Adsorption capacity and rate are critical factors for removing antibiotics from wastewater. Herein, the synergistic effect of suitable pore size and active site was introduced to construct adsorbents by taking tinidazole (TNZ) as an example, which could help to achieve excellent adsorption capacity and fast adsorption rate simultaneously. Benefited from suitable pore size, μ-OH group, and positively charged surface, MIL-53(Al)-NDC was proved to be able to realize the synergistic effect to lead to a high adsorption capacity of TNZ (510.2 ​mg ​g⁻¹) and a fast adsorption rate (110 ​min), superior to the reported adsorbents. As control experiments, MIL-101(Cr) with only suitable pore size and MIL-53(Al) with only suitable active site exhibit the relatively poor adsorption performances. This work indicates that MIL-53(Al)-NDC have a great potential in TNZ removal, and the synergistic effect of suitable pore size and active site may be helpful for rational design of high-performance adsorbents for removing antibiotics.