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Target Overview
The androgen receptor (AR) is a nuclear hormone receptor which is activated by androgens such as testosterone. It acts as a transcription factor, driving the expression of genes involved in prostate cell growth and differentiation.1,2
Androgen deprivation therapies are a mainstay treatment for metastatic prostate cancer, but resistance inevitably occurs through mechanisms such as AR amplification and AR ligand binding domain mutations.3,4 Degradation of AR is thus an attractive strategy to overcome resistance and potentially drive deeper pathway inhibition than current AR pathway inhibitors (ARPIs).
Compound Overview
AZD9750 is a potent, selective, and orally bioavailable PROTAC (PROteolysis Targeting Chimera) that degrades AR.5 It is being investigated as a therapy for metastatic castration resistant and metastatic hormone-sensitive PC.
Mechanism of Action
References
1. Davey RA, Grossmann M. Clin Biochem Rev. 2016;37(1):3-15. 2. Tan MH, Li J, Xu HE, Melcher K, Yong EL. Acta Pharmacol Sin. 2015;36(1):3-23. 3. Buttigliero C, Tucci M, Bertaglia V, et al. Cancer Treat Rev. 2015;41(10):884-892. 4. Kirby M, Hirst C, Crawford ED. Int J Clin Pract. 2011;65(11):1180-1192. 5. Scott JS, Evans L, Astles PC, et al. J Med Chem. 2026;69(3):3209-3232.
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Abbreviations
AR
androgen receptor
ARPIs
androgen receptor pathway inhibitors
PROTAC
PROteolysis TArgeting Chimera
PC
prostate cancer
Target Overview
The androgen receptor (AR) is a nuclear hormone receptor which is activated by androgens such as testosterone. It acts as a transcription factor, driving the expression of genes involved in prostate cell growth and differentiation.1,2
Androgen deprivation therapies are a mainstay treatment for metastatic prostate cancer, but resistance inevitably occurs through mechanisms such as AR amplification and AR ligand binding domain mutations.3,4 Degradation of AR is thus an attractive strategy to overcome resistance and potentially drive deeper pathway inhibition than current AR pathway inhibitors (ARPIs).
Compound Overview
AZD9750 is a potent, selective, and orally bioavailable PROTAC (PROteolysis Targeting Chimera) that degrades AR.5 It is being investigated as a therapy for metastatic castration resistant and metastatic hormone-sensitive PC.
Mechanism of Action
References
1. Davey RA, Grossmann M. Clin Biochem Rev. 2016;37(1):3-15. 2. Tan MH, Li J, Xu HE, Melcher K, Yong EL. Acta Pharmacol Sin. 2015;36(1):3-23. 3. Buttigliero C, Tucci M, Bertaglia V, et al. Cancer Treat Rev. 2015;41(10):884-892. 4. Kirby M, Hirst C, Crawford ED. Int J Clin Pract. 2011;65(11):1180-1192. 5. Scott JS, Evans L, Astles PC, et al. J Med Chem. 2026;69(3):3209-3232.
Clinical trial information
Select trial for more information
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Abbreviations
AR
androgen receptor
ARPIs
androgen receptor pathway inhibitors
PROTAC
PROteolysis TArgeting Chimera
PC
prostate cancer