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Target Overview
STEAP2, also known as Six Transmembrane Epithelial Antigen of Prostate 2, is a metalloreductase that localizes to the cell surface, endosome, and Golgi.1,2,3 STEAP2 is highly and homogenously expressed across all stages of prostate tumors and is virtually absent in normal adult non-prostate tissues, making it an ideal radioconjugate target for patients with prostate cancer.4,5,6
Compound Overview
AZD2284 is a STEAP2 targeting radioconjugate designed for metastatic castration-resistant prostate cancer. It consists of three parts: 1) a monoclonal antibody that binds to STEAP2, 2) a linker, and 3) a chelator that acts as a “cage” to hold radioactive isotopes, like actinium-225.
AZD2284 is an investigational compound that binds with high affinity to STEAP2 on the surface of prostate cancer cells. The radioactive decay of actinium-225 (and subsequent daughter isotopes) leads to alpha particle emission, which results in significant DNA and cellular damage and apoptotic cell death.7
Mechanism of Action
References
1. Hasegawa H, Li C, Alba BM, et al. Exp Cell Res. 2018;370(2):208-26. 2. Lee JK, Bangayan NJ, Chai T. Proc Natl Acad Sci U S A. 2018;115(19):E4473-E4482. 3. Hubert RS, Vivanco I, Chen E, et al. Proc Natl Acad Sci U S A. 1999;96(25):14523-14528. 4. Porkka KP, Helenius MA, Visakorpi T. Lab Invest. 2002;82(11):1573-1582. 5. Zanvit P, van Dyk D, Fazenbaker C, et al. J Clin Invest. 2023;133(22):e169655. 6. Korkmaz KS, Elbi C, Korkmaz CG, et al. J Biol Chem. 2002;277(39):36689-96. 7. Bidkar AP, Zerefa L, Yadav S, et al. Theranostics. 2024;14(7):2969-2992.
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Abbreviations
mCRPC
metastatic castration-resistant prostate cancer
STEAP2
six transmembrane epithelial antigen of the prostate 2
Target Overview
STEAP2, also known as Six Transmembrane Epithelial Antigen of Prostate 2, is a metalloreductase that localizes to the cell surface, endosome, and Golgi.1,2,3 STEAP2 is highly and homogenously expressed across all stages of prostate tumors and is virtually absent in normal adult non-prostate tissues, making it an ideal radioconjugate target for patients with prostate cancer.4,5,6
Compound Overview
AZD2284 is a STEAP2 targeting radioconjugate designed for metastatic castration-resistant prostate cancer. It consists of three parts: 1) a monoclonal antibody that binds to STEAP2, 2) a linker, and 3) a chelator that acts as a “cage” to hold radioactive isotopes, like actinium-225.
AZD2284 is an investigational compound that binds with high affinity to STEAP2 on the surface of prostate cancer cells. The radioactive decay of actinium-225 (and subsequent daughter isotopes) leads to alpha particle emission, which results in significant DNA and cellular damage and apoptotic cell death.7
Mechanism of Action
References
1. Hasegawa H, Li C, Alba BM, et al. Exp Cell Res. 2018;370(2):208-26. 2. Lee JK, Bangayan NJ, Chai T. Proc Natl Acad Sci U S A. 2018;115(19):E4473-E4482. 3. Hubert RS, Vivanco I, Chen E, et al. Proc Natl Acad Sci U S A. 1999;96(25):14523-14528. 4. Porkka KP, Helenius MA, Visakorpi T. Lab Invest. 2002;82(11):1573-1582. 5. Zanvit P, van Dyk D, Fazenbaker C, et al. J Clin Invest. 2023;133(22):e169655. 6. Korkmaz KS, Elbi C, Korkmaz CG, et al. J Biol Chem. 2002;277(39):36689-96. 7. Bidkar AP, Zerefa L, Yadav S, et al. Theranostics. 2024;14(7):2969-2992.
Clinical trial information
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Abbreviations
mCRPC
metastatic castration-resistant prostate cancer
STEAP2
six transmembrane epithelial antigen of the prostate 2