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Darolutamide Oral Tablet

Santa Chiara Hospital · FDA-approved active Small molecule

Darolutamide is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting androgen-driven prostate cancer cell growth.

Darolutamide is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting androgen-driven prostate cancer cell growth. Used for Non-metastatic castration-resistant prostate cancer (nmCRPC), Metastatic hormone-sensitive prostate cancer (mHSPC).

At a glance

Generic nameDarolutamide Oral Tablet
SponsorSanta Chiara Hospital
Drug classAndrogen receptor antagonist
TargetAndrogen receptor (AR)
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

Darolutamide competitively binds to the ligand-binding domain of the androgen receptor with high affinity and selectivity, preventing activation by testosterone and dihydrotestosterone. This blocks downstream signaling that drives proliferation and survival of androgen-dependent prostate cancer cells. It is a non-steroidal antiandrogen with improved blood-brain barrier penetration compared to earlier-generation agents.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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