'anti-androgen' originates from the combining form 'anti-' from Greek meaning 'against' and 'androgen', a modern medical coinage from Greek elements 'andr-' meaning 'man' and '-gen' meaning 'to produce'.

'androgen' was coined in modern medical/biological terminology from Greek roots and entered English via Neo-Latin; the compound 'anti-androgen' was formed in English in the 20th century by adding the prefix 'anti-' to 'androgen'.

Initially formed simply to denote 'against androgens', the term has come to be used specifically for drugs and agents that block androgen action in clinical and pharmacological contexts.