On April 4, 2017 CBT Pharmaceuticals, Inc. (CBT), a life sciences company focused on developing innovative oncology therapeutics, presented preclinical data on CBT-101 (bozitinib, PLB-1001, CBI-3103), a highly specific small molecule inhibitor of c-MET receptor tyrosine kinase, demonstrating its selectivity, safety, and efficacy in suppressing tumor growth in lung, gastric, hepatic and pancreatic human primary tumor models (Press release, CBT Pharmaceuticals, APR 4, 2017, View Source [SID1234518475]). The data were presented in a poster at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting (AACR) (Free AACR Whitepaper) being held from April 1 – 5, 2017 in Washington, D.C.

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Presentation Highlights:

CBT-101 inhibited c-MET activation in a range of human primary cancer cell lines.
CBT-101 inhibited in vivo dephosphorylation of c-MET in a dose-dependent manner in a human gastric cancer model.
CBT-101 demonstrated improved tumor growth inhibition as compared to other selective c-MET agents in lung, gastric, hepatic, and pancreatic cancer models.
"These preclinical data support our commitment to advancing the clinical development of bozitinib as a targeted therapy for c-MET dysregulated tumors," said Sanjeev Redkar, Ph.D., President and Chief Executive Officer of CBT Pharmaceuticals. "Based on these promising findings, we plan to submit an Investigational New Drug Application soon and initiate a Phase 1 dose escalation and dose and disease expansion study in 2017."

Bozitinib (CBT-101)

Bozitinib is an orally available tyrosine kinase inhibitor that is expected to potently target tumors in patients with c-MET driver alterations (amplification and mutation) that occur in varying percentages across a variety of tumor types, including, but not limited to, breast, colorectal, gastric, gliomas, head and neck, hepatocellular, lung, ovarian as well as hematologic malignancies. MET is a receptor tyrosine kinase located on the cell surface and is activated by the binding of its ligand, hepatocyte growth factor (HGF). MET activates a variety of signaling pathways within the cell, and in normal circumstances, is involved in embryonic development and wound healing. However, in cancer cells, MET can be aberrantly active and cause abnormal signaling, which leads to tumor growth, angiogenesis, and metastasis. CBT-101 has demonstrated high-affinity to MET irrespective of hepatocye growth factor (HGF) dependency and excellent activity in preclinical models of human cancer. CBT-101 was developed by Crown Bioscience. Beijing Pearl Biotechnology owns development and commercialization rights in People’s Republic of China. CBT retains rest of the world (ROW) rights. An investigational new drug application has been approved by the China Food and Drug Administration (CFDA), and two Phase 1 trials are ongoing in China – non-small cell lung cancer (NSCLC) (NCT02896231) and high grade gliomas with PTPRZ1-MET fusion gene (NCT02978261).