NUBEQA (Darolutamide)
Androgen receptor inhibitor for the treatment of prostate cancer
Quick Facts about NUBEQA
Key Takeaways about NUBEQA
- Proven survival benefit: Clinical trials (ARAMIS and ARASENS) demonstrated significant improvements in metastasis-free survival and overall survival in prostate cancer patients
- Take with food: NUBEQA must be taken with food to ensure proper absorption; the standard dose is two 300 mg tablets twice daily
- Favorable safety profile: Darolutamide has low blood-brain barrier penetration, potentially resulting in fewer central nervous system side effects compared to some alternatives
- Important drug interactions: Strong CYP3A4 inducers (such as rifampicin) may reduce NUBEQA effectiveness; inform your doctor about all medications
- Contraception required: Use effective contraception during treatment and for one week after the last dose to prevent potential harm to an unborn child
What Is NUBEQA and What Is It Used For?
NUBEQA (darolutamide) is a prescription androgen receptor inhibitor that blocks the activity of male sex hormones (androgens) to stop prostate cancer cells from growing. It is used to treat non-metastatic castration-resistant prostate cancer (nmCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC).
NUBEQA contains the active substance darolutamide, a next-generation nonsteroidal antiandrogen developed specifically to treat advanced prostate cancer. It received initial approval by the U.S. Food and Drug Administration (FDA) in 2019 for nmCRPC and subsequently gained approval for mHSPC in 2022. The European Medicines Agency (EMA) has also approved darolutamide for both indications across the European Union.
Prostate cancer is the second most commonly diagnosed cancer in men worldwide, with approximately 1.4 million new cases annually according to the World Health Organization (WHO). While many prostate cancers grow slowly and may not require aggressive treatment, some progress to more advanced stages where the cancer either no longer responds to standard hormone therapy (castration-resistant) or has spread to other parts of the body (metastatic).
NUBEQA is indicated for two distinct clinical scenarios in adult men:
- Non-metastatic castration-resistant prostate cancer (nmCRPC): The cancer has not spread to other parts of the body but no longer responds to medical or surgical treatments that lower testosterone levels. In this setting, NUBEQA is used alongside continued androgen deprivation therapy (ADT) to delay the cancer from spreading.
- Metastatic hormone-sensitive prostate cancer (mHSPC): The cancer has spread to other parts of the body but still responds to treatments that lower testosterone levels. In this setting, NUBEQA is used in combination with docetaxel chemotherapy and ADT to improve overall survival.
How Does NUBEQA Work?
NUBEQA works by blocking the androgen receptor, a protein found on the surface and inside prostate cancer cells. Under normal circumstances, androgens such as testosterone and dihydrotestosterone (DHT) bind to the androgen receptor, activating a signaling cascade that promotes cell growth and division. Even when testosterone levels are reduced through castration or medical ADT, residual androgens and adaptations within the cancer cells can continue to drive tumor growth through the androgen receptor pathway.
Darolutamide competitively inhibits the binding of androgens to the androgen receptor. This prevents the receptor from translocating into the cell nucleus, binding to DNA, and activating the transcription of genes that promote cancer cell proliferation. By blocking this critical signaling pathway, NUBEQA effectively inhibits the growth and survival of prostate cancer cells.
A distinguishing feature of darolutamide is its unique chemical structure, which results in low penetration of the blood-brain barrier. This pharmacological property may contribute to a more favorable central nervous system (CNS) safety profile compared to some other androgen receptor inhibitors, potentially reducing the risk of seizures, falls, and cognitive impairment. This characteristic has been highlighted in clinical studies and is considered a meaningful advantage in the treatment of elderly patients.
NUBEQA is always used in combination with ongoing ADT, which reduces testosterone production either through surgical castration (orchiectomy) or medical castration using GnRH agonists or antagonists. The combination of NUBEQA with ADT provides more complete androgen signaling blockade than ADT alone.
What Should You Know Before Taking NUBEQA?
Before starting NUBEQA, inform your doctor about any kidney or liver problems, heart conditions, or all other medications you are taking. NUBEQA must not be used by women, especially during pregnancy. Regular blood tests are recommended during treatment to monitor liver function.
