Rivoceranib (Apatinib): A Comprehensive Oncological Monograph

Executive Summary

Rivoceranib, also known internationally as apatinib, is an orally bioavailable, small-molecule tyrosine kinase inhibitor (TKI) that functions primarily as a potent and highly selective antagonist of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). Its principal mechanism of action is the inhibition of tumor angiogenesis, a critical process for cancer growth and metastasis. Beyond its antiangiogenic properties, preclinical and clinical evidence suggests that rivoceranib also possesses secondary activities, including mild inhibition of c-Kit and c-SRC kinases and a novel capacity to reverse multidrug resistance by inhibiting key cellular efflux pumps.[1]

The clinical development of rivoceranib has yielded significant, albeit mixed, results across different malignancies and therapeutic settings. In unresectable hepatocellular carcinoma (uHCC), rivoceranib has demonstrated landmark efficacy. The global Phase III CARES-310 trial, which evaluated rivoceranib in combination with the anti-PD-1 antibody camrelizumab, met its primary endpoints, showing statistically significant and clinically meaningful improvements in both overall survival (OS) and progression-free survival (PFS) compared to the then-standard-of-care, sorafenib. The final analysis reported a median OS of 23.8 months for the combination, establishing a new benchmark for first-line systemic therapy in this patient population.[3]