darolutamide: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
darolutamide: clinical details
Prescribing considerations
- Initiate and supervise treatment through a clinician experienced in prostate-cancer management.
- Review renal and hepatic function; exposure may increase with severe renal or moderate hepatic impairment.
- Assess cardiovascular disease, modifiable cardiovascular risks and seizure history.
- Review interacting medicines, herbal products and QT-prolonging therapy.
Contraindications and cautions
- Hypersensitivity to darolutamide or an excipient.
- Women who are or may become pregnant.
- The selected product contains lactose and should not be used in specified rare hereditary disorders of galactose handling.
Monitoring
- Monitor for symptoms of ischaemic heart disease, heart failure and seizure.
- Assess liver function when clinically indicated and investigate possible drug-induced liver injury.
- Monitor blood pressure, blood counts and liver tests, particularly with docetaxel.
- Monitor for toxicity from BCRP, OATP1B1 or OATP1B3 substrates.
Clinical pharmacology
Darolutamide and its active keto metabolite inhibit androgen binding, receptor nuclear translocation and androgen-receptor-mediated transcription. Food substantially increases oral bioavailability. Metabolism involves CYP3A4 and UGT pathways, and darolutamide is a substrate of P-glycoprotein and BCRP.
Formulation and product differences
- The selected product is a film-coated oral tablet that must be swallowed whole with food.
- It contains lactose monohydrate.
darolutamide preparations and strengths
Tablet
Route: Oral
Strengths: 300 mg
darolutamide interactions
Review prescription, non-prescription and herbal products before treatment. Important examples include:
Rifampicin, carbamazepine, phenobarbital, phenytoin and St John's wort
These can substantially reduce darolutamide exposure, so alternatives should be considered.
Rosuvastatin
Darolutamide can markedly increase rosuvastatin exposure; concurrent use should generally be avoided unless no suitable alternative exists.
Atorvastatin, fluvastatin, pitavastatin, methotrexate and sulfasalazine
Darolutamide may increase their concentrations, requiring adverse-effect monitoring.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.