Initial US Approval:

2019

Key Clinical Studies:

ARANOTE (NCT02799602)

Drug Class/Description:

Androgen receptor inhibitor

Indications and Usage:

NUBEQA is an androgen receptor inhibitor indicated for the treatment of adult patients with:

• non-metastatic castration-resistant prostate cancer (nmCRPC).
• metastatic castration-sensitive prostate cancer (mCSPC).
• metastatic castration-sensitive prostate cancer (mCSPC) in combination with docetaxel. 

Dosage and Administration:

Recommended Dosage: NUBEQA 600 mg (two 300 mg tablets) administered orally twice daily. Swallow tablets whole. Take NUBEQA with food.

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.

Patients should also receive a gonadotropin-releasing hormone (GnRH) agonist or antagonist concurrently or have had bilateral orchiectomy. 

Dosage Forms and Strengths:

Tablets: 300 mg

Contraindications:

None.

Warnings and Precautions:

• Ischemic Heart Disease: Optimize management of cardiovascular risk factors. Monitor for signs and symptoms of coronary artery disease. Discontinue NUBEQA for Grade 3-4 events. 
• Seizure: Consider discontinuation of NUBEQA in patients who develop a seizure during treatment.
• Embryo-Fetal Toxicity: NUBEQA can cause fetal harm and loss of pregnancy. Advise males with female partners of reproductive potential to use effective contraception. 

Adverse Reactions:

In nmCRPC and mCSPC: The most common adverse reactions (>10% with a ≥2% increase over placebo), including laboratory test abnormalities, are increased AST, decreased neutrophil count, increased bilirubin, fatigue, and increased ALT.

In mCSPC in combination with docetaxel: The most common adverse reactions (≥10% with a ≥2% increase over placebo) are constipation, rash, decreased appetite, hemorrhage, increased weight, and hypertension.  The most common laboratory test abnormalities (≥30%) are anemia, hyperglycemia, decreased lymphocyte count, decreased neutrophil count, increased AST, increased ALT, and hypocalcemia. 

Drug Interactions:

• Combined P-gp and Strong or Moderate CYP3A Inducers: Avoid concomitant use. 
• Combined P-gp and Strong CYP3A Inhibitors: Monitor patients more frequently for NUBEQA adverse reactions.
• BCRP Substrates: 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.
• 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. 

Use in Specific Populations:

• Severe Renal Impairment (not on hemodialysis): Recommended dose is 300 mg twice daily. 
• Moderate Hepatic Impairment: Recommended dose is 300 mg twice daily.

Adapted From:

https://labeling.bayerhealthcare.com/html/products/pi/Nubeqa_PI.pdf?inline=

 

Every health-care provider should make their own determination regarding specific safe and appropriate patient care practices, including drug dosages and indications. The provider should always consult the most recent prescribing/product information. FDA Focus information is not guaranteed to be accurate, complete, or current. JADPRO and its editors, authors, reviewers, and commentators cannot be held responsible for any liability incurred as a consequence of the application of any of the information listed within.