Drug intelligence / Profile preview

apatinib + pembrolizumab

Development stage
Unknown
Lead developer
University of Utah
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Apatinib + pembrolizumab is a combination therapy investigated for the treatment of various advanced solid tumors. It consists of apatinib (also known as rivoceranib), a small-molecule tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptor 2 (VEGFR2), and pembrolizumab, a humanized monoclonal antibody that blocks the programmed cell death protein 1 (PD-1) receptor. By inhibiting VEGFR2, apatinib reduces tumor angiogenesis and may normalize tumor vasculature, potentially improving the delivery and efficacy of immunotherapy. Pembrolizumab acts as a checkpoint inhibitor, restoring the ability of T cells to recognize and attack cancer cells. This combination is being evaluated in the Phase I/II APPEASE trial (NCT03407976) at the University of Utah's Huntsman Cancer Institute for patients with advanced malignancies, including urothelial carcinoma, MSI-H/dMMR solid tumors, and gastric or gastroesophageal junction adenocarcinomas.

Brand names
Keytruda
Other names
rivoceranib + pembrolizumabapatinib and pembrolizumabrivoceranib and pembrolizumab
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)

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