Beyond First-Generation KRAS Inhibitors: BBO-8520 Tests the Dual Mechanism Hypothesis

Zhiwei Zhou; Kenneth D. Westover

doi:10.1158/2159-8290.CD-24-1885

Beyond First-Generation KRAS Inhibitors: BBO-8520 Tests the Dual Mechanism Hypothesis

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Abstract

This issue highlights the development of a first-in-class small-molecule covalent KRASG12C inhibitor, BBO-8520, which targets both the active (ON) and inactive (OFF) states of KRAS. This dual-state targeting offers a significant opportunity to overcome the resistance mechanisms that have limited the efficacy of first-generation KRAS inhibitors and addresses critical challenges in KRAS-targeted therapy. See related article by Maciag et al., p. 578.

Original language	English (US)
Pages (from-to)	455-457
Number of pages	3
Journal	Cancer discovery
Volume	15
Issue number	3
DOIs	https://doi.org/10.1158/2159-8290.CD-24-1885
State	Published - Mar 3 2025

ASJC Scopus subject areas

Oncology

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10.1158/2159-8290.CD-24-1885

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abstract = "This issue highlights the development of a first-in-class small-molecule covalent KRASG12C inhibitor, BBO-8520, which targets both the active (ON) and inactive (OFF) states of KRAS. This dual-state targeting offers a significant opportunity to overcome the resistance mechanisms that have limited the efficacy of first-generation KRAS inhibitors and addresses critical challenges in KRAS-targeted therapy. See related article by Maciag et al., p. 578.",

author = "Zhiwei Zhou and Westover, {Kenneth D.}",

note = "Publisher Copyright: {\textcopyright}2025 American Association for Cancer Research.",

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Beyond First-Generation KRAS Inhibitors: BBO-8520 Tests the Dual Mechanism Hypothesis

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