Products
Apalutamide was approved in the US and EU in 2018 and in many countries in 2019 in film-coated tablet form (Erleada).
Structure and properties
Apalutamide (C21H15F4N5O2S, Mr = 477.4 g/mol) exists as a white to slightly yellow powder that is practically insoluble in water. The active metabolite -demethylapalutamide is also active, but more weakly than the parent compound.
Effects
Apalutamide (ATC L02BB05) has antiandrogenic properties. The effects are due to antagonism at the binding site of the androgen receptor. This prevents the interaction of the androgen receptor with DNA.
Indications
For the treatment of nonmetastatic castration-resistant prostate cancer (NM-CRPC).
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
Apalutamide is harmful to fertility (teratogenic) and is contraindicated during pregnancy and in women of childbearing potential. For complete precautions, see the drug label.
Interactions
Apalutamide is a substrate of CYP2C8 and CYP3A4.
Adverse effects
The most common potential adverse effects include fatigue, hypertension, rash, diarrhea, nausea, weight loss, falls, flushing, poor appetite, fractures, and peripheral edema.