Contraindications
NUBEQA should not be taken in the following circumstances:
- Hypersensitivity: If you are allergic to darolutamide or any of the other ingredients in NUBEQA (see the Ingredients section)
- Women who are or may become pregnant: NUBEQA is indicated only for use in adult men. Darolutamide may cause harm to a developing fetus and must not be taken by women
Warnings and Precautions
Before starting treatment with NUBEQA, it is essential to discuss your complete medical history with your healthcare provider. Special caution is advised in the following situations:
- Kidney problems: If you have impaired kidney function, your doctor may need to adjust your NUBEQA dose. Patients with severe renal impairment should be closely monitored
- Liver problems: Liver function should be assessed before starting treatment and monitored periodically during therapy. NUBEQA can affect liver function, and elevated liver enzymes (ALT, AST, bilirubin) have been reported in clinical trials. If blood tests show abnormal liver function values, your doctor may decide to permanently discontinue NUBEQA
- Heart conditions: Inform your doctor if you have any cardiovascular conditions, including heart rhythm problems (arrhythmias), coronary artery disease, or heart failure. Cardiovascular events including ischemic heart disease and cardiac failure have been observed in patients taking NUBEQA
- History of vascular surgery: If you have undergone surgery to treat blood vessel diseases, your doctor should be informed
- Bone health: Androgen deprivation therapy (which is used alongside NUBEQA) is associated with decreased bone mineral density and increased fracture risk. Bone fractures have been reported in patients receiving NUBEQA. Your doctor may recommend bone density monitoring and supplementation with calcium and vitamin D
NUBEQA can affect liver function. Your doctor will perform blood tests before and during treatment to monitor liver enzymes. Report any symptoms of liver problems immediately, including unexplained nausea, vomiting, abdominal pain, fatigue, loss of appetite, dark urine, or yellowing of the skin or eyes (jaundice).
Pregnancy, Fertility, and Breastfeeding
NUBEQA is intended for use in adult male patients only and must not be used by women.
Effects on male fertility: Darolutamide may reduce male fertility. Based on its mechanism of action as an androgen receptor inhibitor, NUBEQA may impair spermatogenesis and male reproductive function. Men who wish to father children should discuss fertility preservation options with their healthcare provider before starting treatment.
During treatment with NUBEQA and for one week after the last dose, the following precautions must be observed:
- Use a condom or other highly effective method of contraception during sexual intercourse with a woman of childbearing potential, to prevent pregnancy
- Use a condom during sexual intercourse with a pregnant woman, to protect the unborn child from potential exposure to darolutamide through seminal fluid
Children and Adolescents
NUBEQA should not be used in children and adolescents under 18 years of age. Prostate cancer does not occur in this age group, and the safety and efficacy of darolutamide have not been established in pediatric patients.
Driving and Operating Machinery
NUBEQA is unlikely to affect your ability to drive or use machines. However, fatigue is a common side effect. If you experience fatigue or any other symptoms that could impair your concentration or reaction time, exercise caution when driving or operating machinery.
NUBEQA contains lactose monohydrate as an excipient. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
How Does NUBEQA Interact with Other Drugs?
NUBEQA can interact with several medications. Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin) may reduce its effectiveness. NUBEQA may increase blood levels of certain drugs including rosuvastatin, methotrexate, and sulfasalazine. Always inform your doctor about all medicines you take.
Drug interactions are a critical consideration when taking NUBEQA. Darolutamide is metabolized primarily by CYP3A4 and also acts as an inhibitor of the breast cancer resistance protein (BCRP) and organic anion transporting polypeptide (OATP) 1B1/1B3 transporters. These properties can lead to clinically significant interactions with other medications.
It is essential to inform your healthcare provider and pharmacist about all medicines you are currently taking, have recently taken, or plan to take, including over-the-counter medications, herbal supplements, and vitamins.
Drugs That May Reduce NUBEQA Effectiveness
The following drugs are strong inducers of CYP3A4 and may significantly reduce darolutamide exposure (blood levels), potentially decreasing its anticancer activity:
| Drug | Common Use | Interaction Type | Clinical Impact |
|---|---|---|---|
| Rifampicin | Bacterial infections (tuberculosis) | Strong CYP3A4 inducer | May significantly reduce darolutamide exposure |
| Carbamazepine | Epilepsy, neuropathic pain | Strong CYP3A4 inducer | May significantly reduce darolutamide exposure |
| Phenobarbital | Epilepsy | Strong CYP3A4 inducer | May significantly reduce darolutamide exposure |
| Phenytoin | Epilepsy | Strong CYP3A4 inducer | May significantly reduce darolutamide exposure |
| St. John’s Wort | Mild depression and anxiety (herbal) | Strong CYP3A4 inducer | May significantly reduce darolutamide exposure |
Drugs Whose Levels May Be Increased by NUBEQA
NUBEQA inhibits BCRP and OATP1B1/1B3 transporters, which may increase the blood levels of medications that are substrates of these transporters. Your doctor may need to adjust the dose of the following medications:
| Drug | Common Use | Transporter | Recommendation |
|---|---|---|---|
| Rosuvastatin | High cholesterol | BCRP / OATP1B1 | Monitor for statin-related side effects; dose adjustment may be needed |
| Fluvastatin | High cholesterol | BCRP / OATP1B1 | Monitor for statin-related side effects |
| Atorvastatin | High cholesterol | OATP1B1 | Monitor for statin-related side effects |
| Pitavastatin | High cholesterol | OATP1B1 | Monitor for statin-related side effects |
| Methotrexate | Severe arthritis, psoriasis, cancer | BCRP / OATP1B1 | Monitor methotrexate levels; dose adjustment may be needed |
| Sulfasalazine | Inflammatory bowel disease | BCRP | Monitor for increased sulfasalazine effects |
Always bring a complete list of your current medications to every medical appointment. This includes prescription drugs, over-the-counter medicines, vitamins, supplements, and herbal products. Do not start, stop, or change the dose of any medication without consulting your prescribing oncologist first.
