Ulixertinib

作者：Ji, N.; Yang, Y.; Chen, Y.^*; Shen, W-X^*; Chen, Z-S

来源：DRUGS OF THE FUTURE, 2021, 46(11): 891-900.

DOI：10.1358/dof.2021.46.11.3328879

• Ulixertinib
• RAS-ERK signaling
• BRAF
• Mitogen-activated protein kinases (MAPKs)
• Drug resistance

Mutations in the RAS-ERK pathways are observed in approximately 33% of tumors expressing a constitutively activated mutant form of RAS and approximately 8% of tumors expressing an activated form of BRAF. Small-molecule agents targeting upstream molecules, including BRAF, are emerging. These include molecules such as sorafenib, vemurafenib, dabrafenib, etc. However, targeting aberrant activation of ERK by RAF inhibitors has also been the topic of extensive investigation over recent decades, which makes ERK a potentially effective target in RAS-ERK-dependent cancers. In this review, we systematically summarize the spectrum of RAS-ERK signaling in human cancers. Specifically, the pharmacological features, and preclinical and clinical studies of ulixertinib as a novel ERK1/2 inhibitor, are summarized and discussed.

• 单位
  南方医科大学; y