Linifanib

Monitoring Tumor Response to Linifanib Therapy with SPECT/CT Using the Integrin avb3–Targeted Radiotracer Tc-3P-RGD2

The objective of this study was to determine the utility of Tc3P-Arg-Gly-Asp (RGD2) single photon emission computed tomography (SPECT)/computed tomography (CT) for noninvasive monitoring of integrin avb3-expression response to antiangiogenic treatment with linifanib. Linifanib or vehicle therapy was carried out in female athymic nu/nu mice bearing U87MG glioma (high avb3 expression) or PC-3 pro...

Radiosensitization of Head & Neck Carcinoma Cells by Linifanib, A Receptor Tyrosine Kinase Inhibitor

Autophagy inhibition sensitizes hepatocellular carcinoma to the multikinase inhibitor linifanib

Autophagy is a critical survival pathway for cancer cells under conditions of stress. Thus, induction of autophagy has emerged as a drug resistance mechanism. This study is to determine whether autophagy is activated by a novel multikinase inhibitor linifanib, thereby impairing the sensitivity of hepatocellular carcinoma (HCC) cells to this targeted therapy. Here, we found that linifanib induce...

Efficacy and Safety of Systemic Therapies for Advanced Hepatocellular Carcinoma: A Network Meta-Analysis of Phase III Trials.

Aim/Background After the introduction of sorafenib in the treatment of advanced hepatocellular carcinoma (HCC), different studies tried to evaluate whether other systemic therapies can improve survival. To provide a comprehensive indirect treatment comparison of efficacy and safety of novel drugs, a network meta-analysis (NMA) of phase III randomized controlled trials was performed. Methods A...

Simple, sensitive and rapid determination of linifanib (ABT-869), a novel tyrosine kinase inhibitor in rat plasma by UHPLC-MS/MS

BACKGROUND Linifanib (ABT-869) is an orally active receptor tyrosine kinase inhibitor, which simultaneously inhibits vascular endothelial and platelet derived growth factor receptor. The aim of the present study was to develop an UHPLC-MS/MS method for the quantification of linifanib in rat plasma to support the pharmacokinetic and toxicokinetic studies. RESULTS Linifanib was separated on Acq...

Integrin αvβ3-Targeted Radiotracer 99mTc-3P-RGD2 Useful for Noninvasive Monitoring of Breast Tumor Response to Antiangiogenic Linifanib Therapy but not Anti-Integrin αvβ3 RGD2 Therapy

PURPOSE (99m)Tc-3P-RGD2 is a (99m)Tc-labeled dimeric cyclic RGD peptide that binds to integrin α(v)β₃ with high affinity and specificity. The purpose of this study was to demonstrate the utility of (99m)Tc-3P-RGD₂ SPECT/CT (single photon emission computed tomography/computed tomography) as a molecular imaging tool for noninvasive monitoring breast tumor early response to antiangiogenesis therap...