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Indications

High Alert

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypertension, MYOCARDIAL ISCHEMIA/INFARCTION.

Derm: alopecia, ERYTHEMA MULTIFORME, impaired wound healing, PALMAR-PLANTAR ERYTHRODYSESTHESIA, rash, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN).

EENT: dysphonia.

Endo: hypothyroidism.

F and E: hypocalcemia, hypokalemia, hypophosphatemia, hyponatremia.

GI: appetite, weight, lipase, diarrhea, mucositis, amylase, liver enzymes, dry mouth, GI FISTULA/PERFORATION, HEPATOTOXICITY, reflux.

GU: proteinuria, fertility.

Hemat: anemia, bleeding, lymphopenia, thrombocytopenia.

MS: pain, musculoskeletal stiffness.

Neuro: fatigue, dysgeusia, headache, POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), tremor.
Misc: fever, infection.

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Availability

Route/Dosage

US Brand Names

Stivarga

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics

Absorption: Well absorbed following oral administration (69–83%).

Distribution: Unknown.

Protein Binding: Regorafenib: >99.5%, M-2 metabolite: 99.8%, M-5 metabolite: 99.95%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme and UGT1A9; 2 metabolites (M-2 and M-5) have antineoplastic activity. Undergoes enterohepatic circulation. 47% excreted in feces as parent compound, 24% as metabolites; 19% excreted in urine (mostly as inactive metabolites).

Half-life: Regorafenib: 28 hr, M-2 metabolite: 25 hr, M-5 metabolite: 51 hr.

Time/Action Profile

(improved survival)

ROUTEONSETPEAKDURATION
PO3 mo3 moup to 10 mo

Patient/Family Teaching

Pronunciation

re-goe-RAF-e-nib