SANTA CLARA, Calif.--(BUSINESS WIRE)--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. The data were presented in a poster at the American Association for Cancer Research Annual Meeting (AACR) being held from April 1 – 5, 2017 in Washington, D.C.
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).
About CBT Pharmaceuticals
CBT Pharmaceuticals is a life
sciences company developing innovative oncology therapeutics targeting
the growth and proliferation of cancer cells. The company is advancing a
pipeline of four development-stage assets including CBT-101, an oral
c-Met inhibitor targeting the epithelial-mesenchymal transition (EMT)
pathway in cancers and CBT-501, a novel humanized monoclonal antibody
targeting the Programmed Death-1 (PD-1) membrane receptor of immune
cells, as well as two investigational products – a preclinical
multi-targeted kinase inhibitor that targets uncontrolled growth
signaling pathways and a novel humanized Programmed Death Ligand-1
(PD-L1) antibody that restores the body’s immune system to recognize and
kill cancer cells. CBT is headquartered in California and has an
Australian subsidiary, CBT Pharmaceuticals (Australia) Pty Ltd to manage
all trials conducted in Australia. For additional information, please
visit: www.cbtpharma.com