Minoxidil was the first drug approved by the FDA for the treatment of androgenetic alopecia (hair loss). Before that, minoxidil had been used as vasodilator drug prescribed as oral tablet to treat high blood pressure, with side effects that included hair growth and reversal of male baldness. In the 1980s, UpJohn Corporation came out with a topical solution of 2% minoxidil, called Rogaine, for the specific treatment of androgenetic alopecia. Since the 1990s, numerous generic forms of minoxidil have become available to treat hair loss while the oral form is still used to treat high blood pressure.

The popularity hair loss treatment is due to the general preference in the overall population for the cosmetic appearance of a full head of hair. Minoxidil is used to stimulate hair growth in areas of the scalp that have stopped growing hair. As of early 2001, the exact mechanism of action of minoxidil is not known.