AKR1C3 inhibitors and exploiters for the treatment and therapeutic monitoring of cancer: a patent review (2020-present).

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2026-08-01 Epub Date: 2026-07-28 DOI:10.1080/13543776.2026.2699768

Alfie M Case, Melanie M Smith, Cole A Mack, Paul C Trippier

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引用次数: 0

Abstract

Introduction: Aldo-keto reductase 1C3 (AKR1C3) is a drug target for the treatment of various androgen‑dependent malignancies, including castration-resistant prostate cancer as well as hematological cancers. The enzyme plays a key role in the conversion of androgen precursors into potent androgen receptor ligands and the conversion of prostaglandins from pro-differential to pro-proliferative, thereby facilitating the progression of these malignancies. Additionally, AKR1C3 plays a role in chemotherapy resistance, reducing therapeutics to inactive forms and stabilizing the expression of mutant androgen receptors.

Area covered: This article reviews patents published since 2020, obtained from WIPO and SciFinder, covering AKR1C3 inhibitors, compounds that exploit AKR1C3 for prodrug activation, and the use of AKR1C3 expression levels as a biomarker for measuring disease and therapeutic response. In addition to inhibitors, this article reviews the first reported AKR1C3/AR-v7 dual degrader.

Expert opinion: Multiple compounds have been reported to potently and selectively inhibit AKR1C3, eliciting tumor growth inhibition as standalone agents and when used in combination with clinically approved chemotherapeutics. With drug resistance an ever-present issue, exploration of alternative routes for treating malignancies via AKR1C3 targeting offers tremendous potential. Translation to clinical trials and their effect in patients is expected to be revealed in the coming years.

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用于癌症治疗和治疗监测的AKR1C3抑制剂和利用物：2020年至今的专利审查

Aldo-keto reductase 1C3 （AKR1C3）是治疗各种雄激素依赖性恶性肿瘤的药物靶点，包括去势抵抗性前列腺癌和血液学癌症。该酶在雄激素前体转化为强效雄激素受体配体和前列腺素从促分化转化为促增殖中起关键作用，促进这些恶性肿瘤的进展。此外，AKR1C3在化疗耐药中发挥作用，将治疗药物减少到无活性形式，并稳定突变雄激素受体的表达。涵盖领域：本文回顾了自2020年以来从WIPO和SciFinder获得的专利，涵盖AKR1C3抑制剂、利用AKR1C3进行前药激活的化合物，以及使用AKR1C3表达水平作为测量疾病和治疗反应的生物标志物。除抑制剂外，本文还综述了首次报道的AKR1C3/AR-v7双降解剂。专家意见：据报道，多种化合物可作为单独药物或与临床批准的化疗药物联合使用时，有效和选择性地抑制AKR1C3引发的肿瘤生长抑制。由于耐药性是一个一直存在的问题，探索通过AKR1C3靶向治疗恶性肿瘤的替代途径提供了巨大的潜力。转化为临床试验及其对患者的影响预计将在未来几年揭晓。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Expert Opinion on Therapeutic Patents 医学-药学

CiteScore

12.10

自引率

1.50%

发文量

审稿时长

6-12 weeks

期刊介绍： Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.