On October 25, 2024 Rakovina Therapeutics Inc. (TSX-V: RKV) ("Rakovina" or the "Company"), a biopharmaceutical company committed to advancing new cancer therapies based on novel DNA-damage response targeting technologies, reported the presentation of its research on novel small-molecule bifunctional inhibitors of PARP1/2 and HDAC enzymes at the 36th EORTC-NCI-AARC Symposium in Barcelona, Spain, on October 25, 2024 (Press release, Rakovina Therapeutics, OCT 25, 2024, View Source;utm_medium=rss&utm_campaign=rakovina-therapeutics-to-present-research-highlighting-small-molecule-bifunctional-inhibitors-of-parp1-2-and-hdac-enzymes-at-the-36th-eortc-nci-aacr-symposium-in-barcelona-spain [SID1234647423]).
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Rakovina’s novel class of bifunctional small molecule compounds, known as the kt-3000 series, has demonstrated potent dual inhibition of PARP1/2 and HDAC enzymes in preclinical studies. Compared to single-function inhibitors such as olaparib (PARP) and vorinostat (HDAC), dual-function kt-3000 compounds demonstrate greater potency against both HR-deficient and proficient cancer cells.
Based on these results, the Company intends to explore formulations of the lead compound, kt-3283, to support potential advancement to human clinical trials, while continuing to further medicinal chemistry efforts that refine properties of the class.
"The kt-3000 series represents a significant advancement toward overcoming treatment resistance to first-generation PARP-inhibitors. These bifunctional PARP+HDAC inhibitors could enable us to effectively address resistance in various cancers while minimizing toxicity associated with traditional combination therapies," said Rakovina Therapeutics Executive Chairman Jeffrey Bacha.
"We are excited to present our findings at the symposium and to continue advancing these promising compounds toward clinical development," he added.
Presentation Details:
Title: Small-molecule bifunctional inhibitors of PARP1/2 and HDAC enzymes
Presentation Date: October 25, 2024
Abstract Number: 338