Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis.

doi:10.1158/0008-5472.CAN-21-4152

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Article

Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis.

Cancer research - 18 Jul 2022

Bonfill-Teixidor Ester, Iurlaro Raffaella, Handl Cornelia, Wichmann Jürgen, Arias Alexandra, Cuartas Isabel, Emmenegger Jasmin, Romagnani Andrea, Mangano Luca, Lorber Thomas, Berrera Marco, Godfried Sie Christina, Köchl Fabian, Eckmann Jan, Feddersen Romi, Kornacker Martin, Schnetzler Gabriel, Cicuendez Marta, Cordero Esteban, Topczewski Thomaz E, Ferres-Pijoan Abel, González Josep, Martínez-Ricarte Francisco, Muñoz-Couselo Eva, Tabernero Josep, Bischoff James R, Pettazzoni Piergiorgio, Seoane Joan

Abstract excerpt

The therapeutic benefit of approved BRAF and MEK inhibitors (BRAFi/MEKi) in patients with brain metastatic BRAF V600E/K-mutated melanoma is limited and transient. Resistance largely occurs through the restoration of MAPK signaling via paradoxical BRAF activation, highlighting the need for more effective therapeutic options. Aiming to address this clinical challenge, we characterized the activity of a potent,...

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Identifiers

PMID: 35584009
DOI: 10.1158/0008-5472.CAN-21-4152

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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