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arv-110
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Overview
NCI Definition [1]:
An orally available selective androgen receptor (AR)-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. ARV-110 is composed of an AR ligand attached to an E3 ligase recognition moiety. Upon oral administration, ARV-110 targets and binds to the AR ligand binding domain. E3 ligase is recruited to the AR by the E3 ligase recognition moiety and the AR target protein is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome. This prevents the expression of AR target genes and halts AR-mediated signaling. This results in an inhibition of proliferation in AR-overexpressing tumor cells. In addition, the degradation of the AR protein releases the ARV-110 is released and can bind to additional AR target proteins. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC).
Clinical Trials
Arv-110 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating arv-110, 1 is phase 1/phase 2 (1 open).
Prostate adenocarcinoma is the most common disease being investigated in arv-110 clinical trials [2].
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.
