'antiestrogenic' originates from modern English, specifically formed from the Greek prefix 'anti-' meaning 'against', combined with 'estrogen' (from Greek 'oistros' via Neo-Latin/modern coinage) and the adjectival suffix '-ic' from Greek/Latin meaning 'pertaining to'.

'estrogen' was coined in modern scientific English (often seen as 'oestrogen' in older British spelling) from Greek 'oistros' (meaning 'gadfly, sexual desire') via New Latin/modern medical terminology; the adjective 'estrogenic' developed from that noun, and 'anti-' was prefixed to form 'antiestrogenic' in 20th-century medical usage.

Initially the root related to 'oestrus' or the physiological state associated with sexual receptivity; over time the combined modern term 'antiestrogenic' evolved to mean specifically 'opposing or inhibiting estrogen's biological effects'.