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Comment
. 2024 Apr 1;30(7):1217-1219.
doi: 10.1158/1078-0432.CCR-23-3571.

From Serendipity to Intention: Development of Brain-Penetrant PARP1-Selective Inhibitors

Filipa Lynce  1   2   3 , Nancy U Lin  1   2
Affiliations
Comment

From Serendipity to Intention: Development of Brain-Penetrant PARP1-Selective Inhibitors

Filipa Lynce et al. Clin Cancer Res. .

Abstract

Primary and secondary brain tumors cause significant mortality and constitute an important unmet need. The development of AZD9574, a brain-penetrant, PARP1-selective inhibitor with favorable pharmacologic properties and intriguing preclinical activity, has led to an ongoing clinical trial evaluating it alone and in combination with temozolomide or antibody drug conjugates. See related article by Staniszewska et al., p. 1338.

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Comment on

  • Preclinical Characterization of AZD9574, a Blood-Brain Barrier Penetrant Inhibitor of PARP1.
    Staniszewska AD, Pilger D, Gill SJ, Jamal K, Bohin N, Guzzetti S, Gordon J, Hamm G, Mundin G, Illuzzi G, Pike A, McWilliams L, Maglennon G, Rose J, Hawthorne G, Cortes Gonzalez M, Halldin C, Johnström P, Schou M, Critchlow SE, Fawell S, Johannes JW, Leo E, Davies BR, Cosulich S, Sarkaria JN, O'Connor MJ, Hamerlik P. Staniszewska AD, et al. Clin Cancer Res. 2024 Apr 1;30(7):1338-1351. doi: 10.1158/1078-0432.CCR-23-2094. Clin Cancer Res. 2024. PMID: 37967136

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