Stivarga (regorafenib)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Company:

Approval Status:

Approved February 2013

Specific Treatments:

gastrointestinal stromal tumor

Therapeutic Areas

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General Information

Stivarga (regorafenib) is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment.

Stivarga is specifically indicated for patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor who have been previously treated with imatinib mesylate and sunitinib malate.

Stivarga is supplied as a tablet for oral administration. The recommended dose is 160 mg (four 40 mg tablets) taken orally once daily for the first 21 days of each 28 day cycle. Continue treatment until disease progression or unacceptable toxicity. Stivarga should swallowed whole and taken with a low-fat breakfast.

Clinical Results

FDA Approval
The FDA approval of Stivarga for GIST was based on an international, multi-center, randomized (2:1), double-blind, placebo-controlled trial in 199 subjects with unresectable, locally advanced or metastatic gastrointestinal stromal tumor (GIST), who had been previously treated with imatinib mesylate and sunitinib malate. The subjects received 160 mg regorafenib orally once daily plus best supportive care (BSC) or placebo plus BSC for the first 21 days of each 28-day cycle. Treatment continued until disease progression or unacceptable toxicity. The primary endpoint was progression-free survival (PFS) based on disease assessment by independent radiological review using modified RECIST 1.1 criteria. The percentage of subjects with death or progression was 62% in the Stivarga arm versus 96% in the placebo arm. The median PFS was 4.8 months versus 0.9 months for the Stivarga and placebo arms, respectively.

Side Effects

Adverse events associated with the use of Stivarga for GIST may include, but are not limited to, the following:

  • asthenia/fatigue
  • HFSR
  • diarrhea
  • decreased appetite/food intake
  • hypertension
  • mucositis
  • dysphonia
  • infection
  • pain (not otherwise specified)
  • decreased weight
  • gastrointestinal and abdominal pain
  • rash
  • fever
  • nausea

Mechanism of Action

Stivarga (regorafenib) is a potent oral multi-kinase inhibitor with a kinase inhibition profile targeting angiogenic, stromal and oncogenic receptor tyrosine kinases (TK). This distinct anti-angiogenic profile includes inhibition of both VEGFR2 and TIE2 TK.

Literature References

Demetri GD, Reichardt P, Kang YK, Blay JY, Rutkowski P, Gelderblom H, Hohenberger P, Leahy M, von Mehren M, Joensuu H, Badalamenti G, Blackstein M, Le Cesne A, Schöffski P, Maki RG, Bauer S, Nguyen BB, Xu J, Nishida T, Chung J, Kappeler C, Kuss I, Laurent D, Casali PG; GRID study investigators Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet 2013 Jan 26;381(9863):295-302

Additional Information

For additional information regarding Stivarga or gastrointestinal stromal tumor, please visit the Stivarga web page.