The highway runs north–south, from the South Carolina state line to NC 274 near the unincorporated community of Tryon.

[1] NC 216 was established in 1930 as a new primary route from US 29/NC 205 to the South Carolina state line.

Around 1956, NC 216 was extended north along US 29 for 1.5-mile (2.4 km), then replacing US 29 into Kings Mountain.

It then continued north on several upgraded secondary roads to its current terminus on NC 274.

In the early 1960s, SC 216 was established as a continuation of NC 216 to Kings Mountain National Military Park.