Drug intelligence / Profile preview

AZD0516

Development stage
Phase 2
Lead developer
AstraZeneca
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

AZD0516 is a **first-in-class antibody-drug conjugate (ADC)** targeting the six-transmembrane epithelial antigen of the prostate-2 (**STEAP2**), a novel tumor-associated antigen that is highly expressed in metastatic prostate cancer. Its mechanism involves selectively binding to STEAP2, enabling targeted delivery of its cytotoxic payload to STEAP2-expressing tumor cells. The payload inhibits **DNA topoisomerase I (TOP1)**, leading to DNA damage and cell death. AZD0516 is under investigation as both monotherapy and in combination with other agents (such as AZD9574) for metastatic castration-resistant prostate cancer (mCRPC). It is currently in Phase I/II clinical trials. It was developed by AstraZeneca[1][2][3][5][7][9][11][12].

Brand names
AZD0516AZD-0516AZD 0516
Other names
AZD0516AZD-0516AZD 0516
02

Targets

STEAP2 (Six-transmembrane epithelial antigen of the prostate 2)TOP1 (DNA Topoisomerase I)

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