Second-generation androgen receptor antagonist Pregnancy: Safety and efficacy have not been established in females. Based on its mechanism of action, darolutamide can cause fetal harm and loss of pregnancy; there are no human data in pregnant females and animal embryo-fetal developmental toxicology studies were not conducted. Advise males with female partners of reproductive potential to use effective contraception (US PI §8.1, §5.3).

Darolutamide

Brand names: Nubeqa

Darolutamide is an oral androgen receptor inhibitor used, with androgen deprivation therapy, in non-metastatic castration-resistant prostate cancer and in metastatic hormone-sensitive prostate cancer alongside chemotherapy.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 600 mg (two 300 mg tablets) twice daily

Route: Oral

Frequency: Twice daily, with food

US prescribing information (NUBEQA §2.1): the recommended dose is 600 mg (two 300 mg tablets) taken orally twice daily, with food; swallow tablets whole. Continue treatment until disease progression or unacceptable toxicity occurs. Patients receiving darolutamide should also receive a gonadotropin-releasing hormone (GnRH) agonist or antagonist concurrently, or have had a bilateral orchiectomy. When used in combination with docetaxel for mCSPC, administer the first of 6 cycles of docetaxel within 6 weeks after the start of darolutamide; treatment may be continued until disease progression or unacceptable toxicity even if a docetaxel cycle is delayed, interrupted or discontinued. Advise patients to take any missed dose as soon as they remember prior to the next scheduled dose, and not to take two doses together to make up for a missed dose. Dose modification (§2.2): if a patient experiences a ≥Grade 3 or an intolerable adverse reaction, withhold darolutamide or reduce the dose to 300 mg twice daily until symptoms improve, then resume at 600 mg twice daily when the reaction returns to baseline; dosage reduction below 300 mg twice daily is not recommended. Additional dose modifications may be required for ischaemic heart disease or seizure. Moderate hepatic impairment (Child-Pugh Class B): 300 mg twice daily (§2.4). No eMC/UK SPC was available in this bundle — US labelling may differ from UK; clinician to verify against the UK SPC. Paediatric: safety and effectiveness have not been established.

Dose adjustments

Renal

Severe renal impairment (eGFR 15–29 mL/min/1.73 m²) not receiving haemodialysis: 300 mg twice daily (US PI §2.3).

Dose auto-extracted from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

None — US prescribing information §4 states 'None'

Side effects

Increased AST
Decreased neutrophil count
Increased bilirubin
Fatigue
Increased ALT
In combination with docetaxel (mCSPC): constipation, rash, decreased appetite, haemorrhage, increased weight and hypertension; laboratory abnormalities include anaemia, hyperglycaemia, decreased lymphocyte count and hypocalcaemia
Ischaemic heart disease, including fatal cases (3.4% vs 2.2% placebo in pooled ARAMIS/ARANOTE); seizure

Interactions

Combined P-glycoprotein and strong or moderate CYP3A4 inducers — avoid concomitant use; they decrease darolutamide exposure, which may decrease activity
Combined P-glycoprotein and strong CYP3A4 inhibitors — increase darolutamide exposure and the risk of adverse reactions; monitor patients more frequently and modify the darolutamide dose accordingly
BCRP substrates — avoid concomitant use where possible; if used together, monitor more frequently for adverse reactions and consider a dose reduction of the BCRP substrate
OATP1B1 and OATP1B3 substrates — plasma concentrations may increase; monitor more frequently for adverse reactions and consider a dose reduction of these drugs

Clinical monograph

How it works

It binds the androgen receptor and inhibits its nuclear translocation and downstream transcriptional activity, suppressing androgen-driven prostate tumour growth.

Prescribing in practice

It must be combined with ongoing androgen deprivation therapy (or bilateral orchidectomy) and is not a substitute for it.
Fatigue, rashes and changes in some blood parameters may occur, and it can interact with breast cancer resistance protein and CYP3A4 substrates.
Women who are or may become pregnant should not handle the tablets without protection given the potential to affect a developing fetus.

Monitoring

Monitor prostate-specific antigen and clinical response, together with tolerability and relevant drug interactions during treatment.

Counselling the patient

Continue your hormone injections or implants as well as taking these tablets.
Take the tablets with food as directed and report troublesome fatigue or rash.
Tell your team about all other medicines because interactions are possible.

Evidence & guidelines

The ARAMIS trial showed darolutamide prolonged metastasis-free survival in non-metastatic castration-resistant prostate cancer, and ARASENS supported its use in metastatic hormone-sensitive disease.

Reference: NICE TA660; NICE TA805; NICE NG131; ESMO; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways