'androgen-antagonistic' originates from combining two elements: 'androgen' (from Greek roots) and 'antagonistic' (from Greek/Latin via English). 'androgen' derives from Greek 'andr-'/'andros' meaning 'man' and a root related to 'generate/produce'; 'antagonistic' traces to Greek 'antagonistēs' meaning 'opponent'.

'androgen' was coined in modern scientific nomenclature in the late 19th–early 20th century from Greek elements and was adopted into English medical vocabulary; 'antagonistic' developed from Greek into Latin and Old French forms (via 'antagonista'/'antagonistes') and entered modern English as 'antagonistic'. The compound form 'androgen-antagonistic' arises in 20th-century biomedical English by compounding these established terms.

Initially the roots referred separately to 'male' (andr-) and 'opponent' (antagon-); over time, the compounded adjective has come to mean specifically 'having the property of opposing or blocking androgen action' in pharmacology and endocrinology.