Darolutamide (Systemic)
Brand names: Nubeqa
Drug class:
Antineoplastic Agents
Usage of Darolutamide (Systemic)
Nonmetastatic Castration-resisitant Prostate Cancer
Treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC) in adult patients who are either receiving concomitant treatment with a gonadotropin-releasing hormone (GnRH) analog or who have had a bilateral orchiectomy.
The use of an androgen receptor antagonist (i.e., darolUTAmide, apalutamide, Enzalutamide) is recommended for patients with nmCRPC who are at high risk of metastases.
Metastatic Hormone-sensitive Prostate Cancer
Treatment of metastatic hormone-sensitive prostate cancer (mHSPC) in combination with docetaxel in adult patients who are receiving concomitant treatment with a GnRH analog or who have had a bilateral orchiectomy.
In selected patients with de novo mHSPC, clinicians should offer androgen deprivation therapy (ADT) in combination with docetaxel and either abiraterone acetate plus prednisone or darolutamide.
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How to use Darolutamide (Systemic)
General
Patient Monitoring
Dispensing and Administration Precautions
Other General Considerations
Administration
Oral Administration
Administer orally twice daily with food. Swallow tablets whole.
Dosage
Adults
Nonmetastic Castration-resistant Prostate Cancer Oral600 mg twice daily. Continue therapy until disease progression or unacceptable toxicity occurs.
Metastatic Hormone-sensitive Prostate Cancer Oral600 mg twice daily.
In combination with docetaxel, administer the first of 6 cycles of docetaxel within 6 weeks after the start of darolutamide treatment. Refer to docetaxel prescribing information for additional dosing information, including dosage modifications.
Continue treatment until disease progression or unacceptable toxicity occurs, even if a cycle of docetaxel is delayed, interrupted, or discontinued.
Dosage Modifications for Toxicity OralInterupt therapy or reduce dosage to 300 mg twice daily if intolerable or grade 3 or greater adverse effect occurs. Resume dosage of 600 mg twice daily when the adverse Reaction returns to baseline. Dosage reduction <300 mg twice daily not recommended.
Special Populations
Hepatic Impairment
Mild hepatic impairment (Child-Pugh class A): No initial dosage adjustment required.
Moderate hepatic impairment (Child-Pugh class B): 300 mg twice daily.
Severe hepatic impairment (Child-Pugh class C): Not studied.
Renal Impairment
Mild or moderate renal impairment (eGFR 30–89 mL/minute per 1.73 m2): No initial dosage adjustment required.
Severe renal impairment (eGFR 15–29 mL/minute per 1.73 m2) not receiving hemodialysis: 300 mg twice daily.
End-stage renal disease (eGFR <15 mL/minute per 1.73 m2): Not studied.
Geriatric Use
No special dosage recommendations; most patients in principal efficacy study were geriatric.
Warnings
Contraindications
Warnings/Precautions
Ischemic Heart Disease
Ischemic heart disease reported, including fatalities.
Monitor for signs and symptoms of ischemic heart disease. Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia. Discontinue for Grade 3 or 4 ischemic heart disease.
Seizures
Seizures reported.
Unknown whether anti-epileptic medications will prevent seizures. Advise patients of risk of seizures and risk of engaging in any activity where sudden loss of consciousness could cause harm to themselves or others. Consider discontinuation in patients who develop a seizure during treatment.
Fetal/Neonatal Morbidity and Mortality
May cause fetal harm and potential loss of pregnancy. Safety and efficacy not established in females.
Males with female partners of reproductive potential should use effective methods of contraception during therapy and for 1 week after the last dose of the drug.
Specific Populations
PregnancyMay cause fetal harm and potential loss of pregnancy.
LactationNot known whether darolutamide or its metabolites are distributed into milk, affect milk production, or affect nursing infants.
Female and Males of Reproductive PotentialMales with female partners of reproductive potential should use effective methods of contraception during darolutamide therapy and for 1 week after the last dose of the drug.
Based on animal studies, darolutamide may impair fertility in males of reproductive potential.
Pediatric UseSafety and efficacy not established in pediatric patients.
