The rapid development of precision treatment mode of non-small cell lung cancer (NSCLC) is dependent on the clinical promotion and application of monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs). Non-invasive positron emission tomography (PET) in NSCLC patients with radio-labeled mAbs and TKIs as molecular probes can detect the expression level of corresponding targets. Targets of mAbs-PET are protein receptors on cell surface represented by programmed death protein and its ligand [PD-(L) 1]. Clinical translational studies showed that mAb-PET could detect the expression of corresponding receptor, and the uptake of tumor indicated clinical prognosis. Targets of TKI-PET imaging is tyrosine kinase represented by epidermal growth factor receptor (EGFR). Studies have shown that TKI-PET could indicate whether the corresponding kinase target existed, and the uptake of tumor was related to the expression of the corresponding kinase and the therapeutic effect of TKI. Meanwhile, TKI-PET can assist in screening patients who may benefit from TKI therapy, which is of great clinical significance. Non-invasive targeted PET imaging could display and quantify metabolic distribution of drugs in vivo, which can avoid the invasive receptor expression test relying on tissue biopsy. At the same time, whole-body imaging of PET could identify characteristics of all lesions, thus assisting in diagnosis and prediction of therapeutic effects. This review summarizes researches concerning clinical translation of mAb-PET and TKI-PET in NSCLC, and expounds their role and significance in clinical individualized treatment of this malignancy.