WS-716 enhances the antitumor activity of paclitaxel (PTX) in the multidrug resistance (MDR) patient-derived xenograft (PDX) models. Mice bearing PDX were treated with vehicle (10 mL/kg/day), PTX (5 mg/kg/3 days), WS-716 (100 mg/kg/day) or PTX plus WS-716. Tumor volume and animal body weight were measured periodically. (A) Workflow of establishment of MDR PDX models. (B) HE staining was used for pathological validation and IHC analysis was used for detection of P-gp expression in tumor tissues from the patient (primary tumor), F0 (F0 tumor), and F2 xenografts (F2 tumor). (C) Expression of P-gp in F0 and F2 tumor was detected using Western blot. (D) Tumor volume during treatment. (E) Tumor weight on Day 13. (F) The relative tumor proliferation rate (T/C) of treatment groups (The red dotted line: 40%). (G) Photographs of tumors on Day 13. (H) Body weight during treatment. Data are presented as the mean ± SD, n = 5. ∗P < 0.05, ∗∗P < 0.01, ∗∗∗P < 0.001 vs. vehicle, #P < 0.05, #P < 0.01. Scale bar is 100 μm.