Evaluation of surufatinib, an orally available VEGFR, FGFR1 and CSF-1R inhibitor, in combination with immune checkpoint blockade or chemotherapy in preclinical tumor models

Background: Surufatinib (sulfatinib, HMPL-012) is a small molecule inhibitor targeting VEGFR 1/2/3, FGFR1 and CSF-1R tyrosine kinases. In two randomized, double-blind phase III studies (NCT02589821 and NCT02588170), surufanitib showed a significant PFS benefit in patients with advanced neuroendocrine tumors originating from pancreas or extrapancreas. Given tumor heterogeneity and complexity, monotherapies or single signaling pathway inhibition often fails to induce durable clinical benefit or prevent development of drug resistance, so that exploration of combinations of multiple mechanisms emerges as the trend of cancer treatment. Here, we reported preclinical anti-tumor effect of surufatinib in combination with clinical standard therapies in varied indications.