在临床前模型中鉴定 LSD1 抑制剂 bomedemstat 的结构、生物化学、药代动力学和药效学特性

The Prostate Pub Date : 2024-04-15 DOI:10.1002/pros.24707

Sumer Jasmine, Adel Mandl, Timothy E. G. Krueger, Susan L. Dalrymple, Lizamma Antony, Jennifer Dias, Cassandra A. Celatka, Amy E. Tapper, Maria Kleppe, Mayuko Kanayama, Yuezhou Jing, Valentina Speranzini, Yuzhuo Z. Wang, Jun Luo, Bruce J. Trock, Samuel R. Denmeade, Michael A. Carducci, Andrea Mattevi, Hugh Y. Rienhoff, John T. Isaacs, W. Nathaniel Brennen

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引用次数: 0

摘要

赖氨酸特异性去甲基化酶1（LSD1）正在成为转移性去势抵抗性前列腺癌（mCRPC）肿瘤进展的关键介质。神经内分泌性前列腺癌（NEPC）越来越被认为是雄激素受体轴靶向疗法失败的mCRPC患者的一种适应性耐药机制。要确定前列腺癌模型中的抗肿瘤反应，必须使用安全有效的 LSD1 抑制剂。为此，我们研究了 LSD1 抑制剂 bomedemstat 的特性，以评估其在 NEPC 及其他 mCRPC 病理亚型中的临床潜力。

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Characterization of structural, biochemical, pharmacokinetic, and pharmacodynamic properties of the LSD1 inhibitor bomedemstat in preclinical models

Lysine-specific demethylase 1 (LSD1) is emerging as a critical mediator of tumor progression in metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine prostate cancer (NEPC) is increasingly recognized as an adaptive mechanism of resistance in mCRPC patients failing androgen receptor axis-targeted therapies. Safe and effective LSD1 inhibitors are necessary to determine antitumor response in prostate cancer models. For this reason, we characterize the LSD1 inhibitor bomedemstat to assess its clinical potential in NEPC as well as other mCRPC pathological subtypes.

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The Prostate

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