Abiraterone Acetate

Products Abiraterone is commercially available in the form of film-coated tablets (Zytiga). It has been approved in many countries since 2011. Structure and properties Abiraterone acetate (C26H33NO2, Mr = 391.5 g/mol) exists as a white crystalline powder that is practically insoluble in water. It is a prodrug and is rapidly biotransformed in the body to … Abiraterone Acetate

Darolutamide

Products Darolutamide was approved in the US in 2019 and in the EU and Switzerland in 2020 in film-coated tablet form (Nubeqa). Structure and properties Darolutamide (C19H19ClN6O2, Mr = 398.8 g/mol) exists as a white to grayish or yellowish-white crystalline powder and is practically insoluble in water. The drug has a nonsteroidal structure and is … Darolutamide

Apalutamide

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 … Apalutamide

Bicalutamide

Products Bicalutamide is commercially available in the form of film-coated tablets (Casodex, generics). It has been approved in many countries since 1995. Structure and properties Bicalutamide (C18H14F4N2O4S, Mr = 430.37 g/mol) is a racemate, with the -enantiomer being almost exclusively responsible for the antiandrogenic effect. It exists as a white powder that is practically insoluble … Bicalutamide

Enzalutamide

Products Enzalutamide was initially registered in capsule form (Xtandi). Film-coated tablets were approved in many countries in 2019. They are smaller and therefore easier to take. Enzalutamide was approved in the United States in 2012 and in many countries and the EU in 2013. Structure and properties Enzalutamide (C21H16F4N4O2S, Mr = 464.4 g/mol) is an … Enzalutamide

Flutamide

Products Flutamide was approved in many countries in 1984 in tablet form (Flucinom, 250 mg) and is no longer registered. It can be replaced by modern antiandrogens if needed or imported from abroad. Structure and properties Flutamide (C11H11F3N2O3, Mr = 276.2 g/mol) exists as a pale yellow crystalline powder that is practically insoluble in water. … Flutamide

Cyproterone Acetate

Products Cyproterone acetate is commercially available in the form of dragées in combination with ethinyl estradiol (generics). The drug has been approved in many countries since 1987. This article refers to the original Diane-35 and corresponding generics. Other drugs containing cyproterone acetate are available for other indications. Bayer’s original Diane-35 goes off the market in … Cyproterone Acetate

Clascoteron

Products Clascoterone was approved as a cream in the United States in 2020 (Winlevi). Structure and properties Clascoterone (C24H34O5, Mr = 402.5 g/mol) corresponds to the steroid cortexolone-17α-propionate. It exists as a white powder that is practically insoluble in water. Effects Clascoterone has antiandrogenic properties. The effects are due to antagonism at androgen receptors. Androgens … Clascoteron