Darolutamide
NUBEQA
Pronunciation: dar-oe-LOO-ta-mide (NOO-be-ka)
What it isNonsteroidal androgen-receptor antagonist; nonmetastatic castration-resistant and metastatic hormone-sensitive prostate cancer.
Why this oneMinimal blood-brain-barrier penetration produces fewer CNS effects and less seizure concern than apalutamide or enzalutamide.
What limits itFatigue, rash, and cardiovascular events can limit treatment; P-gp, BCRP, and CYP3A4 interactions alter exposure.
Darolutamide prescription history
Animated chart of estimated U.S. prescriptions per year, Oral anticancer meds (1953–2026). Darolutamide enters in 2019 (estimated).
Principal riskNo FDA boxed warning.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Non-metastatic castration-resistant prostate cancer (nmCRPC) | Adults | 600 mg (2 x 300 mg tabs) BID with food | 600 mg BID | 600 mg BID |
| Metastatic castration-sensitive prostate cancer (mCSPC), in combination with docetaxel | Adults | 600 mg BID with food (first docetaxel cycle within 6 wk of starting) | 600 mg BID | 600 mg BID |
Renal Severe (eGFR 15-29, not on hemodialysis): 300 mg BID. Mild-moderate (eGFR 30-89): no adjustment. ESRD (eGFR <15): unknown
Hepatic Moderate (Child-Pugh B): 300 mg BID. Mild: no adjustment. Severe (Child-Pugh C): unknown
For >=Grade 3 or intolerable adverse reaction: withhold or reduce to 300 mg BID; resume 600 mg BID when back to baseline. Do not reduce below 300 mg BID. Discontinue for Grade 3-4 ischemic heart disease
Instructions
- Swallow tablets whole, take with food
- Continue GnRH agonist/antagonist concurrently unless prior bilateral orchiectomy
- Missed dose: take as soon as remembered before next scheduled dose; do not double up
- Continue until disease progression or unacceptable toxicity
Available strengths
- tab 300 mg
Cautions
- Ischemic heart disease (incl. fatal): optimize CV risk factors, monitor; discontinue for Grade 3-4 events
- Seizure (0.2-0.8%): consider discontinuation if seizure occurs; caution with activities where loss of consciousness could cause harm
- Embryo-fetal toxicity: males with female partners of reproductive potential use effective contraception during and 1 week after treatment
Adverse reactions
- nmCRPC/mCSPC: increased AST, decreased neutrophils, increased bilirubin, fatigue, increased ALT
- With docetaxel (mCSPC): constipation, rash, decreased appetite, hemorrhage, weight increase, hypertension; labs (>=30%): anemia, hyperglycemia, decreased lymphocytes/neutrophils, increased AST/ALT, hypocalcemia
Pregnancy Not established in females; can cause fetal harm and pregnancy loss based on mechanism; no human data
Lactation Not established in females; no data on presence in human milk or effects on infant/milk production
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 300 mg | tab | 60 BID | not offered |
Generic entry2038 est.
Open Darolutamide in the interactive console ↗
Self-check
- Why does darolutamide cause fewer CNS effects than apalutamide/enzalutamide?
Minimal blood-brain-barrier penetration. - Name two transporters involved in darolutamide interactions.
P-gp and BCRP.