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Efflux protein is an active transport protein family located on cell membranes of various human tissues, including ocular tissues.Efflux proteins can transport exogenous molecules out of the cells to function as a protective mechanism.Scientists have revealed these proteins in various human eye tissues, including cornea, iris and ciliary body, retina, as well as retinal pigment epithelium.Many studies have demonstrated that these efflux proteins have their own unique substrates and inhibitors.The effects of these efflux proteins and inhibitors can alter ocular pharmacokinetics as well as pharmacodynamics of a given therapeutics.Better understanding of the efflux proteins and their functions can provide scientific insight and guideline for development of optimal ocular drug delivery strategy.