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, metastasis and tumor immunity.

STIVARGA is indicated for treatment of:

Metastatic Colorectal Cancer (CRC)
In patients previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, anti-VEGF therapy, and, if RAS wild-type, anti-EGFR therapy.

Gastrointestinal Stromal Tumors (GIST)
In patients with locally advanced, unresectable or metastatic GIST previously treated with imatinib and sunitinib.

Hepatocellular Carcinoma (HCC)
In patients previously treated with sorafenib.

160 mg orally once daily for the first 21 days of each 28-day cycle.

• Pain (abdominal/GI)
• Fatigue/asthenia
• Diarrhea
• Decreased appetite
• Hypertension
• Infections
• HFSR
• Voice changes (dysphonia)
• Hyperbilirubinemia
• Fever
• Weight loss
• Rash
• Nausea

None

Infections: Higher risk of severe infections; may be fatal.

Hemorrhage: Increased risk, including CNS, GI, and respiratory bleeding.

GI Perforation or Fistula: Can be fatal; discontinue if this occurs.

Dermatologic Toxicity: High incidence of HFSR (Hand-Foot Skin Reaction); manage with dose interruptions/reductions.

Hypertension: Common; monitor BP closely, especially in the first 6 weeks.

Cardiac Ischemia: Risk of MI and ischemia; withhold if symptoms develop.

Reversible Posterior Leukoencephalopathy Syndrome (RPLS): Rare; discontinue if diagnosed.

Wound Healing Impairment: Withhold 2 weeks before and after major surgery.

Embryo-Fetal Toxicity: Can cause fetal harm; strict contraceptive measures advised.