What Is the Correct Dosage of NUBEQA?
The recommended dose of NUBEQA is 600 mg (two 300 mg tablets) taken twice daily, for a total daily dose of 1,200 mg. Tablets should be swallowed whole with food and a glass of water. Your doctor may reduce the dose to 300 mg twice daily if you have liver or kidney problems.
Always take NUBEQA exactly as your doctor or pharmacist has told you. Do not change your dose or stop taking NUBEQA without first consulting your healthcare provider.
Standard Adult Dosage
Recommended Dose
600 mg (two 300 mg tablets) taken orally twice daily
Total daily dose: 1,200 mg (four tablets per day)
Take with food and a glass of water. Swallow tablets whole – do not crush, split, or chew.
The tablets should be taken at approximately the same times each day, roughly 12 hours apart (e.g., morning and evening with meals). Taking NUBEQA with food is important because food increases the absorption of darolutamide, ensuring that the drug reaches therapeutic levels in the blood.
Dose Adjustments
| Patient Group | Recommended Dose | Notes |
|---|---|---|
| Standard dose (adults) | 600 mg (2 tablets) twice daily | Total 1,200 mg/day; take with food |
| Hepatic impairment (moderate) | 300 mg (1 tablet) twice daily | Total 600 mg/day; monitor liver function |
| Renal impairment (severe) | 300 mg (1 tablet) twice daily | Total 600 mg/day; monitor renal function |
| Elderly patients | 600 mg (2 tablets) twice daily | No dose adjustment needed based on age alone |
| Children (<18 years) | Not applicable | NUBEQA is not indicated for pediatric use |
What to Do If You Miss a Dose
If you forget to take a dose of NUBEQA, take it as soon as you remember, provided it is before your next scheduled dose. Do not take a double dose to make up for a forgotten dose. Simply continue with your regular dosing schedule at the next planned time.
Overdose
If you take more NUBEQA than prescribed, continue with your treatment as planned with your next scheduled dose. There is no specific antidote for darolutamide overdose. In clinical trials, no dose-limiting toxicities were observed at doses up to 1,800 mg daily. However, if you suspect you have taken significantly more than prescribed, contact your healthcare provider or local poison control center for guidance.
Stopping Treatment
Do not stop taking NUBEQA unless your doctor tells you to. Prostate cancer treatment typically requires continuous medication to maintain disease control. Discontinuing treatment without medical advice could lead to disease progression. If you experience side effects that concern you, discuss them with your oncologist, who can advise on the best course of action, which may include dose adjustment rather than treatment discontinuation.
What Are the Side Effects of NUBEQA?
The most common side effects of NUBEQA include fatigue, decreased white blood cell count (neutropenia), and elevated liver enzymes. Common side effects include coronary artery blockage, heart failure, rash, limb pain, and bone fractures. When combined with docetaxel, high blood pressure and rash are also very common.
Like all medicines, NUBEQA can cause side effects, although not everybody gets them. Most side effects are manageable with appropriate medical care, and your healthcare team will monitor you regularly during treatment. It is important to report any new or worsening symptoms to your doctor promptly.
NUBEQA Monotherapy Side Effects
The following side effects have been reported in clinical trials of NUBEQA when used as monotherapy (without docetaxel):
Very Common
- Fatigue (feeling tired or lacking energy)
- Decreased neutrophil count (a type of white blood cell important for fighting infection, detected by blood tests)
- Elevated bilirubin levels (detected by blood tests, indicating liver function changes)
- Elevated ALT – alanine aminotransferase (liver enzyme detected by blood tests)
- Elevated AST – aspartate aminotransferase (liver enzyme detected by blood tests)
Common
- Coronary artery blockage (ischemic heart disease)
- Heart failure
- Skin rash
- Pain in arms and legs (extremity pain)
- Bone fractures
Side Effects When Combined with Docetaxel
When NUBEQA is used in combination with docetaxel for metastatic hormone-sensitive prostate cancer (mHSPC), the following additional or more frequent side effects have been observed:
Very Common (with Docetaxel)
- High blood pressure (hypertension)
- Skin rash
- Decreased neutrophil count (neutropenia)
- Elevated bilirubin levels
- Elevated ALT (alanine aminotransferase)
- Elevated AST (aspartate aminotransferase)
Common (with Docetaxel)
- Bone fractures
- Gynecomastia (breast enlargement in men)
Contact your doctor or go to the emergency department immediately if you experience: chest pain or tightness, sudden shortness of breath, swelling in your legs or ankles, rapid or irregular heartbeat, signs of severe liver problems (yellowing of skin or eyes, dark urine, severe abdominal pain), or signs of infection (high fever, chills, severe sore throat) especially if blood tests have shown low white blood cell counts.
