Rakovina Therapeutics Inc (TSX-V:RKV) presented its research on novel small-molecule inhibitors at the 36th EORTC-NCI-AARC Symposium in Barcelona, Spain this week.
The company’s kt-3000 series, a class of bifunctional small molecules, has shown potent inhibition of both PARP1/2 and HDAC enzymes in preclinical studies.
Rakovina’s dual-function kt-3000 compounds have demonstrated greater efficacy against both HR-deficient and proficient cancer cells.
“These bifunctional PARP+HDAC inhibitors could enable us to effectively address resistance in various cancers while minimizing toxicity associated with traditional combination therapies,” said Jeffrey Bacha, executive chairman of Rakovina Therapeutics.
“We believe these compounds may enable us to target resistance mechanisms in various cancers, while reducing the toxicity typically associated with combination therapies.”
Following the preclinical success, Rakovina plans to explore formulations of the lead compound, kt-3283, to support future human clinical trials. Additionally, the company aims to continue refining the properties of the kt-3000 series through ongoing medicinal chemistry efforts.
Rakovina Therapeutics specializes in DNA-damage response targeting technologies, seeking to address treatment challenges in various forms of cancer.