Nubeqa

Nubeqa (darolutamide) is an androgen receptor inhibitor (anti-androgen) medicine used to treat prostate cancer in certain patients.

Nubeqa works by blocking androgens, such as testosterone, from binding to the androgen receptor on prostate cancer cells, which slows cancer cell growth and limits further cell division.

Nubeqa tablets are taken twice daily with food. Tablets should be swallowed whole.

Common Nubeqa side effects are tiredness, decreased white blood cells (neutropenia), and an increase in liver function tests.

Nubeqa is FDA-approved to treat adult patients with:

• non-metastatic castration-resistant prostate cancer (nmCRPC):

• Prostate cancer that has not spread to other parts of your body and no longer responds to a medical or surgical treatment that lowers testosterone

• metastatic castration-sensitive prostate cancer (mCSPC):

Take Nubeqa exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Swallow the tablet whole and do not crush, chew, or break it. Take with food.

If you have not had castration surgery (to lower the amount of testosterone in your body), your doctor may also prescribe a gonadotropin-releasing hormone (GnRH) medicine such as Eligard, Lupron, Trelstar, Zoladex, or Vantas. Keep using your GnRH as directed.

Heart disease: Serious heart problems, including blocked arteries (ischemic heart disease), have occurred in some people taking this medicine. Get medical help right away if you have chest pain, discomfort at rest or with activity, or shortness of breath during treatment.

Seizures: Nubeqa may increase the risk of seizures. Avoid activities where loss of consciousness could be dangerous. Tell your healthcare provider immediately if you have a seizure or lose consciousness.

Embryo-Fetal Toxicity: Nubeqa can cause fetal harm and loss of pregnancy. Advise males with female partners of reproductive potential to use effective contraception.

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

To make sure Nubeqa is safe for you, tell your doctor if you have ever had:

• have heart problems
• have high blood pressure
• have diabetes
• have high amounts of fat or cholesterol in your blood (dyslipidemia)
• have a history of seizures, brain injury, stroke, or brain tumors
• have kidney or liver problems.

Nubeqa may harm an unborn baby or cause a miscarriage. Nubeqa is not for use by women. Males should use effective birth control if their sex partner is able to get pregnant. Keep using birth control for at least 1 week after your last dose. Tell your doctor right away if a pregnancy occurs while you are using Nubeqa.

It may be harder for you to get a woman pregnant while you are using Nubeqa. You should still use birth control to prevent pregnancy because the medicine can harm an unborn baby.

Nubeqa is not for use by women or by anyone younger than 18 years old.

Common Nubeqa side effects

Common Nubeqa side effects may include:

• feeling tired;
• low white blood cells; or
• abnormal liver function tests.

When used in combination with docetaxel in mCSPC, the most common side effects of Nubeqa are:

• constipation
• rash
• decreased appetite
• hemorrhage
• increased weight
• high blood pressure
• laboratory test abnormalities, such as anemia, high blood glucose levels, decreased lymphocyte count, decreased neutrophil count, increased AST, increased ALT, and low calcium levels.

Serious side effects

Get emergency medical help if you have signs of an allergic reaction to Nubeqa: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• chest pain or discomfort at rest or with activity, or shortness of breath; or
• loss of consciousness or a seizure.

Your cancer treatments may be delayed if you have certain side effects.

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Usual Adult Dose for Prostate Cancer:

• 600 mg (2 x 300 mg tablets) orally 2 times a day.
• Swallow tablets whole.
• Take with food.

Dose modification:

• Dose should be modified for patients with severe renal impairment or moderate hepatic impairment

Comments:

• Patients receiving this drug should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.
• 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.

Formulation: 300mg tablet

Take the missed dose as soon as you remember. If it is time for your next scheduled dose, you may take the missed dose together with your next scheduled dose. Then go back to your regular schedule taking Nubeqa 2 times a day.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.

Other drugs may interact with darolutamide, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

Effects of other drugs on Nubeqa

Strong CYP3A4 and P-gp inducers:

• Decreases darolutamide exposure, which may decrease the activity of Nubeqa.
• Recommendation: Do not use Nubeqa with combined P-gp and strong or moderate CYP3A4 inducers.
• Examples: rifampin, carbamazepine, phenytoin, St. John’s wort.

Strong CYP3A4 inhibitors:

• Increases darolutamide exposure, which may increase the risk of Nubeqa side effects.
• Recommendation: Use with caution; clinical monitoring advised.
• Examples: itraconazole, clarithromycin.

Effects of Nubeqa on other drugs

Breast Cancer Resistance Protein (BCRP) and Organic Anion Transporting Polypeptides (OATP) 1B1 and 1B3 Substrates

Review the prescribing information of the BCRP, OATP1B1 and OATP1B3 substrates when used concomitantly with Nubeqa.

Not all possible drug interactions are listed here

Store at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.

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.

Manufactured by: Orion Corporation, Orion Pharma, FI-02101 Espoo, Finland

Manufactured for: Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ 07981 USA