when aberrantly activated due to mutations or chromosomal rearrangements, RET can act as an oncogenic driver in many cancers, notably non-small cell lung cancer (NSCLC). The review discusses the early trials of multikinase tyrosine kinase inhibitors (TKIs) that were initially used to treat RET-altered thyroid cancer and NSCLC, with limited success. The development of more potent and selective RET TKIs, such as pralsetinib and selpercatinib, marked a significant advancement in RET-targeted therapy. These drugs…


