Regorafenib (STIVARGA)

Hepatocellular carcinoma, advanced

Gastrointestinal stromal tumor

Hepatocellular carcinoma, advanced

• Dose – Oral: 160 mg once daily on days 1 to 21 out of every 28 days until disease progression or unacceptable toxicity

Gastrointestinal stromal tumor

• Dose – Oral: 160 mg once daily on days 1 to 21 out of every 28 days until disease progression or unacceptable toxicity

Available as 40 mg film-coated tablets. Tablets should NOT be crushed or broken. Store at room temperature.

Multi-targeted TKI (tyrosine kinase inhibitor) which includes action as a VEGF (vascular endothelial growth factor) inhibitor

Take with water after a low-fat meal

If a dose is missed, patients should be instructed to take it as soon as they can if it is remembered on the same day. Otherwise, patients should skip the missed dose and resume with the next scheduled dose.

Common: Diarrhea, Asthenia/fatigue, Stomatitis/mucosal inflammation, Hepatobiliary disorders, Infection, Weight loss, Decreased appetite, Dysphonia, Hand-foot skin reaction , Hypertension, Rash, Hemorrhage.

Less Common: Cardiac adverse events, Gastrointestinal perforation or fistula , Reversible posterior leukoencephalopathy syndrome, Cutaneous reactions (erythema multiforme, Steven Johnson syndrome).

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Baseline before treatment: CBC & differential, platelets, creatinine, sodium, potassium, calcium, magnesium, phosphate, albumin, bilirubin, alkaline phosphatase, ALT, GGT, TSH, urinalysis, Blood Pressure measurement. If clinically indicated: AFP.

During treatment: CBC & differential, platelets, creatinine, sodium, potassium, calcium, magnesium, phosphate, bilirubin, alkaline phosphatase, ALT, urinalysis, Blood Pressure measurement.

If clinically indicated: MUGA scan or echocardiogram, ECG, TSH.

• This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
• Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
• Current drug interaction databases should be consulted for more information.

• Avoid in pregnancy and lactation.
• Hypertension is common with VEGF inhibitors. Monitor blood pressure closely and manage with antihypertensives and dose hold/reductions. Hypertension should be well controlled prior to starting regorafenib.
• Thyroid dysfunction in particular hypothyroidism may occur with this treatment. Monitor for signs and symptoms of thyroid dysfunction and manage as clinically appropriate.
• Impaired wound healing is associated with VEGF inhibitors, drug may need to be held and restarted if patient requires surgery, discuss with team.

BC Cancer. BC Cancer Drug Manual. Regorafenib. Vancouver, British Columbia: BC Cancer Agency. Available at http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Regorafenib_monograph.pdf. Updated August 1, 2023. Accessed 22 Jan 2024.

Lexicomp. Regorafenib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at: https://online-lexi-com.qe2a-proxy.mun.ca/lco/action/doc/retrieve/docid/patch_f/3964611?cesid=5U7OFpQnvfX&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dregorafenib%26t%3Dname%26acs%3Dtrue%26acq%3Dregorafenib. Updated January 24, 2024. Accessed January 25, 2024.

Cancer Care Ontario. Regorafenib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/44306. Updated August 2023. Accessed January 22, 2024.

Bayer Inc. STIVARGA® Product Monograph. Mississauga, Ontario: Bayer Inc. Updated September 29, 2022.