生物活性

• 描述LOXO-101 is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03213704	Advanced Malignant Solid Neopl... more >>asm Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma Malignant Glioma NTRK1 Fusion Positive NTRK2 Fusion Positive NTRK3 Fusion Positive Recurrent Central Nervous System Neoplasm Recurrent Childhood Ependymoma Recurrent Childhood Malignant Germ Cell Tumor Recurrent Childhood Medulloblastoma Recurrent Childhood Non-Hodgkin Lymphoma Recurrent Childhood Rhabdomyosarcoma Recurrent Childhood Soft Tissue Sarcoma Recurrent Ewing Sarcoma Recurrent Glioma Recurrent Hepatoblastoma Recurrent Langerhans Cell Histiocytosis Recurrent Malignant Solid Neoplasm Recurrent Neuroblastoma Recurrent Osteosarcoma Recurrent Peripheral Primitive Neuroectodermal Tumor Refractory Central Nervous System Neoplasm Refractory Childhood Malignant Germ Cell Tumor Refractory Langerhans Cell Histiocytosis Refractory Malignant Solid Neoplasm Refractory Neuroblastoma Refractory Non-Hodgkin Lymphoma Rhabdoid Tumor Stage III Osteosarcoma AJCC v7 Stage III Soft Tissue Sarcoma AJCC v7 Stage IV Osteosarcoma AJCC v7 Stage IV Soft Tissue Sarcoma AJCC v7 Stage IVA Osteosarcoma AJCC v7 Stage IVB Osteosarcoma AJCC v7 Wilms Tumor Collapse <<	Phase 2	Recruiting	September 30, 2024	-
  NCT03025360	-	-	-	-	-
  NCT02576431	Carcinoma, Non-Small-Cell Lung... more >> Thyroid Neoplasms Sarcoma Colorectal Neoplasms Salivary Gland Neoplasms Biliary Tract Neoplasms Brain Neoplasm, Primary Carcinoma, Ductal, Breast Melanoma Solid Tumors Glioblastoma Bile Duct Neoplasms Astrocytoma Head and Neck Squamous Cell Carcinoma Pontine Glioma Pancreatic Neoplasms Ovarian Neoplasms Carcinoma, Renal Cell Cholangiocarcinoma Carcinoma Carcinoma, Bronchogenic Bronchial Neoplasms Lung Neoplasms Respiratory Tract Neoplasms Thoracic Neoplasms Neoplasms, Nerve Tissue Nevi and Melanomas Collapse <<	Phase 2	Recruiting	December 2019	-

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• 参考文献

• [1] Nagasubramanian R, Wei J, et al. Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101. Pediatr Blood Cancer. 2016 Aug;63(8):1468-70.

  [2] Doebele RC, Davis LE, et al. An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101. Cancer Discov. 2015 Oct;5(10):1049-57.