Novel Chemistry Allows Conjugation of Largazole Analogs to Receptor Ligands or Other Cytotoxic Agents
Fort Collins, CO, January 21, 2020 – Cetya Therapeutics, Inc. today announced issuance of US Patent No. 10,538,534 covering Cetya’s novel ability to conjugate receptor ligands or other cytotoxic agents to its unique HDAC inhibitors, creating targeted and dual-acting anticancer compounds. This specific targeting capability represents a novel approach to broadening the therapeutic window for these highly potent compounds.
Delivering a therapeutic agent to a specific cell type or organ is an emerging strategy using established methodology to improve the risk/benefit ratio for drug therapy, providing specific targeting to provide clinical benefit while avoiding damaging exposure to normal tissues. A conjugate of folic acid or its analog methotrexate with Cetya’s compound CT-101 can specifically target tumor tissues utilizing the folate receptor, which is typically found in high levels on tumor cell surfaces. Active transport of the conjugate across the tumor cell membrane ensues, followed by cleavage of the conjugate into its component parts by enzymes in the tumor cell. In the case of a methotrexate conjugate, this approach effectively delivers both a potent HDAC inhibitor and methotrexate, a mainstay of solid tumor therapy, to the tumor cells. A 1000- fold increase in potency has been noted during in vitro studies with this dual-acting compound with selective folate-receptor targeting.
“This patent solidifies Cetya’s position as a leader in novel HDAC inhibitor chemistry”
Robert M. Williams, PhD, Founder, Cetya Therapeutics
“This patent solidifies Cetya’s position as a leader in novel HDAC inhibitor chemistry, opening up a new approach to therapy with these exciting compounds”, stated Dr. Robert M. Williams, Cetya’s Founding Scientist and University Distinguished Professor of Chemistry at Colorado State University (CSU). Cetya’s proprietary conjugation chemistry represents an exciting opportunity to mitigate dose-limiting toxicities and serious adverse events that have plagued HDAC inhibitor drug development. Cliff Hendrick, CEO of Cetya stated, “The concept of targeting a small molecule drug to a target organ or cell type is an established strategy for managing off-target side effects, and this patent demonstrates Cetya’s capability to employ that strategy to great effect with highly Class-I-selective HDAC inhibitors.”
About Cetya Therapeutics
Cetya Therapeutics, Inc. is a development stage pharmaceutical company developing histone deacetylase inhibitors structurally based on the marine natural product Largazole. Cetya has the exclusive worldwide rights to the histone deacetylase (HDAC) inhibitor platform and patent estate developed in the laboratory of Dr. Williams at CSU, with co-inventors Dr. James E. Bradner, formerly of the Dana-Farber Cancer Research Institute and Harvard Medical School and Prof. Olaf G. Wiest of the University of Notre Dame. Cetya has a portfolio of analogs to evaluate for selection of a lead candidate for each of the therapeutic indications under study, both in oncology and in hemoglobin disorders such as sickle cell disease. Cetya is seeking corporate partners to assist in the advancement of its analog portfolio in a number of different therapeutic indications. For more information on Cetya, please visit our website at www.cetyatherapeutics.com or contact Cliff Hendrick at chendrick@cetya-therapeutics.com