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Nubeqa

darolutamide
Androgen Receptor Inhibitor Bayer FDA Approved 2019
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

Non-metastatic castration-resistant prostate cancer (nmCRPC); Metastatic hormone-sensitive prostate cancer (mHSPC) — in combination with docetaxel.

2. Dosage and Administration

600 mg orally twice daily (with food)
Swallow whole with food
Continue LHRH analogue or have had bilateral orchiectomy
Severe hepatic impairment (Child-Pugh C): 300 mg twice daily

3. Dosage Forms and Strengths

Tablets: 300 mg

4. Contraindications

Pregnancy (can cause fetal harm).

5. Warnings and Precautions
  • Ischemic Heart Disease: In 4.3%. Includes MI and unstable angina. Monitor for signs/symptoms.
  • Heart Failure: In 2.1%. Monitor cardiac function in patients with risk factors.
  • Rash: In 5.8% (vs 2.6% placebo). Mostly Grade 1-2.
  • Seizure: Darolutamide has minimal blood-brain barrier penetration and low seizure potential compared to other AR inhibitors.
  • Embryo-Fetal Toxicity
6. Adverse Reactions
Most Common Adverse Reactions

Fatigue (16%), pain in extremity (6%), rash (5.8%), AST increased (5%), decreased appetite (5%), constipation (4%), arthralgia (4%), nausea (3.5%)

Fatigue
16%
Pain In Extremity
6%
AST increased
5%
Decreased Appetite
5%
Constipation
4%
Arthralgia
4%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Darolutamide is a structurally distinct androgen receptor inhibitor that competitively inhibits androgen binding to the AR, inhibits AR nuclear translocation, and blocks AR-mediated transcription. It has two active diastereomers (ORM-16228 and ORM-16229) and an active major metabolite (keto-darolutamide). Darolutamide has minimal blood-brain barrier penetration, which may contribute to its lower incidence of CNS-related adverse effects (seizures, falls, fatigue) compared to enzalutamide and apalutamide.

Pharmacokinetics

Tmax: 4 hours. Half-life: approximately 20 hours. Protein binding: 92%. Metabolized by CYP3A4 and aldo-keto reductases (major metabolite keto-darolutamide has similar activity). Food increases AUC by 2-2.5 fold. Steady-state by Day 5. Excreted in urine (64%) and feces (33%).

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Darolutamide Trials on ClinicalTrials.gov ↗ 📚 PubMed: Darolutamide Clinical Trials ↗
Approved Tumor Types
Prostate Cancer