Simple SummaryThe discovery of actionable oncogenic driver mutations in non-small-cell lung cancer (NSCLC) has revolutionized the treatment and prognosis of this dreadful disease. New targeted therapies are being developed and tested in early phase clinical trials rapidly. We summarize emerging first-in-human clinical trials of targeted therapy that have been conducted or initiated in the past year. We hope this review will benefit our readers to be familiar with new advances in this field and create more opportunities for eligible patients to access clinical trials.AbstractLung cancer remains the leading cause of cancer-related mortality worldwide. Non-small-cell lung cancer (NSCLC) is the most common type and is still incurable for most patients at the advanced stage. Targeted therapy is an effective treatment that has significantly improved survival in NSCLC patients with actionable mutations. However, therapy resistance occurs widely among patients leading to disease progression. In addition, many oncogenic driver mutations in NSCLC still lack targeted agents. New drugs are being developed and tested in clinical trials to overcome these challenges. This review aims to summarize emerging targeted therapy that have been conducted or initiated through first-in-human clinical trials in the past year.