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arv-471

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Overview

NCI Definition [1]:
An orally available hetero-bifunctional molecule and selective estrogen receptor (ER) alpha-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. ARV-471 is composed of an ER alpha ligand attached to an E3 ligase recognition moiety. Upon oral administration, ARV-471 targets and binds to the ER ligand binding domain on ER alpha. E3 ligase is recruited to the ER by the E3 ligase recognition moiety and ER alpha is tagged by ubiquitin. This causes ubiquitination and degradation of ER alpha by the proteasome. This decreases ER alpha protein levels, decreases the expression of ER alpha-target genes and halts ER-mediated signaling. This results in an inhibition of proliferation in ER alpha-overexpressing tumor cells. In addition, the degradation of the ER alpha protein releases the ARV-471 and can bind to additional ER alpha target proteins. ER alpha is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation.

Clinical Trials

View Clinical Trials for arv-471

Arv-471 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating arv-471, 1 is phase 1/phase 2 (1 open).

ER Expression, ER Positive, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for arv-471 clinical trials.

Breast carcinoma is the most common disease being investigated in arv-471 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Arv-471
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating arv-471 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
arv 471, arv471
Drug Target(s) [2]:
ESR1
NCIT ID [1]:
C165420

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.