NUBEQA (darolutamide)
Mechanism of Action (MOA)
NUBEQA (darolutamide) is an oral, non-steroidal, second-generation androgen receptor inhibitor (ARI) indicated for the treatment of adult men with non-metastatic castration-resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease, or with metastatic hormone-sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy, or with mHSPC in combination with docetaxel.
Choose NUBEQA for efficacy that doesn’t compromise your patients’ QoL.
Clinically proven in Phase III studies across three indications in mHSPC and nmCRPC.
Refer to full Summary of Product Characteristics (SmPC) before prescribing.
NUBEQA (darolutamide) MOA - How does NUBEQA (darolutamide) work?
Androgens, specifically testosterone and dihydrotestosterone (DHT), promote the growth of both normal and prostate cancer (PC) cells by binding to the androgen receptor (AR). Upon activation, the AR drives the expression of genes involved in growth, differentiation and survival of PC cells.
NUBEQA competitively inhibits androgens from binding to their receptors, prevents testosterone-induced translocation of AR to the nucleus, as well as AR-mediated gene transcription. These mechanisms ultimately reduce AR-mediated gene expression that promote prostate cancer cell growth leading to antitumour activity and as a result, treatment with NUBEQA decreases prostate tumour cell proliferation leading to potent antitumour activity.
Darolutamide Mechanism of Action
Adapted from Fizazi K, et al. 2018.
NUBEQA also interacts with fewer medications versus other second-generation androgen receptor inhibitors (ARIs)
offering confidence when treating patients who require concomitant medication
How is the NUBEQA (darolutamide) molecular structure distinct to other second-generation androgen receptor inhibitors (ARIs)?
NUBEQA has a distinct molecular structure with proven tolerability and efficacy in both mHSPC and high-risk nmCRPC Phase III clinical trials.
- NUBEQA has a flexible, polar-substituted pyrazole structure that binds with high affinity directly to the AR, leading to potent antitumour activity.
This distinct molecular structure is key to the reduced darolutamide blood-brain barrier (BBB) penetration versus other second-generation androgen receptor inhibitors, as demonstrated in preclinical studies.¶
- Medicines with a reduced blood–brain barrier penetration have been shown to have lower effects on the central nervous system.
¶ Versus apalutamide and enzalutamide in a preclinical model.
* Blood-brain barrier passage rate in a preclinical study.
Adapted from Zurth et al. 2019.¶
How does NUBEQA’s mechanism of action translate to clinical trial outcomes in mHSPC and nmCRPC?
Abbreviations
AR, androgen receptor; ARI, androgen receptor inhibitor; ARE, androgen-response element; BBB, blood-brain barrier; DHT, dihydrotestosterone; HSP, heat shock protein; mHSPC, metastatic hormone-sensitive prostate cancer; MOA, mechanism of action; nmCRPC, non-metastatic castration-resistant prostate cancer; P, phosphate; PC, prostate cancer; PSA, prostate-specific antigen; QoL, quality of life.
PP-NUB-GB-2541 | August 2025