Medically reviewed by Drugs.com. Last updated on July 25, 2020.
(DAR oh LOO ta mide)
- BAY 1841788
- ODM 201
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Nubeqa: 300 mg
Brand Names: U.S.
- Antineoplastic Agent, Antiandrogen
Darolutamide is a competitive androgen receptor inhibitor. In addition to androgen binding inhibition, darolutamide also inhibits androgen receptor translocation and androgen receptor-mediated transcription. Keto-darolutamide (active metabolite) has similar in vitro activity to darolutamide. Androgen receptor inhibition results in decreased proliferation of prostate tumor cells and increased apoptosis, leading to a decrease in tumor volume.
119 L; darolutamide has low blood-brain barrier penetration (Fizazi 2019).
Primarily metabolized by CYP3A4, as well as by UGT1A9 and UGT1A1; active metabolite is keto-darolutamide.
Urine: 63.4% (~7% as unchanged drug); feces: 32.4% (~30% as unchanged drug); Clearance: 116 mL/minute.
Time to Peak
~20 hours (darolutamide and keto-darolutamide).
Darolutamide: 92%; keto-darolutamide (active metabolite): 99.8%; primarily to serum albumin.
Special Populations: Renal Function Impairment
Darolutamide exposure was increased by ~2.5-fold in noncancer subjects with severe renal impairment (eGFR 15 to 29 mL/minute/1.73 m2) not receiving dialysis as compared to healthy subjects.
Special Populations: Hepatic Function Impairment
Darolutamide exposure was increased by ~1.9-fold in noncancer subjects with moderate (Child Pugh class B) hepatic impairment as compared to healthy subjects.
Use: Labeled Indications
Prostate cancer, nonmetastatic, castration-resistant: Treatment of nonmetastatic castration-resistant prostate cancer.
There are no contraindications listed in the US manufacturer's labeling.
Canadian labeling: Hypersensitivity to darolutamide or any component of the formulation.
Prostate cancer, nonmetastatic, castration-resistant: Oral: 600 mg twice daily (in combination with a gonadotropin-releasing hormone analog [if had not received bilateral orchiectomy]); continue until disease progression or unacceptable toxicity (Fizazi 2019).
Missed dose: If a dose is missed, administer as soon as possible prior to the next scheduled dose; do not take 2 doses at the same time to make up for a missed dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Refer to adult dosing.
Dosing: Adjustment for Toxicity
Grade 3 or higher toxicity (or intolerable adverse reaction): Withhold darolutamide or reduce dose to 300 mg twice daily until symptoms improve; may then resume therapy at 600 mg twice daily. Dose reduction <300 mg twice daily is not recommended.
Oral: Administer with food. Swallow tablets whole.
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). Keep the bottle tightly closed after initial opening.
Alpelisib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Consider therapy modification
Asunaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Asunaprevir. Avoid combination
Cladribine: BCRP/ABCG2 Inhibitors may increase the serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Consider therapy modification
CloZAPine: CYP3A4 Inducers (Weak) may decrease the serum concentration of CloZAPine. Monitor therapy
Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Avoid combination
Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Avoid combination
Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with OATP1B1/1B3 inhibitors and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification
Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Grazoprevir. Avoid combination
Inducers of CYP3A4 (Moderate) and P-glycoprotein: May decrease the serum concentration of Darolutamide. Avoid combination
Inducers of CYP3A4 (Strong) and P-glycoprotein: May decrease the serum concentration of Darolutamide. Avoid combination
Inhibitors of CYP3A4 (Strong) and P-glycoprotein: May increase the serum concentration of Darolutamide. Monitor therapy
NiMODipine: CYP3A4 Inducers (Weak) may decrease the serum concentration of NiMODipine. Monitor therapy
Ozanimod: BCRP/ABCG2 Inhibitors may increase serum concentrations of the active metabolite(s) of Ozanimod. Avoid combination
PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Avoid combination
Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Avoid combination
Rimegepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Rimegepant. Avoid combination
Rosuvastatin: Darolutamide may increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 5 mg daily when combined with darolutamide. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Consider therapy modification
Selpercatinib: CYP3A4 Inducers (Weak) may decrease the serum concentration of Selpercatinib. Monitor therapy
Tacrolimus (Systemic): CYP3A4 Inducers (Weak) may decrease the serum concentration of Tacrolimus (Systemic). Monitor therapy
Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Monitor therapy
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Avoid combination
Ubrogepant: CYP3A4 Inducers (Weak) may decrease the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 100 mg and second dose (if needed) of 100 mg when used with a weak CYP3A4 inducer. Consider therapy modification
Ubrogepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Consider therapy modification
Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Avoid combination
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Central nervous system: Fatigue (16%)
Hematologic & oncologic: Neutropenia (20%; grade 3/4 4%)
Hepatic: Increased serum aspartate aminotransferase (20%), increased serum bilirubin (16%)
Neuromuscular & skeletal: Asthenia (≤16%)
1% to 10%:
Cardiovascular: Ischemic heart disease (4%), cardiac failure (2%)
Dermatologic: Skin rash (3%)
Neuromuscular & skeletal: Limb pain (6%)
Frequency not defined:
Genitourinary: Hematuria, urinary retention
Concerns related to adverse effects:
• Bone marrow suppression: Neutropenia was observed more frequently with darolutamide than placebo in a clinical trial, although the incidence was not high.
• Cardiovascular disease: Androgen-deprivation therapy may increase the risk for cardiovascular disease (Levine 2010).
• Hepatic impairment: Patients with moderate hepatic impairment (Child-Pugh class B) have increased darolutamide exposure; dose reduction is recommended.
• Renal impairment: Patients with severe renal impairment (eGFR 15 to 29 mL/minute/1.73 m2) who are not receiving hemodialysis have increased darolutamide exposure; dose reduction is recommended.
Monitor hepatic and renal function as clinically necessary. Monitor adherence.
Males with female partners of reproductive potential should use effective contraception during darolutamide treatment and for 1 week after the last darolutamide dose.
Based on the mechanism of action, darolutamide may cause fetal harm and pregnancy loss if utero exposure occurs.
What is this drug used for?
• It is used to treat prostate cancer.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Loss of strength and energy
• Pain in arms or legs
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
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More about darolutamide
- Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- En Español
- Drug class: antiandrogens
Other brands: Nubeqa