Evidence map›Paper›PMID 42396977›Full record

ReviewExpert opinion on therapeutic patents2026

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

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

Abstract readReview
In one paragraph

Review in Expert opinion on therapeutic patents, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors.

Alfie M CaseDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, USA.
Melanie M SmithDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, USA.
Cole A MackDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, USA.
Paul C TrippierDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, USA.

Funding

UNMC/EPPLEY CANCER CENTER SUPPORT GRANTP30CA036727 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI James Eudy · 1985 to 2026
$55.0M
AKR1C Inhibitors as Chemotherapeutic PotentiatorsR01CA226436 · NCI · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI TRIPPIER, PAUL · 2019 to 2023
$2.0M
NCI NIH HHS P30 CA036727NCI NIH HHS R01 CA226436
6 · The paper itself

Abstract

introductionAldo-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.

Indexed as

Aldo-Keto Reductase Family 1 Member C3Antineoplastic AgentsNeoplasmsAnimalsBiomarkers, TumorDrug DevelopmentDrug Resistance, NeoplasmHumansMaleMolecular Targeted TherapyPatents as TopicProteolysis Targeting ChimeraReceptors, AndrogenAKR1C3 protein, humanAldo-Keto Reductase Family 1 Member C3Antineoplastic AgentsBiomarkers, TumorProteolysis Targeting ChimeraReceptors, AndrogenAldo-keto reductaseandrogen receptorbiomarkerbreast cancer, castration-resistant prostate cancernon-small cell lung cancerPROTAC degrader

Identifiers

PMID42396977
PMCPMC13367418

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.