Undisclosed p300-selective degrader / SK Bio - LARVOL DELTA

Late-Breaking Research from SK Life Science Labs at AACR Annual Meeting Shows p300-Selective Degraders are Potent Growth Inhibitors in Models of Aggressive Prostate Cancers and Solid Tumors (PRNewswire) - "SK Life Science Labs...presented late-breaking research at the American Association for Cancer Research (AACR) Annual Meeting 2025 in Chicago. The research identified novel orally bioavailable p300-selective degraders that have therapeutic potential for difficult-to-treat prostate cancer and multiple cancers where the protein CBP is mutated or missing....Targeted p300 degraders demonstrate superb selectivity and potency, inhibiting tumor cell growth across several indications including castrate-resistant prostate cancer and cancers where the related protein, CBP, is missing or mutated. Once daily oral administration of these potent p300-selective degraders in tumor-bearing mice results in rapid degradation of p300 and a significant reduction in tumor growth."

Late-breaking abstract • Preclinical • Castration-Resistant Prostate Cancer

p300-selective degraders illustrate potent anti-tumor activity in a distinct subset of cancers (AACR 2025) - "Once daily oral administration of our compound led to almost complete degradation of p300 within xenograft tumors, resulting in a pronounced inhibition of tumor growth. Lastly, we profiled p300 degradation in human bone marrow derived myeloid progenitor colony-forming assays where we observed a significant reduction in toxicity (IC50 = 4µM) compared to a dual CBP/p300 inhibitor (IC50 = 121nM) or degrader (IC50 = 16nM), supporting the hypothesis that a p300-specific mechanism will offer an improved therapeutic index while maintaining anti-tumor efficacy.Taken together, these results underscore the therapeutic potential of a selective p300 degrader in both castrate-resistant prostate and CBP LoF cancers.SK Life Science Labs Proprietary / Confidential"

Late-breaking abstract • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AR • MYC

SK Biopharmaceuticals’ Proteovant Therapeutics Presents Preclinical Data at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (PRNewswire) - "SK Biopharmaceuticals...and its U.S. R&D subsidiary, Proteovant Therapeutics, presented data showing that selectively degrading the epigenetic protein p300, with minimal impact on its paralog CBP, results in suppression of androgen receptor signaling and inhibition of tumor growth in a mouse model of androgen receptor (AR) positive prostate cancer. Findings are being presented today at the American Association for Cancer Research (AACR), National Cancer Institute (NCI), and the European Organisation for Research and Treatment (EORTC) International Conference on Molecular Targets and Cancer Therapeutics being held in Boston."

Preclinical • Prostate Cancer