To date, 14 small molecules targeting the VEGFR pathway have received FDA approval for the treatment of diverse malignancies (Fig. 5). Table 2 represents the pharmacokinetic profile, drug dose, and dose-limiting toxicities associated with the FDA-approved VEGFR inhibitors [53], [151], [152], [153], [154], [155], [156], [157], [158], [159], [160], [161], [162], [163], [164], [165], [166]. Table 3 illustrates the investigational VEGFR inhibitors undergoing clinical trials.