pharmacopeia
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/api/v1/drug/darolutamide

Mechanism of action

Sourced from openFDA

Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription.

Androgen Receptor

Indications

Sourced from openFDA
  • NUBEQA is an androgen receptor inhibitor indicated for the treatment of adult patients with: non-metastatic castration-resistant prostate cancer (nmCRPC). ( 1 ) metastatic castration-sensitive prostate cancer (mCSPC).ICD-10: C61

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

Recommended Dosage : NUBEQA 600 mg (two 300 mg tablets) administered orally twice daily. Swallow tablets whole. Take NUBEQA with food. ( 2.1 ) For patients with mCSPC treated with NUBEQA in combination with docetaxel, administer the first cycle of docetaxel within 6 weeks after the start of NUBEQA treatment. ( 2.1 ) Patients should also receive a gonadotropin-releasing hormone (GnRH) agonist or antagonist concurrently or have had bilateral orchiectomy. ( 2.1 ) 2.1 Recommended Dosage The recommended dose of NUBEQA is 600 mg (two 300 mg tablets) taken orally, twice daily, with food [see Clinical Pharmacology (12.3) ]. Continue treatment until disease progression or unacceptable toxicity occurs. Patients receiving NUBEQA 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 NUBEQA treatment. Refer to docetaxel prescribing information for additional dosing information, including dosage modifications. Treatment with NUBEQA may be continued until disease progression or unacceptable toxicity, even if a cycle of docetaxel is delayed, interrupted, or discontinued [see Dosage and Administration (2.2) ] . Advise patients to swallow tablets whole with food, 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.

Warnings & precautions

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Ischemic Heart Disease : Optimize management of cardiovascular risk factors. Monitor for signs and symptoms of coronary artery disease. Discontinue NUBEQA for Grade 3-4 events. ( 5.1 ) Seizure : Consider discontinuation of NUBEQA in patients who develop a seizure during treatment. ( 5.2 ) Embryo-Fetal Toxicity : NUBEQA can cause fetal harm and loss of pregnancy. Advise males with female partners of reproductive potential to use effective contraception. ( 5.3 , 8.1 , 8.3 ) 5.1 Ischemic Heart Disease Ischemic heart disease, including fatal cases, occurred in patients receiving NUBEQA. In a pooled analysis of ARAMIS and ARANOTE, ischemic heart disease occurred in 3.4% of patients receiving NUBEQA and 2.2% receiving placebo, including Grade 3-4 events in 1.4% and 0.3%, respectively. Ischemic events led to death in 0.4% of patients receiving NUBEQA and 0.4% receiving placebo. In ARASENS, ischemic heart disease occurred in 3.2% of patients receiving NUBEQA with docetaxel and 2% receiving placebo with docetaxel, including Grade 3-4 events in 1.3% and 1.1%, respectively. Ischemic events led to death in 0.3% of patients receiving NUBEQA with docetaxel and 0% receiving placebo with docetaxel. Monitor for signs and symptoms of ischemic heart disease. Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia. Discontinue NUBEQA for Grade 3-4 ischemic heart disease. 5.2 Seizure Seizure occurred in patients receiving NUBEQA. In a pooled analysis of ARAMIS and ARANOTE, Grade 1-3 seizure occurred in 0.2% of patients receiving NUBEQA.

Adverse reactions

Sourced from openFDA

In nmCRPC and mCSPC : The most common adverse reactions (>10% with a ≥2% increase over placebo), including laboratory test abnormalities, are increased AST, decreased neutrophil count, increased bilirubin, fatigue, and increased ALT. ( 6.1 ) In mCSPC in combination with docetaxel : The most common adverse reactions (≥10% with a ≥2% increase over placebo) are constipation, rash, decreased appetite, hemorrhage, increased weight, and hypertension. The most common laboratory test abnormalities (≥30%) are anemia, hyperglycemia, decreased lymphocyte count, decreased neutrophil count, increased AST, increased ALT, and hypocalcemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or WWW.FDA.GOV/MEDWATCH. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled data in WARNINGS and PRECAUTIONS reflect two randomized clinical trials [ARAMIS, ARANOTE] in patients with nmCRPC (N = 954) and mCSPC (N = 445) treated with NUBEQA. In these trials, the median duration of treatment was 18.2 months (range 0.03 to 44.3) for patients who received NUBEQA [ see Clinical Studies (14) ].

