Darolutamide

What is Darolutamide?

• Darolutamide (Nubeqa) is an androgen receptor inhibitor used to treat men with prostate cancer.

What are the uses of this medicine?

• This medicine is used to treat men with prostate cancer that has not spread to other parts of the body and no longer responds to a medical or surgical treatment that lowers testosterone.

How does this medicine work?

• A formulation containing an androgen receptor (AR) antagonist with potential antineoplastic activity.
• Darolutamide binds to ARs in target tissues; subsequently, inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus.
• This prevents binding to and transcription of AR-responsive genes that regulate prostate cancer cell proliferation.
• This ultimately leads to an inhibition of growth in AR-expressing prostate cancer cells.
• Check for active clinical trialsusing this agent.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid concomitant use of Nubeqa with clinical combined P-gp and strong or moderate CYP3A4 inducers.
• Avoid concomitant use of Nubeqa with a combined P-gp and strong CYP3A4 inhibitor which may increase darolutamide exposure.
• Avoid concomitant use with drugs that are BCRP substrates where possible. If used together, monitor patients more frequently for adverse reactions, and consider dose reduction of the BCRP substrate drug.
• Avoid concomitant use with OATP1B1 and OATP1B3 Substrates. Concomitant use of Nubeqa may increase the plasma concentrations of OATP1B1 or OATP1B3 substrates. If used together, monitor patients more frequently for adverse reactions and consider dose reduction of these drugs.

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

Recommended Dosage

• The recommended dose of Nubeqa is 600 mg (two 300 mg film-coated tablets) taken orally, twice daily, equivalent to a total daily dose of 1200 mg.
• Patients receiving Nubeqa should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.

Recommended Dosage in Patients with Severe Renal Impairment

• For patients with severe renal impairment (eGFR 15–29 mL/min/1.73 m2) not receiving hemodialysis, the recommended dose of Nubeqa is 300 mg twice daily.

Recommended Dosage in Patients with Moderate Hepatic Impairment

• For patients with moderate hepatic impairment (Child-Pugh Class B), the recommended dose of Nubeqa is 300 mg twice daily.

Administration

• Take Nubeqa exactly as your healthcare provider tells you.
• Your healthcare provider may change your dose if needed.
• Take your prescribed dose of Nubeqa 2 times a day with food.
• Swallow Nubeqa tablets whole.
• If you are receiving gonadotropin-releasing hormone (GnRH) analog therapy, you should continue with this treatment during your treatment with Nubeqa unless you have had a surgery to lower the amount of testosterone in your body (surgical castration).
• If you miss a dose of Nubeqa, take your prescribed dose as soon as you remember before the next scheduled dose. Do not take 2 doses together to make up for a missed dose.
• If you take more Nubeqa than prescribed, call your healthcare provider right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 300 mg

This medicine is available in fallowing brand namesː

• Nubeqa

What side effects can this medication cause?

The most common side effects of this medicine include:

• feeling more tired than usual
• arm, leg, hand or foot pain
• rash
• decreased white blood cells (neutropenia)
• changes in liver function tests

What special precautions should I follow?

• Nubeqa can cause fetal harm and loss of pregnancy.
• Advise males with female partners of reproductive potential to use effective contraception.

What to do in case of emergency/overdose?

• 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.
• 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.

Can this medicine be used in pregnancy?

• 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.

Can this medicine be used in children?

• Safety and effectiveness of Nubeqa in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• darolutamide

Inactive ingredients:

• calcium hydrogen phosphate, croscarmellose sodium, lactose monohydrate, magnesium stearate, povidone K 30, hypromellose 15 cP, macrogol 3350, and titanium dioxide.

Who manufactures and distributes this medicine?

• Manufactured by:
• Orion Corporation, Orion Pharma, Espoo, Finland

• Manufactured for:
• Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ USA

What should I know about storage and disposal of this medication?

• Store Nubeqa at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep the bottle tightly closed after you first open it.
• Keep Nubeqa and all medicines out of the reach of children.

• Dailymed label info on Darolutamide
• FDA Darolutamide

Darolutamide Resources
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