ADT-1004: a first-in-class, oral pan-RAS inhibitor with robust antitumor activity in preclinical models of pancreatic ductal adenocarcinoma.

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Tác giả: Mehmet Akce, Asfar S Azmi, Sejong Bae, Dhana Sekhar Reddy Bandi, Kristy L Berry, Michael R Boyd, Donald J Buchsbaum, Julienne L Carstens, Xi Chen, Bassel F El-Rayes, Yu-Hua D Fang, Jeremy B Foote, Greg Gorman, Emily C Graff, Adam B Keeton, Upender Manne, Yulia Y Maxuitenko, Ganji Purnachandra Nagaraju, Gary A Piazza, Sujith Sarvesh, Jacob Valiyaveettil, Karina J Yoon

Ngôn ngữ: eng

Ký hiệu phân loại: 978.02 1800–1899

Thông tin xuất bản: England : Molecular cancer , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 711850

BACKGROUND: Oncogenic KRAS mutations occur in nearly, 90% of patients with pancreatic ductal adenocarcinoma (PDAC). Targeting KRAS has been complicated by mutational heterogeneity and rapid resistance. We developed a novel pan-RAS inhibitor, ADT-1004 (an oral prodrug of ADT-007) and evaluated antitumor activity in murine and human PDAC models. METHODOLOGY: Murine PDAC cells with KRAS RESULTS: ADT-1004 potently blocked tumor growth and RAS activation in mouse PDAC models without discernable toxicity with target engagement and reduced activated RAS and ERK phosphorylation. In addition, ADT-1004 suppressed tumor growth in PDX PDAC models with KRAS CONCLUSION/SIGNIFICANCE: ADT-1004 has strong antitumor activity in aggressive and clinically relevant PDAC models with unique selectivity to block RAS-mediated signaling in RAS mutant cells. As a pan-RAS inhibitor, ADT-1004 has broad activity and potential efficacy advantages over allele-specific KRAS inhibitors. These findings support clinical trials of ADT-1004 for KRAS mutant PDAC.
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