'antiprotease' originates from Modern English, formed by combining the prefix 'anti-' (from Greek anti- meaning 'against') with 'protease' (an enzyme name), where 'anti-' meant 'against' and 'protease' referred to a 'protein‑digesting enzyme'.

'protease' itself comes from 'protein' + the enzyme suffix '-ase' (used in Modern scientific nomenclature); 'protein' derives from Greek 'proteios' meaning 'primary' or 'of first importance'. 'antiprotease' was created by adding the prefix 'anti-' to the enzyme name 'protease' to denote an inhibitor.

Initially constructed to mean 'against proteases' in a literal morphological sense; it has come to mean specifically 'a substance that inhibits protease enzymes' in modern biochemical usage.