NUBEQA Film-coated tablet (2019)

Βιβλιογραφική αναφορά

Συγγραφείς

Bayer HealthCare Pharmaceuticals Inc.

Λέξεις κλειδιά

50419-395

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1. Indications and Usage

NUBEQA is indicated for the treatment of patients with non-metastatic castration resistant prostate cancer (nmCRPC).

2. Dosage and Administration

2.1 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. Swallow tablets whole with food ...

3. Dosage Forms and Strengths

Tablets (300 mg): white to off-white oval film-coated tablets marked with 300 on one side and Bayer on the other.

4. Contraindications

None.

5. Warnings and Precautions

5.1 Embryo-Fetal Toxicity 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 when administered to ...

6. Adverse Reactions

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

7. Drug Interactions

7.1 Effects of Other Drugs on NUBEQA Combined P-gp and Strong or Moderate CYP3A4 Inducer Concomitant use of NUBEQA with a combined P-gp and strong or moderate CYP3A4 inducer decreases darolutamide exposure ...

8.1. Pregnancy

Risk Summary 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 [see Clinical Pharmacology (12.1)] ...

8.2. Lactation

Risk Summary The safety and efficacy of NUBEQA have not been established in females. There are no data on the presence of darolutamide or its metabolites in human milk, the effect on the breastfed child, ...

8.3. Females and Males of Reproductive Potential

Contraception Males 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 ...

8.4. Pediatric Use

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

8.5. Geriatric Use

Of the 954 patients who received NUBEQA in ARAMIS, 88% of patients were 65 years and over, and 49% were 75 years and over. No overall differences in safety or efficacy were observed between these patients ...

8.6. Renal Impairment

Patients with severe renal impairment (eGFR 15–29 mL/min/1.73 m² who are not receiving hemodialysis have a higher exposure to NUBEQA and reduction of the dose is recommended [see Dosage and Administration ...

8.7. Hepatic Impairment

Patients with moderate hepatic impairment (Child-Pugh Class B) have a higher exposure to NUBEQA and reduction of the dose is recommended [see Dosage and Administration (2.4) and Clinical Pharmacology ...

10. Overdosage

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 ...

11. Description

NUBEQA is an androgen receptor inhibitor. The chemical name is N-{(2S)1[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propan-2-yl}5(1-hydroxyethyl)-1H-pyrazole-3-carboxamide. The molecular weight is 398.85 ...

12.1. Mechanism of Action

Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription. A major metabolite, keto-darolutamide, ...

12.2. Pharmacodynamics

Darolutamide exposure at 600 mg twice daily results in PSA mean reduction of more than 90% from baseline. Cardiac Electrophysiology The effect of darolutamide (600 mg twice daily) on the QTc interval was ...

12.3. Pharmacokinetics

Following administration of 600 mg twice daily, darolutamide mean (CV) steady-state peak plasma concentration (Cmax) is 4.79 mg/L (30.9) and area under the plasma concentration-time curve from ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term animal studies to evaluate the carcinogenic potential of darolutamide have not been conducted. Darolutamide was clastogenic in an in vitro chromosome aberration assay in human peripheral ...

14. Clinical Studies

ARAMIS (NCT02200614) was a multicenter, double-blind, placebo-controlled clinical trial in 1509 patients with non-metastatic castration resistant prostate cancer with a prostate-specific antigen doubling ...

16.1. How Supplied

NUBEQA (darolutamide) 300 mg film-coated tablets are white to off-white, oval shaped tablets, marked with 300 on one side, and BAYER on the other side. NUBEQA 300 mg tablets are available in bottles of ...

16.2. Storage and Handling

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature]. Keep the bottle tightly closed after first opening.

17. Patient Counseling Information

Dosage and Administration Inform patients receiving concomitant gonadotropin-releasing hormone (GnRH) analog therapy that they need to maintain this treatment during the course of treatment with NUBEQA. ...