Reporting Side Effects
If you experience any side effects, including any not listed here, talk to your doctor or pharmacist. You can also report side effects directly to your national medicines regulatory authority. By reporting side effects, you can help provide more information on the safety of this medicine.
How Should You Store NUBEQA?
Store NUBEQA at room temperature. Keep the medicine out of the sight and reach of children. Do not use after the expiry date printed on the carton and blister pack. No special storage conditions are required.
Proper storage of NUBEQA helps ensure the medication remains effective and safe throughout its shelf life. Follow these guidelines:
- Keep out of reach of children: Store NUBEQA in a secure location where children cannot access it
- Check the expiry date: Do not use NUBEQA after the expiry date stated on the carton and on each blister after “EXP.” The expiry date refers to the last day of that month
- No special storage conditions: NUBEQA does not require any special temperature or humidity conditions for storage
- Keep in original packaging: Store the tablets in their original blister packaging to protect them from moisture and light
- Proper disposal: Do not throw away medicines via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. These measures help to protect the environment
Package Information
NUBEQA film-coated tablets are white to off-white, oval in shape, measuring 16 mm long and 8 mm wide. They are debossed with “300” on one side and “BAYER” on the other side. Each carton contains 112 film-coated tablets in 7 blisters, with each blister containing 16 tablets. This provides a 28-day (4-week) supply at the standard dose.
What Does NUBEQA Contain?
Each NUBEQA tablet contains 300 mg of darolutamide as the active substance, along with inactive ingredients including calcium hydrogen phosphate, croscarmellose sodium, hypromellose, lactose monohydrate, macrogol, magnesium stearate, povidone, and titanium dioxide.
Active Ingredient
The active substance in NUBEQA is darolutamide. Each film-coated tablet contains exactly 300 mg of darolutamide. Darolutamide is a nonsteroidal androgen receptor inhibitor with the molecular formula C19H19ClN2O2. It exists as a mixture of two diastereomers, (S,R)-darolutamide and (S,S)-darolutamide, which interconvert in vivo.
Inactive Ingredients (Excipients)
The following inactive ingredients are included in NUBEQA tablets:
- Tablet core: Calcium hydrogen phosphate (E 341), croscarmellose sodium, magnesium stearate (E 470b), povidone (E 1201), lactose monohydrate
- Film coating: Hypromellose, macrogol (E 1521), titanium dioxide (E 171)
NUBEQA tablets contain lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption should not take this medicine. Discuss with your doctor if you have been diagnosed with any sugar intolerance.
Frequently Asked Questions about NUBEQA
References and Medical Sources
All information in this article is based on internationally recognized medical guidelines, regulatory documents, and peer-reviewed clinical research:
- European Medicines Agency (EMA). NUBEQA (darolutamide) – Summary of Product Characteristics. Available at: www.ema.europa.eu. Last updated 2025.
- U.S. Food and Drug Administration (FDA). NUBEQA (darolutamide) prescribing information. Approved 2019 (nmCRPC), 2022 (mHSPC).
- Fizazi K, Shore N, Tammela TL, et al. Darolutamide in Nonmetastatic, Castration-Resistant Prostate Cancer (ARAMIS trial). N Engl J Med. 2019;380(13):1235-1246. doi:10.1056/NEJMoa1815671
- Smith MR, Hussain M, Saad F, et al. Darolutamide and Survival in Metastatic, Hormone-Sensitive Prostate Cancer (ARASENS trial). N Engl J Med. 2022;386(12):1132-1142. doi:10.1056/NEJMoa2119115
- National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Prostate Cancer. Version 4.2025.
- Parker C, Castro E, Fizazi K, et al. Prostate cancer: ESMO Clinical Practice Guidelines. Ann Oncol. 2020;31(9):1119-1134. doi:10.1016/j.annonc.2020.06.011
- World Health Organization (WHO). Cancer Fact Sheet: Prostate Cancer. 2024. Available at: www.who.int
- Moilanen AM, Riikonen R, Oksala R, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor. Sci Rep. 2015;5:12007. doi:10.1038/srep12007
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