Initial in vivo testing of a multitarget kinase inhibitor, regorafenib, by the Pediatric Preclinical Testing Consortium.

Abstract

BACKGROUND:

Regorafenib is a small molecule multikinase inhibitor that inhibits multiple kinases including BRAF, KIT, PDGFRB, RAF, RET, and VEGFR1-3.

PROCEDURES:

The in vivo anticancer effects of regorafenib were assessed in a panel of six osteosarcoma models, three rhabdomyosarcoma models, and one Ewing sarcoma model.

RESULTS:

Regorafenib induced modest inhibition of tumor growth in the models evaluated.

CONCLUSION:

The overall pattern of response to regorafenib appears similar to that of the kinase inhibitor sorafenib, with pronounced slowing of tumor growth in some models, limited to the period of agent administration, being the primary treatment effect.

• Authors: Douglas J Harrison, Jonathan D Gill, Michael E Roth, Wendong Zhang, Beverly Teicher, Stephen Erickson, Greg Gatto, Raushan T Kurmasheva, Peter J Houghton, Malcolm A Smith, Edward Anders Kolb, Richard Gorlick
• Journal: Pediatric blood & cancer (Pediatr Blood Cancer) Vol. 67 Issue 6 Pg. e28222 (06 2020) ISSN: 1545-5017 [Electronic] United States
• PMID: 32207565 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: © 2020 Wiley Periodicals, Inc.

Chemical References

• Phenylurea Compounds
• Protein Kinase Inhibitors
• Pyridines
• regorafenib

Topics

• Animals
• Apoptosis
• Bone Neoplasms (drug therapy, enzymology, pathology)
• Cell Proliferation
• Child
• Female
• Humans
• Mice
• Mice, SCID
• Osteosarcoma (drug therapy, enzymology, pathology)
• Phenylurea Compounds (pharmacology)
• Protein Kinase Inhibitors (pharmacology)
• Pyridines (pharmacology)
• Rhabdomyosarcoma (drug therapy, enzymology, pathology)
• Sarcoma, Ewing (drug therapy, enzymology, pathology)
• Tumor Cells, Cultured
• Xenograft Model Antitumor Assays