Abstract: Objective: To evaluate the safety and efficacy of sunpla as a single agent therapy for the treatment of inoperable gastric cancer and to compare the safety and efficacy of sunpla vs. cisplatin combined with Calcium Folinate and 5-Fluorouracil for the treatment of inoperable gastric cancer as first-line treatment. Methods: A randomized, multi-central, open and prospective controlled clinical trial was carried out. A total of 217 patients (pts) with gastric cancer confirmed by histopathology were enrolled in the study, and all of them have signed the written informed consent. Fifty pts were allocated to single-drug arm (single use of sunpla, A arm), 83 were assigned to combination treatment arm (sunpla+Calcium Folinate+5-Fluorouracil, B arm), 84 pts were allocated to combination controlled arm (cisplatin+Calcium Folinate+5-Fluorouracil, C arm). Every treatment cycle included three weeks, and 1 to 3 cycles was given for each pt. Results: At the end of the second treatment cycle in the B arm, there was no CR pts among the 79 evaluable pts, with 18 PR pts, 44 SD pts and 17 PD pts. The total response rate was 22.78%. At the end of the second treatment cycle in the C arm, there were no CR pts among the 82 evaluable pts, with 17 PR pts, 47 SD pts and 18 PD pts. The total response rate was 20.73%. The response rate between the two arms had no significant difference (P=0.8131). Among the 47 evaluable pts in the A arm, there were 1 CR, 6 PR, 25 SD and 15 PD. The response rate for single use of the sunpla was 14.90%. Conclusions: The efficacy of sunpla as a single-agent therapy in the treatment of gastric cancer was in accordance with certain reports, and there is no significant difference between sunpla vs. cisplatin combined with Calcium Folinate and 5-Fluorouracil. The major adverse events are nausea, vomiting, anorexia and digestive tract reaction. The abnormalities of laboratory examination are leucopenia and neutropenia. No serious hepatonephrotoxicity has been observed during the trial.