The Development of AXL Inhibitors in Lung Cancer: Recent Progress and Challenges

Yun Beom Sang, Joo Hang Kim, Chang Gon Kim, Min Hee Hong, Hye Ryun Kim, Byoung Chul Cho, Sun Min Lim

Research output: Contribution to journalReview articlepeer-review

6 Citations (Scopus)


AXL, along with MER and TYRO3, is a receptor tyrosine kinase from the TAM family. Although AXL itself is not thought to be a potent oncogenic driver, overexpression of AXL is known to trigger tumor cell growth, survival, invasion, metastasis, angiogenesis, epithelial to mesenchymal transition, and immune suppression. Overexpression of AXL is associated with therapy resistance and poor prognosis. Therefore, it is being studied as a marker of prognosis in cancer treatment or as a target in various cancer types. Recently, many preclinical and clinical studies on agents with various mechanisms targeting AXL have been actively conducted. They include small molecule inhibitors, monoclonal antibodies, and antibody-drug conjugates. This article reviewed the fundamental role of AXL in solid tumors, and the development in research of AXL inhibitors in recent years. Emphasis was placed on the function of AXL in acquired therapy resistance in patients with non-small cell lung cancer (NSCLC). Since clinical needs increase in NSCLC patients with acquired resistance after initial therapy, recent research efforts have focused on a combination treatment with AXL inhibitors and tyrosine kinase inhibitors or immunotherapy to overcome resistance. Lastly, we deal with challenges and limitations encountered in the development of AXL inhibitors.

Original languageEnglish
Article number811247
JournalFrontiers in Oncology
Publication statusPublished - 2022 Mar 3

Bibliographical note

Funding Information:
This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2019R1A2C4069993) to SL.

Publisher Copyright:
Copyright © 2022 Sang, Kim, Kim, Hong, Kim, Cho and Lim.

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research


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