Darolutamide is a highly selective androgen receptor (AR) inhibitor that inhibits the proliferation of prostate cancer cells by competitively suppressing androgen binding, blocking AR nuclear translocation, and AR mediated transcription processes.

1、 Drug name

1. Common name: Darolutamide

2. Product Name: NUBEQA ®

2、 Indications

Used to treat adult male prostate cancer patients:

1. Non metastatic castration resistant prostate cancer (nmCRPC).

2. Metastatic castration sensitive prostate cancer (mCSPC) can be used alone or in combination with docetaxel.

3、 Specifications

Specification: 300mg per piece.

4、 Main components

Active ingredient: Daretamide.

5、 Usage and dosage

1. Recommended dosage: 600mg each time (2 tablets 300mg), twice daily, orally.

2. It should be taken with food and swallowed whole.

3. Simultaneously receiving treatment with gonadotropin-releasing hormone agonists/antagonists or having undergone bilateral orchidectomy.

4. If used in combination with docetaxel, the first cycle of docetaxel treatment should be initiated within 6 weeks after starting treatment with darotamine.

6、 Dose adjustment

1. If there are grade 3 or intolerable adverse reactions, the medication should be suspended or reduced to 300mg twice daily until symptoms improve.

2. For patients with severe renal dysfunction (eGFR15-29mL/min/1.73m ², non dialysis patients) or moderate liver dysfunction (Child Pugh B grade), the recommended dose is 300mg twice daily.

3. If ischemic heart disease or epilepsy occurs, dosage adjustment or discontinuation of medication may be necessary.

7、 Medication precautions

1. Before and after meals: must be taken with food to increase bioavailability.

2. Missed dose: If missed, it should be taken as soon as possible before the next scheduled medication, and double the dose should not be taken at the same time.

3. Vomiting: If vomiting occurs after taking medication, there is no need to take additional doses, and the next dose should be taken according to the original plan.

8、 Medication for special populations

1. Renal insufficiency: mild to moderate without dose adjustment; Severe renal insufficiency (non dialysis) requires a reduction to 300mg twice daily.

2. Liver dysfunction: mild without adjustment; Moderate dosage should be reduced to 300mg twice a day; There is no data available for severe (Child Pugh C grade).

3. Elderly: No need to adjust dosage.

4. Pregnant and lactating women: not applicable to females; The female partner of male patients should take effective contraceptive measures during the treatment period and one week after the last dose.

5. Children: Safety and efficacy have not yet been determined.

9、 Adverse reactions

1. Common adverse reactions (>10%): elevated AST, decreased neutrophil count, elevated bilirubin, fatigue, elevated ALT.

2. Common adverse reactions when used in combination with docetaxel include constipation, rash, decreased appetite, bleeding, weight gain, and hypertension.

3. Serious adverse reactions include ischemic heart disease, epilepsy, and embryo fetal toxicity.

10、 Contraindications

There are no known contraindications.

11、 Drug interactions

1. Avoid co administration with P-glycoprotein and strong/moderate CYP3A4 inducers.

2. When combined with P-glycoprotein and strong CYP3A4 inhibitors, it is necessary to strengthen adverse reaction monitoring.

3. Avoid co administration with BCRP substrate drugs, and if co administration is necessary, monitor and consider reducing dosage.

4. When combined with OATP1B1/OATP1B3 substrates, it may increase their blood drug concentration, which needs to be monitored and considered for reduction.

12、 Storage method

1. Stored at 20 ° C-25 ° C (68 ° F-77 ° F), short-term storage between 15 ° C-30 ° C (59 ° F-86 ° F) is allowed.

2. After opening the bottle for the first time, the cap should be tightly closed and kept out of reach of children.

Darolutamidinformation