Geriatric UseNo overall differences in safety or efficacy relative to younger adults.
Hepatic ImpairmentExposure to darolutamide increased in individuals with moderate hepatic impairment. Pharmacokinetics not established in patients with severe hepatic impairment.
Renal ImpairmentExposure to darolutamide increased in individuals with severe renal impairment not receiving dialysis. Pharmacokinetics not established in patients with end-stage renal disease.
Common Adverse Effects
Adverse effects occurring in ≥2% of patients with nmCRPC include fatigue, pain in extremity, and rash. Laboratory test abnormalities reported in ≥2% of these patients include increased AST, decreased Neutrophil count, and increased bilirubin.
Adverse effects occuring in ≥10% of patients with mHSPC include constipation, decreased appetite, rash, hemorrhage, increased weight, and hypertension. Laboratory test abnormalities in these patients (≥30%) include anemia, hyperglycemia, decreased lymphocyte count, decreased neutrophil count, increased AST and ALT, and hypocalcemia.
What other drugs will affect Darolutamide (Systemic)
Metabolized principally by CYP3A4; also metabolized by UGT1A9 and UGT1A1.
Induces CYP3A4 and inhibits P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) in vitro; also inhibits organic anion transport protein (OATP) 1B1 and OATP1B3 in vitro.
Did not inhibit the major CYP enzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 or transporters, including multidrug resistance protein 2 (MRP2), bile salt export pump (BSEP), organic anion transporters (OATs), organic cation transporters (OCTs), multidrug and toxin extrusion transporters (MATEs), OATP2B1, and sodium taurocholate co-transporting polypeptide (NTCP), at clinically relevant concentrations.
Drugs Affecting Hepatic Microsomal Enzymes and P-glycoprotein
Combined P-gp and potent CYP3A4 inhibitors: Increased darolutamide exposure and possible increased risk of darolutamide adverse effects. Monitor patients more frequently for darolutamide toxicity, and modify darolutamide dosage as needed.
Combined P-gp and moderate or potent CYP3A4 inducers: Decreased darolutamide exposure and possible decreased darolutamide activity. Avoid concomitant use.
Moderate CYP3A4 inducers: Decrease of 36–58% in darolutamide exposure expected.
Drugs Affected by Breast Cancer Resistance Protein and Organic Anion Transport Protein
BCRP substrates: Increased exposure of BCRP substrate and possible increased risk of BCRP substrate-related toxicity. Avoid concomitant use when possible. If concomitant use cannot be avoided, monitor patients more frequently for adverse effects; consult manufacturer's prescribing information for BCRP substrate and consider dosage reduction of BCRP substrate.
OATP1B1/OATP1B3 substrates: Increased exposure of OATP1B1 or OATP1B3 substrate and possible increased risk of substrate-related toxicity. Monitor for adverse reactions of these drugs and reduce dosage if needed while taking darolutamide.
Specific Drugs
Drug
Interaction
Comments
Dabigatran
No clinically important effects on dabigatran pharmacokinetics
Docetaxel
No clinically important effects on docetaxel pharmacokinetics in mHSPC patients
No clinically important effects on darolutamide pharmacokinetics
Itraconazole
Darolutamide AUC and peak plasma concentration increased by 1.7- and 1.4-fold, respectively
Monitor more frequently for darolutamide toxicity; modify darolutamide dosage as needed
Midazolam
Midazolam AUC and peak plasma concentration decreased by 29 and 32%, respectively
Not considered clinically important
Rifampin
Darolutamide AUC and peak plasma concentration decreased by 72 and 52%, respectively
Avoid concomitant use
Rosuvastatin
Rosuvastatin AUC and peak plasma concentration increased approximately fivefold; no clinically important effects on darolutamide pharmacokinetics
In efficacy study, increased Scr, AST/ALT, and bilirubin concentrations more common in those receiving darolutamide (rather than placebo) with a BCRP substrate statin (e.g., rosuvastatin)
Avoid concomitant use; if concomitant use cannot be avoided, monitor more frequently for adverse effects; consult rosuvastatin prescribing information and consider rosuvastatin dosage reduction
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