Inclusion Criteria:
* Histologically or cytologically confirmed Stage IIIB or IV NSCLC
* Resistance to EGFR TKI (1st, 2nd or 3rd generation)
* Histological or cytological evidence of EGFR mutation and T790M negative after progression on last EGFR TKI therapy
* c-Met GCN ≥ 6 or cluster amplification is required if participant is resistant to1st or 2nd generation EGFR-TKI ;c-MET GCN statue is not required, If participant is resistant to3rd generation EGFR-TKI (osimertinib);
* Measurable disease according to Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST 1.1)
* Toxicity recovered to NCI CTCAE v.4.03 Grade ≤1 from previous treatments (except alopecia)
* ECOG performance status (PS) 0 or 1
* Life expectancy of ≥ 12 weeks
* Adequate organ function
Exclusion Criteria:
* Prior treatments
* Chemotherapy, targeted therapy (except EGFR TKI), immunotherapy, radiotherapy, or major surgery within 4 weeks prior to study treatment
* Nitrosourea and mitomycin chemotherapy within 6 weeks prior to study treatment
* EGFR TKI treatment within 2 weeks prior to study treatment
* Had received live vaccine within 4 weeks prior to study treatment
* Had received any investigational agent from other clinical study within 4 weeks prior to study treatment or are currently participating in other clinical trials
* Previous treatment with any other c-MET inhibitor or Axl inhibitor (eg, crizotinib, cabozantinib, volitinib, INC280)
* Symptomatic, untreated or unstable central nervous system metastases
* Spinal cord compression, carcinomatous meningitis or leptomeningeal diseaseonly (patient are only permitted if treated, asymptomatic and stable for at least 4 weeks prior to start of study treatment)
* Interstitial pneumonia or radiation pneumonitis
* Uncontrolled hypertension that require more than two anti-hypertensive agents to control, or systolic blood pressure (BP) \>140mmHg or diastolic BP \>90 mmHg before the first administration (BP is the mean blood pressure of two measures that 1 hours interval or above)
* Doppler ultrasound evaluation:Left ventricular ejection fraction \< 50%
* Grade ≥ 2 of arrhythmia (assessed by NCI CTCAE 4.03), or symptomatic bradycardia, or male with QTCF \> 450 ms or female with QTCF \> 470 ms, or patients with a history of torsion or congenital QT prolonged syndrome long QT syndrome
* Certain factors that would preclude adequate absorption of CT053PTSA and gefitinib (eg. unable to swallow, chronic diarrhea, intestinal obstruction)
* Significant hemoptysis within 2 months prior to enrollment, or a daily hemoptysis volume is 2.5 ml or above
* Patients with evidence of bleeding tendency, including the following cases: gastrointestinal bleeding, hemorrhagic gastric ulcer, fecal occult blood ++ and above; or melena or hematemesis within 2 months; or visceral bleeding that may occur considered by investigator
* History of immunodeficiency, or other acquired or congenital immunodeficiency, or history of organ transplantation
* Any disease of the following bellowed within 12 months prior to administration: Myocardial infarction, severe angina, or unstable angina, coronary or peripheral artery bypass graft, congestive heart failure, or cerebrovascular events (including transient ischemic attack)
* Pulmonary embolism within 6 months prior to administration
* Active infection of hepatitis B, or infection of HIV
* Other malignancies within 5 years prior to enrollment, with the exception of carcinoma in situ of the cervix, basal or squamous cell skin cancer
* History of thyroid dysfunction, and the thyroid function cannot be maintained at the normal range with drugs.
* Serious electrolyte imbalance in the investigator's judgment
* Pregnant or lactating woman
* Any other reason the investigator considers the patient is not suitable to participate in the study