Evidence map›Paper›PMID 32456317›Full record

ReviewMolecules (Basel, Switzerland)2020

Second-Generation Androgen Receptor Antagonists as Hormonal Therapeutics for Three Forms of Prostate Cancer.

Pravien Rajaram, Alyssa Rivera, Kevin Muthima, Nicholas Olveda, Hubert Muchalski, Qiao-Hong Chen

Open access · goldAbstract readReview
In one paragraph

Review in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
4.2field-weighted citation impact, top 4% of its field
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

24 citing papers in PubMed, 57 citations in OpenAlex.

  1. Article
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  7. Article
  8. Review
  9. Review
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  11. Article
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  13. Review
  14. Constitutively Active Androgen Receptor in Hepatocellular Carcinoma.International journal of molecular sciences · 2022
    Review
  15. Synthesis and biological evaluation of niclosamide PROTACs.Bioorganic & medicinal chemistry letters · 2022
    Article
  16. Article
  17. Review
  18. Review
  19. Observational
  20. Article
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

6 authors at 1 institution in 1 country.

Pravien RajaramDepartment of Chemistry, California State University, Fresno, CA 93740, USA.
Alyssa RiveraDepartment of Chemistry, California State University, Fresno, CA 93740, USA.
Kevin MuthimaDepartment of Chemistry, California State University, Fresno, CA 93740, USA.
Nicholas OlvedaDepartment of Chemistry, California State University, Fresno, CA 93740, USA.
Hubert MuchalskiDepartment of Chemistry, California State University, Fresno, CA 93740, USA.ORCID 0000-0002-9507-0081
Qiao-Hong ChenDepartment of Chemistry, California State University, Fresno, CA 93740, USA.ORCID 0000-0001-6753-1824
California State University, Fresno · US

Funding

Introduction to Quantitative Genomic Analysis - A CUREs ApproachR25GM131956 · NIGMS · CALIFORNIA STATE UNIVERSITY FRESNO · PI KRISHNAN, VISWANATHAN V · 2019 to 2023
$2.5M
Fresno State and UC Merced Bridges to the Doctorate Program in Biomedical and Behavioral SciencesR25GM115293 · NIGMS · CALIFORNIA STATE UNIVERSITY FRESNO · PI KRISHNAN, VISWANATHAN V, LIWANG, ANDY · 2015 to 2019
$1.2M
Development of Stabilized Zampanolide Mimics as Chemotherapeutics for Prostate CancerSC2GM121185 · NIGMS · CALIFORNIA STATE UNIVERSITY FRESNO · PI CHEN, QIAOHONG · 2017 to 2019
$420k
NIGMS NIH HHS R25 GM115293NIGMS NIH HHS R25 GM131956NIGMS NIH HHS SC2 GM121185NIH HHS R25GM115293NIH HHS R25GM131956NIH HHS SC2GM121185
6 · The paper itself

Abstract

Enzalutamide is the first second-generation nonsteroidal androgen receptor (AR) antagonist with a strong binding affinity to AR. Most significantly, enzalutamide can prolong not only overall survival time and metastatic free survival time for patients with lethal castration-resistant prostate cancer (CRPC), but also castration-resistant free survival time for patients with castration-sensitive prostate cancer (CSPC). Enzalutamide has thus been approved by the US Food and Drug Administration (FDA) for the treatment of both metastatic (in 2012) and non-metastatic (in 2018) CRPC, as well as CSPC (2019). This is an inspiring drug discovery story created by an amazing interdisciplinary collaboration. Equally important, the successful clinical use of enzalutamide proves the notion that the second-generation AR antagonists can serve as hormonal therapeutics for three forms of advanced prostate cancer. This has been further verified by the recent FDA approval of the other two second-generation AR antagonists, apalutamide and darolutamide, for the treatment of prostate cancer. This review focuses on the rational design and discovery of these three second-generation AR antagonists, and then highlights their syntheses, clinical studies, and use. Strategies to overcome the resistance to the second-generation AR antagonists are also reviewed.

Indexed as

Androgen Receptor AntagonistsBenzamidesDrug Resistance, NeoplasmHumansMaleNitrilesPhenylthiohydantoinProstatic NeoplasmsProstatic Neoplasms, Castration-ResistantPyrazolesReceptors, AndrogenSignal TransductionThiohydantoinsAndrogen Receptor AntagonistsapalutamideBenzamidesdarolutamideenzalutamideNitrilesPhenylthiohydantoinPyrazolesReceptors, AndrogenThiohydantoinsandrogen receptorapalutamidedarolutamideenzalutamideprostate cancer

Identifiers

PMID32456317
PMCPMC7287767
OpenAlexW3027456845

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

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.