darolutamide

High Alert

Nonmetastatic castration resistant prostate cancer.
Metastatic hormone-sensitive prostate cancer (as monotherapy or in combination with docetaxel).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

End-stage renal disease;
Severe hepatic impairment.

Use Cautiously in:

Severe renal impairment (↓ dose);
Moderate hepatic impairment (↓ dose);
Rep: Men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: HF, ISCHEMIC HEART DISEASE

Derm: rash

GI: ↑liver enzymes, hyperbilirubinemia

Hemat: neutropenia

Neuro: fatigue, SEIZURES

Interactions ⬆ ⬇

Drug-drug:

Combined P-glycoprotein and strong or moderate CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.
Combined P-glycoprotein and strong CYP3A4 inhibitors, including itraconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
May ↑ levels and risk of toxicity of breast cancer resistance protein substrates, including rosuvastatin; avoid concurrent use.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

Patients should also be taking a gonadotropin-releasing hormone (GnRH) analog or should have undergone a bilateral orchiectomy.
PO (Adults ): 600 mg twice daily; continue until disease progression or unacceptable toxicity.

Renal Impairment

PO (Adults ): CCr 15–29 mL/min: 300 mg twice daily; continue until disease progression or unacceptable toxicity.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: 300 mg twice daily; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as an androgen receptor inhibitor, preventing the binding of androgen; decreases proliferation and induces cell death of prostate cancer cells.

Therapeutic effects:

Decreased growth and spread of prostate cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: androgen receptor inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 30% absorbed following oral administration; absorption ↑ with food.

Distribution: Extensively distributed to tissues.

Protein Binding: Darolutamide: 92%; Keto-darolutamide: 99.8%.

Metabolism/Excretion: Primarily metabolized in the liver by the CYP3A4 isoenzyme as well as by UGT1A1 and UGT1A9 to an active metabolite (keto-darolutamide). Primarily excreted in urine (63%, 7% as unchanged drug) and 32% excreted in feces (30% as unchanged drug).

Half-Life: 20 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient to take missed dose as soon as remembered, but do not double doses.
Advise patient that therapy may ↑ risk of seizures. Avoid activities where a sudden loss of consciousness could cause serious harm to self or others. Notify health care provider immediately if seizure symptoms occur.
Advise patient to immediately notify health care provider of chest pain or difficulty breathing.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Rep: May cause fetal harm. Advise men with female partners of reproductive potential to use effective contraception for 1 wk after last dose. Inform patient that darolutamide may impair fertility.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

50419- Bayer HealthCare Pharmaceuticals Inc.
- 50419-395- NUBEQA
  - 50419-395-01- 1 BOTTLE in 1 CARTON (50419-395-01) / 120 TABLET, FILM COATED in 1 BOTTLE

50419- Bayer HealthCare Pharmaceuticals Inc.
- 50419-395- NUBEQA
  - 50419-395-72- 1 BOTTLE in 1 CARTON (50419-395-72) / 120 TABLET, FILM COATED in 1 BOTTLE

52483- Orion Corporation, ORION PHARMA
- 52483-6300-
  - 52483-6300-0- 120 BOTTLE in 1 CASE (52483-6300-0) / 120 TABLET in 1 BOTTLE

54893- MSN Laboratories Private Limited
- 54893-0107-
  - 54893-0107-1- 50 kg in 1 DRUM (54893-0107-1)

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Indications ⬇