'antituberculosis' originates from the combining form 'anti-' from Greek, meaning 'against', and 'tuberculosis', from New Latin 'tuberculosis' (related to Latin 'tuberculum').

'tuberculosis' derives from Latin 'tuberculum' meaning 'small swelling' (from 'tuber' meaning 'swelling' or 'lump'); medical Latin formed 'tuberculosis' to denote the disease of tubercles, and modern English formed the compound 'antituberculosis' by prefixing 'anti-' to indicate action against the disease.

Initially medical usage focused on 'tubercle' (a small swelling); over time 'tuberculosis' came to denote the disease caused by those tubercles, and 'antituberculosis' evolved to mean 'against or used to treat tuberculosis'.