Number of patients screened	20
Number of patients enrolled	18
Number of patients evaluable for toxicity	18
Number of patients evaluated for efficacy	18
Evaluation method	RECIST version 1.1
Response assessment CR	n = 0 (0%)
Response assessment PR	n = 11.1 (2%)
Response assessment SD	n = 50 (9%)
Response assessment PD	n = 38.9 (7%)
Response assessment OTHER	n = 0 (0%)
Median duration assessments PFS	84 days, CI: 59.887–120.891
Median duration assessments TTP	84 days, CI: 59.887–120.891
Median duration of treatment	75 days

Outcome Notes

According to the RECIST version 1.1 criteria, 18 patients (including one patient who discontinued the study after receiving a single dose of metatinib) were assessed radiologically at day 32. In the first cycle, one patient (5.6%) in the 300 mg/day group had partial response (PR), 10 patients (55.6%) maintained stable disease (SD), 8 patients presented progressive disease (PD), and all 3 patients in the 25 mg/day group had PD.

In the first cycle, the DCR was 61.1% (11/18); among the patients who was achieved DCR, 10 patients continued on the treatment in the following extended period. During the extended period, three patients had PD, and seven patients had SD at the first efficacy evaluation; another patient in the 200 mg/day group achieved PR after 3 months entering into the extended period, although he experienced severe skin toxicity and reduced the dose to 100 mg/day. In total, in the current phase I study, two patients had PR, and nine patients exhibited SD, including four patients with tumor burden shrinkage; the objective response rate and DCR were 11.1% and 61.1%, respectively.

The median PFS in 18 patients was 2.75 months, ranging from 1.0 to 8.5 months, and the median PFS in 10 patients included in the extended period was 4.0 months, ranging from 2 to 8.5 months.

MET analysis: Samples from a total of 18 patients, in 162 paraffin‐embedded tumor slides, were evaluated for MET expression status by MET immunohistochemistry (IHC) and dual‐color fluorescence in situ hybridization (FISH), and for MET mutation by sequence analysis (Table 2). There were 2 cases with IHC 2+, 3 cases with IHC 1+, and 13 cases with IHC 0. MET gene amplification was not detected, and MET exon 14 skipping was exhibited in one patient with IHC 2+, showing a weak concordance between IHC and FISH. One patient in the 200 mg/day group whose tumor showed both MET IHC 2+ and exon 14 skipping achieved PR and 8.5 months’ PFS. A 5.5‐month PFS was also observed in another patient with MET IHC 2+, suggesting that MET status might be associated with the efficacy in the study.