期刊
PHARMACEUTICALS
卷 14, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/ph14070632
关键词
Trk; NTRK; tissue-agnostic; larotrectinib; entrectinib; Trk fusion
资金
- National Research Foundation, Government of Korea [2021R1A2C1007790]
- National Research Foundation of Korea [2021R1A2C1007790] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Recently approved Trk inhibitors, larotrectinib and entrectinib, have shown promising results for Trk fusion-positive cancer patients, using a tissue-agnostic development approach to expedite the drug development process. The on-target effects of Trk inhibitors on the central nervous system pose challenges, but a next generation sequencing-based companion diagnostic has been approved for detecting various types of Trk fusions. Through the adoption of tissue-agnostic approach, the development of Trk inhibitors has been accelerated.
Recently, two tropomycin receptor kinase (Trk) inhibitors, larotrectinib and entrectinib, have been approved for Trk fusion-positive cancer patients. Clinical trials for larotrectinib and entrectinib were performed with patients selected based on the presence of Trk fusion, regardless of cancer type. This unique approach, called tissue-agnostic development, expedited the process of Trk inhibitor development. In the present review, the development processes of larotrectinib and entrectinib have been described, along with discussion on other Trk inhibitors currently in clinical trials. The on-target effects of Trk inhibitors in Trk signaling exhibit adverse effects on the central nervous system, such as withdrawal pain, weight gain, and dizziness. A next generation sequencing-based method has been approved for companion diagnostics of larotrectinib, which can detect various types of Trk fusions in tumor samples. With the adoption of the tissue-agnostic approach, the development of Trk inhibitors has been accelerated.
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