On September 18,2017 Karus Therapeutics Ltd (‘Karus’), a leader in the design and development of innovative medicines with breakthrough potential in the treatment of cancer, reported that the first patients have been dosed with its histone deacetylase 6 (HDAC6) inhibitor, KA2507, in a Phase I clinical study (Press release, Karus Therapeutics, SEP 18, 2017, View Source [SID1234520560]). This is the Company’s second orally-active small molecule cancer therapeutic agent to enter clinical trials during the past 12 months.
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This Phase I study has been designed to assess the safety, tolerability, pharmacokinetic and pharmacodynamic profiles of KA2507 in patients with PD-L1-expressing solid tumors. The trial is being conducted at the University of Texas MD Anderson Cancer Center in Houston, Texas, USA, and is part of a collaboration between the two organizations.
KA2507 is a highly-selective and potent inhibitor of the tubulin deacetylase, HDAC6. Selective inhibition of this enzyme confers a cancer immunotherapeutic response by regulating immune checkpoint markers within the tumor microenvironment. HDAC6 has also emerged as a potentially important therapeutic target due to its overexpression in solid tumors and its role in specific mutant-harboring cancers. Karus considers KA2507 to hold broad therapeutic potential for the treatment of solid tumors, as both a single agent and in combination with other drugs.
Stephen Shuttleworth – COO, CSO and founding scientist of Karus’s R&D programs – commented: "KA2507 is Karus’s second small molecule cancer therapeutic agent designed in our laboratories to enter Phase I trials within the last year, and the commencement of this clinical study represents another significant milestone for the Company. HDAC6 is an exciting new target in cancer, and KA2507 is the product of many years’ research and development. The drug has the potential to be a best-in-class agent, and represents another major step in our mission towards the development of new life-changing therapies for cancer patients."
Apostolia Tsimberidou MD, PhD, Professor in the Department of Investigational Cancer Therapeutics at the MDACC is the Principal Investigator for the clinical study.