AR-LDD
- Generic Name
- AR-LDD
BMS-986365, a First-in-Class AR Degrader, Shows Promise in Castration-Resistant Prostate Cancer
• BMS-986365 is a novel, orally bioavailable androgen receptor ligand-directed degrader with a dual mechanism of action, degrading and competitively inhibiting the androgen receptor.
• Phase I/II trial data reveals promising efficacy, particularly in patients without prior chemotherapy, showing a median radiographic progression-free survival (rPFS) of 16.5 months.
• The drug demonstrates activity against both wild-type and mutant AR, suggesting potential to overcome resistance to AR pathway inhibitors in castration-resistant prostate cancer.
• The treatment was generally well-tolerated, with manageable side effects like QTC prolongation, offering a new option for patients progressing on prior AR-targeted therapies.
BridgeBio's BBO-8520: A Novel KRAS(G12C) Inhibitor Shows Promise in NSCLC
• BridgeBio's BBO-8520 is a selective, covalent KRAS(G12C) inhibitor designed to target the 'ON' state of the protein, potentially enhancing clinical efficacy.
• Presented at the 2024 AACR Annual Meeting, BBO-8520 is currently undergoing a Phase I trial in patients with advanced non-small-cell lung cancer (NSCLC).
• Preclinical data suggests that BBO-8520 may overcome resistance to existing KRAS(G12C) inhibitors, offering a new therapeutic avenue for KRAS(G12C)-driven cancers.
Drug Development Updates
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