SCARB1 and cancer: Despite the successes described thus far in targeting SR-BI to enhance and confine cancer therapy to target tumor tissue, associated biodistribution data demonstrated significant off-target accumulation of drugs, particularly in the liver and spleen (Zhang et al., 2009; Yang et al., 2011a; Tripathy et al., 2014); an unsurprising observation given the abundant expression of SR-BI in normal hepatic and steroidogenic tissue (Table 1).