Heroin was first isolated from morphine in 1874 by the British Chemist C.R. Alder Wright, however it did not lead to any further developments. It was independently re-synthesized in 1897 by another chemist, Felix Hoffmann, who was working at the Bayer pharmaceutical company in Germany and was instructed by his supervisor Heinrich Dreser to search for a pain killer which was 'Free of the disagreeable effects of morphine' (i.e. not habit forming).

From 1898 through to 1910 heroin was marketed as a non-addictive morphine substitute and cough suppressant. It was also marketed as a cure for morphine addiction before it was discovered that heroin is rapidly metabolized into morphine, and as such was more addictive rather than less.