Drug intelligence / Profile preview

AZD3514

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZD3514 is a first-in-class, orally bioavailable small molecule that acts as a selective androgen receptor downregulator (SARD) and androgen receptor antagonist. It inhibits both androgen-dependent and androgen-independent signaling by the androgen receptor (AR). The drug works through two main mechanisms of action: it blocks ligand-driven nuclear translocation of the AR and downregulates AR protein levels within cells. AZD3514 was developed primarily for the treatment of metastatic castration-resistant prostate cancer (CRPC), where continued AR signaling drives disease progression even after classical hormone ablation therapies have failed. Clinical studies showed moderate anti-tumor activity in CRPC patients but also significant side effects, particularly nausea and vomiting, which limited its further development[1][2][3][6][8].

02

Targets

AR (Adrenergic receptors)

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