Nubeqa

Instructions for Darolutamide Film Tablets

Common name: Darolutamide
Trade name: Nubeqa
Full names: Darolutamide Film Tablets, Darolutamide, Darolutamide, Nubeqa,

Indications:
NUBEQA is an androgen receptor inhibitor, suitable for the treatment of patients with non-metastatic castration-resistant prostate cancer.

Dosage:
The recommended dose is 600 mg (two 300 mg tablets) taken orally twice daily.
Swallow tablet whole. Take with food.

Adverse Reactions:
The most common adverse reactions (≥2%) are fatigue, pain in extremities, and cramping.

Taboos:
None.

Precautions:
Embryo-Fetal Toxicity: NUBEQA can cause fetal injury and loss of pregnancy. Men with female partners of reproductive potential are advised to use effective contraception.

Storage:
Store at 20°C to 25°C (68°F to 77°F), with an allowable deviation of 15°C to 30°C (59°F to 86°F)
Keep the bottle tightly closed after first opening.

Mechanism of action:
Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription. The major metabolite ketone, darotadine, exhibits similar in vitro activity to todarolutamide. In addition, darolutamide acts as a progesterone receptor (PR) antagonist in vitro (approximately 1% activity compared to AR). In a mouse xenograft model of prostate cancer, Darolutamide reduces in vitro prostate cancer cell proliferation and tumor volume.

Safety and efficacy: The FDA approved the marketing of darolutamide based on its performance in the Phase 3 clinical trial called ARAMIS. The trial results showed that compared with placebo combined with androgen deprivation therapy (ADT), darolutamide combined with ADT significantly improved metastasis-free survival (MFS) (HR=0.41, 95% CI 0.34-0.50; P<0.001), which meant that the patient's risk of metastasis or death was reduced by 59%.
The median MFS in the Darolutamide combined ADT treatment group was 40.4 months, compared with 18.4 months in the placebo group, and the overall median MFS improvement was 22 months. A positive trend in overall survival (OS) was observed (HR=0.71, 95% CI 0.50-0.99; P=0.045), and all other secondary endpoints favored darolutamide.