Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity. RXDX-101 has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. PXDX-101 is currently in clinical trials, and is being developed by Ignyta.
Reference: Menichincheri, Maria; Ardini, Elena; Magnaghi, Paola; Avanzi, Nilla; Banfi, Patrizia; Bossi, Roberto; Buffa, Laura; Canevari, Giulia; Ceriani, Lucio; Colombo, Maristella; Corti, Luca; Donati, Daniele; Fasolini, Marina; Felder, Eduard; Fiorelli, Claudio; Fiorentini, Francesco; Galvani, Arturo; Isacchi, Antonella; Borgia, Andrea Lombardi; Marchionni, Chiara; Nesi, Marcella; Orrenius, Christian; Panzeri, Achille; Pesenti, Enrico; Rusconi, Luisa; Saccardo, Maria Beatrice; Vanotti, Ermes; Perrone, Ettore; Orsini, Paolo. Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. Journal of Medicinal Chemistry. Volume 59. Issue 7. Pages 3392-3408. Journal; Online Computer File. (2016).
Menichincheri, Maria; Ardini, Elena; Magnaghi, Paola; Avanzi, Nilla; Banfi, Patrizia; Bossi, Roberto; Buffa, Laura; Canevari, Giulia; Ceriani, Lucio; Colombo, Maristella; Corti, Luca; Donati, Daniele; Fasolini, Marina; Felder, Eduard; Fiorelli, Claudio; Fiorentini, Francesco; Galvani, Arturo; Isacchi, Antonella; Borgia, Andrea Lombardi; Marchionni, Chiara; Nesi, Marcella; Orrenius, Christian; Panzeri, Achille; Pesenti, Enrico; Rusconi, Luisa; Saccardo, Maria Beatrice; Vanotti, Ermes; Perrone, Ettore; Orsini, Paolo. Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. Journal of Medicinal Chemistry. Volume 59. Issue 7. Pages 3392-3408. Journal; Online Computer File. (2016).
Reference: Wang, Yihan; Li, Huanyin. Indazole compounds for inhibiting kinase activity, their composition and application in field of medical technology. Assignee Shenzhen TargetRx Biomedical Co., Ltd., Peop. Rep. China. CN 108623576. (2018).
Wang, Yihan; Li, Huanyin. Indazole compounds for inhibiting kinase activity, their composition and application in field of medical technology. Assignee Shenzhen TargetRx Biomedical Co., Ltd., Peop. Rep. China. CN 108623576. (2018).
Lombardi Borgia, Andrea; Menichincheri, Maria; Orsini, Paolo; Panzeri, Achille; Perrone, Ettore; Vanotti, Ermes; Nesi, Marcella; Marchionni, Chiara. Preparation of substituted indazole derivatives for use as kinase inhibitors (Assignee Nerviano Medical Sciences S.r.l., Italy) WO 2009013126 (2009).
