Drug candidate active against EGFR and KRAS mutant lung cancer cell lines
Fort Collins, CO, June xx, 2020 – Cetya Therapeutics, Inc. today announced issuance of US Patent No. 10,676,504 and Australian Patent No. 2016229324 covering CT-102, Cetya’s proprietary HDAC inhibitor. CT-102 has demonstrated excellent activity in vitro against difficult to treat lung cell lines. As no HDAC inhibitor is yet approved for treatment of any solid tumor, CT-102 has a different mechanism of action to existing therapies and is thus a good candidate to include in combinatorial approaches to treatment of these resistant subtypes of lung cancer. Gene expression analysis has been performed on these cell lines with and without treatment with CT-102 to better understand why CT-102 is showing sub-micromolar single agent activity in these growth inhibition assays. CT-102 was seen to alter the expression of genes in important oncogenic pathways related to Check 1 and Wnt inhibitors.
“These patents solidify Cetya’s position as a leader in novel HDAC inhibitor chemistry, potentially opening up new therapies for treatment-resistant solid tumors such as KRAS mutant and EGFR mutant lung cancer.”
Cliff Hendrick, CEO, Cetya
The tumor cell lines in use at CU Anschutz were originally grown from primary or metastatic tumor specimens surgically removed from patients with these treatment-resistant lung cancer subtypes. CT- 102 exhibited nanomolar activity against cell lines derived from human lung adenocarcinoma harboring the KRAS mutation, cell lines harboring the epidermal growth factor receptor (EGFR) mutation, against wild type (no KRAS or EGFR mutation) human adenocarcinoma and human squamous cell carcinoma, and against a p53 deficient cell line. CT-102 exhibited synergistic effects when combined with an EGFR inhibitor in the EGFR mutant cell lines. “The strong cytotoxic activity observed with CT-102 is all the more compelling given the lineage of these tumor lines” stated Dr. Samir E. Witta, newly appointed Chair of Cetya’s Scientific Advisory Board. Future work will look at combination therapies and explore in more depth the results of the gene expression analysis following exposure of these tumor lines to CT-102.
“These patents solidify Cetya’s position as a leader in novel HDAC inhibitor chemistry, potentially opening up new therapies for treatment-resistant solid tumors such as KRAS mutant and EGFR mutant lung cancer”, Cliff Hendrick, CEO of Cetya, stated. “The activity of CT-102 against these difficult to treat lung cancer subtypes is very encouraging and warrants additional investigation with this high potency, Class I- restricted HDAC inhibitor.”
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. Robert M. Williams at CSU. Cetya has a portfolio of analogs, including CT-102, to evaluate in solid tumor indications and has selected a lead candidate for treatment of 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