Drug transporters are integral membrane proteins that transport a broad range of substrates into and out of cells, usually against a concentration gradient. Studies have shown that efflux pumps such as P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) localize at the blood–testis barrier (BTB), where they protect the testis from drugs and xenobiotics that are detrimental to spermatogenesis. At the same time, efflux pumps might also preclude entry of non-hormonal contraceptives to the testis. In more recent studies, P-gp function was correlated with BTB integrity. In this review, we discuss findings that have made a significant impact on our understanding of efflux pumps in the testis. Modulation of efflux pump function via specific inhibitors could help to deliver contraceptives to the testis in the future.