SUZHOU, China I October 21, 2024 I CStone Pharmaceuticals (HKEX: 2616), an innovation-driven biopharmaceutical company focused on the research and development of anti-cancer therapies, today announced the patent (WO/2024/208354) for its internally developed antibody-drug conjugate (ADC) CS5006 was published on October 10, 2024.
CS5006 is a first-in-class ADC with a novel therapeutic target – integrin β4 (ITGB4). ITGB4 is a transmembrane protein that pairs exclusively with integrin α6 (ITGA6) to form the heterodimer α6β4, with laminin as its extracellular ligand. ITGB4 is recognized as a biomarker in various cancers, with its overexpression linked to tumor aggressiveness and poor prognosis. Utilizing our internally developed bioinformatics platform, combined with cutting-edge AI algorithms and a comprehensive analysis of published literature, we identified that ITGB4 is highly expressed in non-small cell lung cancer, colorectal cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, etc., making it a promising candidate for targeted therapy.
During the development of CS5006, CStone combined the candidate monoclonal antibody with clinically validated linkers and cytotoxic payloads, including GGFG-DXd and VC-MMAE, to create model ADC molecules for proof-of-concept studies. In vitro studies showed that both CS5006-GGFG-DXd and CS5006-VC-MMAE ADCs efficiently released cytotoxins upon internalization in tumor cells, rapidly inducing cell death. In vivo data further confirmed the potent anti-tumor activity and favorable tolerability of these two ADCs, providing robust support for the next phase of clinical development. CS5006, with an internally developed proprietary linker is approaching completion of its preclinical candidate (PCC) selection, with an Investigational New Drug (IND) application expected in 2025.
Dr. Jason Yang, CEO, President of R&D, and Executive Director at CStone, said, “The publication of the CS5006 patent highlights our innovations in the ADC field and underscores CStone’s end-to-end capabilities from research to commercialization. We are hopeful of the clinical potential of CS5006 and other innovative ADCs in our pipeline, and look forward to bringing groundbreaking therapies to cancer patients worldwide.”
As alluded, CStone is actively advancing the development of next-generation linkers with proprietary IP to enhance the hydrophilicity and tumor selectivity of widely used linkers such as the GGFG tetrapeptide and VA/C dipeptide linkers. These new linkers aim to maximize ADC safety and efficacy, increase compatibility with diverse targets and antibodies, and support multiple upcoming ADC projects in CStone’s pipeline 2.0, including CS5005 targeting SSTR2, CS5006 targeting ITGB4, and CS5007 targeting EGFR/HER3.
About CStone
CStone (HKEX: 2616), established in late 2015, is an innovation-driven biopharmaceutical company focused on the research and development of anti-cancer therapies. Dedicated to addressing patients’ unmet medical needs in China and globally, the Company has made significant strides since its inception. To date, the Company has successfully launched 4 innovative drugs and secured approvals for 15 new drug applications (NDAs) covering 9 indications. The company’s pipeline is balanced by 16 promising candidates, featuring potentially first-in-class or best-in-class antibody-drug conjugates (ADCs), multispecific antibodies, immunotherapies and precision medicines. CStone also prides itself on a management team with comprehensive experiences and capabilities that span the entire drug development spectrum, from preclinical and translational research to clinical development, drug manufacturing, business development, and commercialization.
For more information about CStone, please visit www.cstonepharma.com.
SOURCE: CStone Pharmaceuticals
Post Views: 16
SUZHOU, China I October 21, 2024 I CStone Pharmaceuticals (HKEX: 2616), an innovation-driven biopharmaceutical company focused on the research and development of anti-cancer therapies, today announced the patent (WO/2024/208354) for its internally developed antibody-drug conjugate (ADC) CS5006 was published on October 10, 2024.
CS5006 is a first-in-class ADC with a novel therapeutic target – integrin β4 (ITGB4). ITGB4 is a transmembrane protein that pairs exclusively with integrin α6 (ITGA6) to form the heterodimer α6β4, with laminin as its extracellular ligand. ITGB4 is recognized as a biomarker in various cancers, with its overexpression linked to tumor aggressiveness and poor prognosis. Utilizing our internally developed bioinformatics platform, combined with cutting-edge AI algorithms and a comprehensive analysis of published literature, we identified that ITGB4 is highly expressed in non-small cell lung cancer, colorectal cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, etc., making it a promising candidate for targeted therapy.
During the development of CS5006, CStone combined the candidate monoclonal antibody with clinically validated linkers and cytotoxic payloads, including GGFG-DXd and VC-MMAE, to create model ADC molecules for proof-of-concept studies. In vitro studies showed that both CS5006-GGFG-DXd and CS5006-VC-MMAE ADCs efficiently released cytotoxins upon internalization in tumor cells, rapidly inducing cell death. In vivo data further confirmed the potent anti-tumor activity and favorable tolerability of these two ADCs, providing robust support for the next phase of clinical development. CS5006, with an internally developed proprietary linker is approaching completion of its preclinical candidate (PCC) selection, with an Investigational New Drug (IND) application expected in 2025.
Dr. Jason Yang, CEO, President of R&D, and Executive Director at CStone, said, “The publication of the CS5006 patent highlights our innovations in the ADC field and underscores CStone’s end-to-end capabilities from research to commercialization. We are hopeful of the clinical potential of CS5006 and other innovative ADCs in our pipeline, and look forward to bringing groundbreaking therapies to cancer patients worldwide.”
As alluded, CStone is actively advancing the development of next-generation linkers with proprietary IP to enhance the hydrophilicity and tumor selectivity of widely used linkers such as the GGFG tetrapeptide and VA/C dipeptide linkers. These new linkers aim to maximize ADC safety and efficacy, increase compatibility with diverse targets and antibodies, and support multiple upcoming ADC projects in CStone’s pipeline 2.0, including CS5005 targeting SSTR2, CS5006 targeting ITGB4, and CS5007 targeting EGFR/HER3.
About CStone
CStone (HKEX: 2616), established in late 2015, is an innovation-driven biopharmaceutical company focused on the research and development of anti-cancer therapies. Dedicated to addressing patients’ unmet medical needs in China and globally, the Company has made significant strides since its inception. To date, the Company has successfully launched 4 innovative drugs and secured approvals for 15 new drug applications (NDAs) covering 9 indications. The company’s pipeline is balanced by 16 promising candidates, featuring potentially first-in-class or best-in-class antibody-drug conjugates (ADCs), multispecific antibodies, immunotherapies and precision medicines. CStone also prides itself on a management team with comprehensive experiences and capabilities that span the entire drug development spectrum, from preclinical and translational research to clinical development, drug manufacturing, business development, and commercialization.
For more information about CStone, please visit www.cstonepharma.com.
SOURCE: CStone Pharmaceuticals
Post Views: 16
