Flowing blood is more than a drug transporter in pharmacology; its mechanical impact should also be considered. The in vitro pharmacological dose-response pattern of endothelial cellular functions can be significantly modified by in vivo shear stress. A new borderline discipline, biomechanopharmacology, is forming at the boundary between biomechanics and pharmacology. Biomechanopharmacology will probably consist of both the pharmacological intervention of signals induced by biomechanical factors and the biomechanical influence on pharmacokinetics and pharmacodynamics, in addition to the joint effect of biomechanical and pharmacological factors. Recent investigations show that exercise enhances the shear of pulsatile blood flow to stimulate angiogenesis. The benefits of exercise for gaining joint biomechanical and pharmacological effects should be emphasized.