The highway runs north–south, traversing the central Piedmont region of the state.

A two-lane rural highway, it traverses 53.9 miles (86.7 km) from Mooresville to U.S. Route 601 (US 601) near Farmington.

It links several small towns and communities including Cooleemee, Advance, Farmington, and Bermuda Run.

Between 1934 and 1936, NC 801 was rerouted in the Hillsdale area, eliminating a concurrency with US 158.

In the early 1950s, another short concurrency, with US 64, was replaced with a continuous alignment.