Use in specific populations

Sourced from openFDA

Severe Renal Impairment (not on hemodialysis): Recommended dose is 300 mg twice daily. ( 8.6 ) Moderate Hepatic Impairment: Recommended dose is 300 mg twice daily. ( 8.7 ) 8.1 Pregnancy Risk Summary The safety and efficacy of NUBEQA have not been established in females. Based on its mechanism of action, NUBEQA can cause fetal harm and loss of pregnancy [see Clinical Pharmacology (12.1) ]. Animal embryo-fetal developmental toxicology studies were not conducted with darolutamide. There are no human data on the use of NUBEQA in pregnant females. 8.2 Lactation Risk Summary The safety and efficacy of NUBEQA have not been established in females. There are no data on the presence of darolutamide or its metabolites in human milk, the effect on the breastfed child, or the effect on milk production. 8.3 Females and Males of Reproductive Potential Contraception Males Based on the mechanism of action, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 1 week after the last dose of NUBEQA [see Use in Specific Populations (8.1) ]. Infertility Males Based on animal studies, NUBEQA may impair fertility in males of reproductive potential [see Nonclinical Toxicology (13.1) ] . 8.4 Pediatric Use Safety and effectiveness of NUBEQA in pediatric patients have not been established.

Pharmacokinetics

Sourced from openFDA
Metabolism
Following administration of 600 mg twice daily, darolutamide mean (%CV) steady-state peak plasma concentration (C max ) is 4.79 mg/L (30.9%) and area under the plasma concentration-time curve from time 0 to 12 hours (AUC 12h ) is 52.82 h∙µg/mL (33.9%). Steady-state is reached 2–5 days after repeated dosing with food, with an approximate 2-fold accumulation.

Overdosage

Sourced from openFDA

There is no known specific antidote for darolutamide overdose. The highest dose of NUBEQA studied clinically was 900 mg twice daily, equivalent to a total daily dose of 1800 mg. No dose limiting toxicities were observed with this dose. Considering the saturable absorption and the absence of evidence for acute toxicity, an intake of a higher than recommended dose of darolutamide is not expected to lead to systemic toxicity in patients with intact hepatic and renal function [see Clinical Pharmacology (12.3) ] . In the event of intake of a higher than recommended dose in patients with severe renal impairment or moderate hepatic impairment, if there is suspicion of toxicity, interrupt NUBEQA treatment and undertake general supportive measures until clinical toxicity has been diminished or resolved. If there is no suspicion of toxicity, NUBEQA treatment can be continued with the next dose as scheduled.

Approval history

Sourced from openFDA
  • Jul 30, 2019NDANDA212099Bayer Healthcare

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
5,120 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue78015%
  2. 2Hot Flush58311%
  3. 3Death4278.3%
  4. 4Asthenia3256.3%
  5. 5Prostatic Specific Antigen Increased2214.3%
  6. 6Arthralgia2194.3%
  7. 7Dizziness2184.3%
  8. 8Diarrhoea2174.2%
  9. 9Product Dose Omission Issue1973.8%
  10. 10Incorrect Dose Administered1903.7%
  11. 11Nausea1823.6%
  12. 12Dyspnoea1813.5%
  13. 13Neuropathy Peripheral1653.2%
  14. 14Rash1623.2%
  15. 15Pain In Extremity1593.1%

Clinical trials

View JSON

The 10 most recently updated of 149 ClinicalTrials.gov registrations naming Darolutamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Darolutamide work?
Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription.
What is Darolutamide used for?
According to FDA labeling, Darolutamide carries indications including: NUBEQA is an androgen receptor inhibitor indicated for the treatment of adult patients with: non-metastatic castration-resistant prostate cancer (nmCRPC). ( 1 ) metastatic castration-sensitive prostate cancer (mCSPC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Darolutamide?
Darolutamide is classified as Anti-androgens, Androgen Receptor Antagonists, Cellular Proliferation Alteration, Cellular Transport Alteration, Decreased Transcription to RNA.
What are the brand names for Darolutamide?
Darolutamide is marketed under brand names including Nubeqa.
What are the contraindications for Darolutamide?
Darolutamide labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for darolutamide is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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