Video

Dr. Demetri Describes the MOA of Regorafenib in GIST

Dr. George Demetri, from the Dana-Farber Cancer Institute, Describes the Mechanism of Action of Regorafenib in Gastrointestinal Stromal Tumors.

George Demetri, MD, director of the Ludwig Center at Dana-Farber Cancer Institute and Sarcoma Center at Harvard Medical School in Boston, Massachusetts, discusses the oral multikinase inhibitor regorafenib that is being investigated for patients with gastrointestinal stromal tumors (GISTs).

GISTs are driven primarily by mutations in the KIT kinase pathway, Demetri explains. Overtime, 90% of patients receiving imatinib (Gleevec) and sunitinib (Sutent) for their GIST will develop resistance. Following progression, the unique shape of the regorafenib molecule allows it to bind to targets that have developed resistance to sunitinib and imatinib, according to Demetri.

Overall, regorafenib has a very different profile than the other agents used to treat GIST. Its ability to specifically inhibit fibroblast growth factor receptors (FGFR) is still being investigated as a possible route for overcoming resistance. In total, regorafenib inhibits VEGFR1-3, TIE2, PDGFR, FGFR, KIT and RET.

For the treating oncologist, Demetri notes that the unique activity of regorafenib, as demonstrated in the phase III GRID trial, justifies the agent for patients with GIST who have no other therapeutic options. In the trial, the risk of disease progression was reduced by 73% when compared to placebo for patients who were resistant to imatinib or sunitinib.

Newsletter

Stay up to date on the most recent and practice-changing oncology data

Latest CME

View All
Show Me Your Care Plan!™ Insights for Oncology Nurses on Comprehensive SCLC Treatment and Care Strategies
Audio

Show Me Your Care Plan!™ Insights for Oncology Nurses on Comprehensive SCLC Treatment and Care Strategies

Jun 18th 2025 - Jun 19th 2026

online-activity
Tumor Board: Expert Insights on Managing Classical 𝘌𝘎𝘍𝘙 Mutations, 𝘌𝘎𝘍𝘙 Exon 20 Insertions, and Atypical 𝘌𝘎𝘍𝘙 Mutations in Metastatic NSCLC
Video

Tumor Board: Expert Insights on Managing Classical 𝘌𝘎𝘍𝘙 Mutations, 𝘌𝘎𝘍𝘙 Exon 20 Insertions, and Atypical 𝘌𝘎𝘍𝘙 Mutations in Metastatic NSCLC

Jun 6th 2025 - Jul 12th 2025

online-activity
Medical Crossfire®: Expert Perspectives on Targeting c-Met Overexpression and 𝘔𝘌𝘛 Genomic Alterations in NSCLC – Unveiling the Complexities of 𝘔𝘌𝘛 Dysregulation
Video

Medical Crossfire®: Expert Perspectives on Targeting c-Met Overexpression and 𝘔𝘌𝘛 Genomic Alterations in NSCLC – Unveiling the Complexities of 𝘔𝘌𝘛 Dysregulation

Jun 6th 2025 - Jul 12th 2025

online-activity