Darolutamide

Darolutamide is a prescription medication used for the treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC).

• Darolutamide is available under the following different brand names: Nubeqa

Common side effects of Darolutamide include:

• fatigue
• pain in extremities
• rash

Serious side effects of Darolutamide include:

• arm, leg, hand, or foot pain
• rash
• blood in the urine
• fever, rapid and/or shallow breathing
• cough
• chest pain or feeling of pressure in the chest
• seizures

Rare side effects of Darolutamide include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, light-headedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 300 mg

Nonmetastatic castration-resistant prostate cancer

Adult dosage

• 600 mg orally twice daily

Prostate cancer

Adult dosage

• Darolutamide 600 mg orally two times a day; continue until disease progression or unacceptable toxicity occurs, even if a docetaxel cycle is delayed, interrupted, or discontinued
• Docetaxel 75 mg/m2 IV every 3 weeks; administer the first 6 cycles within 6 weeks after initiating darolutamide.
• Refer to docetaxel prescribing information for additional dosing information, including dosage modifications
• Grade more than 3 toxicity or an intolerable adverse reaction
• Withhold the dose or reduce it to 300 mg orally two times a day until symptoms improve
• Resume at 600 mg orally two times a day
• Do not reduce the dose below 300 mg two times a day

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Darolutamide has severe interactions with no other drugs
• Darolutamide has serious interactions with at least 50 other drugs
• Darolutamide has moderate interactions with at least 38 other drugs
• Darolutamide has minor interactions with the following drug:
  • verapamil

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Darolutamide?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Darolutamide?”

Cautions

• Based on its mechanism of action, fetal harm and loss of pregnancy may occur when administered to pregnant women
• Ischemic heart disease
  • Ischemic heart disease, including fatal cases, was reported
  • Monitor for signs and symptoms of ischemic heart disease
  • Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia
  • Discontinue therapy for grade 3-4 ischemic heart disease
  • Inform patients that treatment has been associated with an increased risk for ischemic heart disease; advise patients to seek immediate medical attention if any symptoms suggestive of ischemic heart disease event occur
• Seizures
  • Seizures may occur
  • Unknown if antiepileptic medications will prevent darolutamide-related seizures
  • Advise patients of the risk of developing a seizure during therapy and of engaging in any activity where sudden loss of consciousness could cause harm to themselves or others
  • Consider discontinuing therapy in patients who develop a seizure during treatment
  • Inform patients to contact their healthcare provider right away if they have a loss of consciousness or seizure
• Drug interaction overview
  • P-gp and CYP3A4 substrate
  • Breast cancer resistance protein (BCRP) transporter inhibitor; OATP1B1 and OATP1B3 inhibitor
  • Combined P-gp and strong or moderate CYP3A4 inducers
    • Avoid coadministration
      • Combined P-gp and strong or moderate CYP3A4 inducer decrease darolutamide exposure, which may decrease darolutamide activity
      • Combined P-gp and strong CYP3A4 inhibitors
      • Combined P-gp and strong CYP3A4 inhibitor increase darolutamide exposure, which may increase the risk for darolutamide adverse reactions
      • Monitor more frequently for darolutamide adverse reactions and modify darolutamide dosage as needed
• BCRP substrates
  • Darolutamide increases the AUC and peak plasma concentration of BCRP substrates, which may increase the risk for BCRP substrate-related toxicities
  • Avoid use with drugs that are BCRP substrates where possible
  • If used together, monitor more frequently for adverse reactions, and consider a dose reduction of the BCRP substrate drug; refer to the prescribing information of the BCRP substrate when used concomitantly with darolutamide

Pregnancy and Lactation

• Safety and efficacy have not been established in women
• Based on its mechanism of action, fetal harm and loss of pregnancy may occur
• Animal embryofetal developmental toxicology studies were not conducted with darolutamide
• There are no human data on the use in pregnant women
• Contraception
  • Men: 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
• Infertility
  • Men: Based on animal studies, fertility may be impaired in men’s reproductive potential
• Lactation
  • Safety and efficacy have not been established in women
  • 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