Evidence map›Paper›PMID 34843005›Full record

ArticleInvestigational new drugs2022

A phase 1 study to assess the safety, pharmacokinetics, and anti-tumor activity of the androgen receptor n-terminal domain inhibitor epi-506 in patients with metastatic castration-resistant prostate cancer.

Corinne Maurice-Dror, Ronan Le Moigne, Ulka Vaishampayan, Robert B Montgomery, Michael S Gordon, Nan Hyung Hong, Leah DiMascio, Frank Perabo, Kim N Chi

Abstract readClinical Trial, Phase I
PubMed Publisher
In one paragraph

Article in Investigational new drugs, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
4.3field-weighted citation impact, top 5% 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

19 citing papers in PubMed, 35 citations in OpenAlex.

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  4. α-Mangostin from the mangosteen (Journal of medicinally active plants · 2025
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  14. Targeting the Androgen Signaling Axis in Prostate Cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2023
    Review
  15. Article
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  17. Constitutively Active Androgen Receptor in Hepatocellular Carcinoma.International journal of molecular sciences · 2022
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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

9 authors at 4 institutions in 1 country.

Corinne Maurice-DrorBC Cancer Agency, Vancouver, BC, USA.
Ronan Le MoigneESSA Pharmaceuticals, South San Francisco, Vancouve, CA, USA.
Ulka VaishampayanKarmanos Cancer Institute, Wayne State University, Detroit, MI, USA.
Robert B MontgomeryUniversity of Washington, Seattle, WA, USA.
Michael S GordonHonorHealth Research Institute, Scottsdale, AZ, USA.
Nan Hyung HongESSA Pharmaceuticals, South San Francisco, Vancouve, CA, USA.
Leah DiMascioESSA Pharmaceuticals, South San Francisco, Vancouve, CA, USA.
Frank PeraboESSA Pharmaceuticals, South San Francisco, Vancouve, CA, USA.
Kim N ChiBC Cancer Agency, Vancouver, BC, USA. kchi@bccancer.bc.ca.
Essa Pharma (United States) · USHonorHealth · USUniversity of Washington · USWayne State University · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundEPI-506 is the first of a new class of drugs targeting the N-terminal domain (NTD) of the androgen receptor (AR), potentially overcoming known resistance mechanisms to androgen receptor pathway inhibitors (ARPIs) among men with metastatic castration resistant prostate cancer (mCRPC).

methodsPatients with mCRPC who had progressed on prior ARPI were enrolled in this phase 1 open-label, adaptive 3 + 3 dose escalation study. The primary outcome was safety and tolerability of oral EPI-506. Secondary objectives included determination of the maximal tolerated dose (MTD), pharmacokinetic profile, and antitumor efficacy.

results28 mCRPC patients were enrolled into 7 dose cohorts of EPI-506 ranging from 80-3600 mg given once daily and 1800 mg given twice daily. Six DLTs occurred in 4 patients; Grade 4 elevated amylase; Grade 3 abdominal pain; Grade 3 elevated ALT and Grade 3 elevated AST; Grade 2 nausea and Grade 1 vomiting which resulted in study drug intake of < 75% of the expected dose during the DLT assessment period. The most common drug-related adverse events included diarrhea, nausea and fatigue. Six patients had a PSA decline not meeting PSA response criteria. The study was terminated prior to reaching the MTD due to poor oral bioavailability.

conclusionsThis phase 1 trial established the safety of EPI-506 and provides proof of concept for targeting the AR NTD. Next generation compounds with improved bioavailability and potency are in clinical development.

Indexed as

Androgen Receptor AntagonistsBenzhydryl CompoundsChlorohydrinsProstatic Neoplasms, Castration-ResistantHumansMaleNauseaProstate-Specific AntigenReceptors, AndrogenTreatment OutcomeAndrogen Receptor AntagonistsBenzhydryl CompoundsChlorohydrinsEPI-506Prostate-Specific AntigenReceptors, AndrogenAndrogen receptor-anitenEPI-002EPI-506N-terminal domain of the androgen receptorProstate cancer

Identifiers

PMID34843005
OpenAlexW3216437033

What OpenQuestion holds

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Registered trials

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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.