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Regorafenib for treatment of advanced gastrointestinal stromal tumors

Lindsay C Overton1, Michael C Heinrich

  • 1Portland VA Medical Center, Oregon Helath & Science University and OHSU Knight Cancer Institute , 3710 SW US Veterans Hospital Rd., Building 103 Lab E223, R&D 19, Portland OR 97239-2999 , USA +1 503 220 3405 ; +1 503 273 5158 ; Heinrich@ohsu.edu.

Expert Opinion on Pharmacotherapy
|January 11, 2014
PubMed
Abstract

Insights

Regorafenib is an effective third-line treatment for advanced gastrointestinal stromal tumors (GISTs) that have become resistant to imatinib and sunitinib. While side effects occur, they are manageable, making regorafenib a valuable option for GIST patients.

Area of Science:

  • Oncology
  • Gastroenterology
  • Pharmacology

Background:

  • Gastrointestinal stromal tumors (GISTs) are rare sarcomas resistant to traditional chemotherapy.
  • Kinase inhibitors like imatinib and sunitinib revolutionized GIST treatment but resistance is common.
  • Regorafenib offers a new therapeutic avenue for advanced GISTs.

Purpose of the Study:

  • To review preclinical and clinical data on regorafenib for GIST treatment.
  • To establish regorafenib's role in advanced GIST therapy.

Main Methods:

  • Literature search of PubMed database up to October 2013.
  • Review of preclinical and clinical studies on regorafenib in GIST.

Main Results:

  • Regorafenib improves progression-free survival in third- or fourth-line settings for GIST.
  • Phase III study confirms regorafenib as a proven third-line therapy.
  • Regorafenib's efficacy is attributed to its activity against KIT/PDGFRA.

Conclusions:

  • Regorafenib is the established third-line therapy for advanced GIST.
  • Manageable side effects are similar to other oral kinase inhibitors.
  • Avoid concomitant use of strong CYP3A4 inducers/inhibitors with regorafenib.

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