Entrectinib: A potent new TRK, ROS1, and ALK inhibitor

Francesco Passiglia, Marco Giallombardo, Antonio Russo, Ignacio Gil-Bazo, Marc Peeters, Antonio Russo, Francesco Passiglia, Marco Giallombardo, Rossana Ruiz, Christian Rolfo, Luis Raez, Elisa Giovannetti, Christian Diego Rolfo

Risultato della ricerca: Articlepeer review

87 Citazioni (Scopus)


Introduction: Receptor tyrosine kinases (RTKs) and their signaling pathways, control normal cellular processes; however, their deregulation play important roles in malignant transformation. In advanced non-small cell lung cancer (NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the development of molecularly targeted agents that only benefit roughly 20% of patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent anti-neoplastic activity and tolerability in various neoplastic conditions, particularly NSCLC.Areas covered: This review outlines the pharmacokinetics, pharmacodynamics, mechanism of action, safety, tolerability, pre-clinical studies and clinical trials of entrectinib, a promising novel agent for the treatment of advanced solid tumors with molecular alterations of Trk-A, B and C, ROS1 or ALK.Expert opinion: Among the several experimental drugs under clinical development, entrectinib is emerging as an innovative and promising targeted agent. The encouraging antitumor activity reported in the Phase 1 studies, together with the acceptable toxicity profile, suggest that entrectinib, thanks to its peculiar mechanism of action, could play an important role in the treatment-strategies of multiple TRK-A, B, C, ROS1, and ALK- dependent solid tumors, including NSCLC and colorectal cancer. That being said, further evidence for its clinical use is still needed.
Lingua originaleEnglish
pagine (da-a)1493-1500
Numero di pagine8
RivistaExpert Opinion on Investigational Drugs
Stato di pubblicazionePublished - 2015

All Science Journal Classification (ASJC) codes

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  • ???subjectarea.asjc.2700.2736???


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