Candida albicans is an important human pathogenic yeast, that can become resistant to commonly used antifungal agents, such as azoles. One mechanism of drug resistance is efflux via ATP binding cassette transporters, such as Cdr1. Several studies have investigated the structural organization, binding mechanisms, function and regulation of Cdr1. This review summarizes the findings on the structure and function of Cdr1 and highlights important aspects to consider in future research relating to multidrug ABC transporters.