P65-047
/ Beactica
- LARVOL DELTA
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March 18, 2026
P65-047, a novel TEAD degrader, overcomes KRAS inhibitor resistance through Hippo pathway disruption in NSCLC
(AACR 2026)
- "Background: Allele-specific KRAS inhibitors (e.g. MRTX849, MRTX1133) show clinical benefit in KRAS-mutant NSCLC but face rapid development of resistance mediated by adaptive YAP/TEAD axis activation. P65-047 displays high efficacy, delivering robust in vivo tumour regression and strong resensitization in vitro, establishing TEAD degradation as a mechanistically validated strategy to overcome acquired resistance in KRAS-mutant NSCLC. These data support clinical advancement of TEAD degraders in patients with allele-specific KRAS inhibitor-refractory disease."
Late-breaking abstract • Lung Cancer • Mesothelioma • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CRBN • KRAS • TP53
March 06, 2024
Degraders of TEAD transcription factors based on interface 3 binders
(AACR 2024)
- "Finally, we performed an unbiased, quantitative high-throughput drug combination screening by combining a TEAD degrader with a library of approximately 2,800 oncology-focused drugs. This research was supported in part by the Intramural/Extramural research program of the NCATS, NIH."
Late-breaking abstract • Mesothelioma • Oncology • Solid Tumor • CCN1 • CRBN • CTGF
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