The district comprises more than forty heritage buildings and ten streets and is the largest collection of Victorian-era industrial architecture in North America. The Distillery District was designated a National Historic Site of Canada in 1988. 

The district was founded in 1832 and by the late 1860s was the largest distillery in the world. Once providing over 7,600,000 liters of whisky, mostly for export on the world market. 

In 2001, the site was purchased by Cityscape Holdings Inc., which transformed the district into a pedestrian-orientated area. The new owners refused to lease any of the retail and restaurant space to chains or franchises. The majority of the buildings are occupied with boutiques, jewellery stores, art galleries, restaurants, and coffeehouses, including a well-known microbrewery, the Mill Street Brewery. 

The upper floors of a number of buildings have been leased to artists as studio spaces and to office tenants with a "creative focus".