regorafenib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
regorafenib: clinical details
Prescribing considerations
- Initiate under a physician experienced in anticancer therapy.
- Assess hepatic function, cardiovascular history, blood pressure, bleeding risk, infection, performance status and potential interactions before treatment.
- Consider aneurysm or artery-dissection risk factors, including hypertension and previous aneurysm.
- Review planned major surgery because anti-angiogenic activity may impair wound healing.
- Patients with clinically important hepatic impairment, recent cardiac ischaemia or poor performance status require particularly careful benefit–risk assessment.
Contraindications and cautions
- Contraindicated in hypersensitivity to regorafenib or any excipient.
- Not recommended in severe hepatic impairment because it has not been studied and exposure may be increased.
Monitoring
- Check ALT, AST and bilirubin before treatment, closely during the first two months and periodically thereafter.
- Control blood pressure before treatment and monitor during therapy.
- Monitor full blood count and coagulation parameters where bleeding risk or anticoagulant use is present.
- Monitor electrolytes, metabolic parameters and thyroid function as clinically indicated.
- Assess promptly for hand–foot skin reaction, infection, bleeding, cardiac ischaemia, neurological change, gastrointestinal perforation, proteinuria and impaired wound healing.
Clinical pharmacology
Regorafenib inhibits kinases involved in angiogenesis, oncogenesis, metastasis and tumour immunity. It is extensively protein-bound, metabolised mainly by hepatic CYP3A4 and UGT1A9, and has active M-2 and M-5 metabolites that undergo enterohepatic circulation.
Formulation and product differences
- The selected product is a film-coated oral tablet containing soya-derived lecithin.
- Tablets are supplied in moisture-protective bottles containing a desiccant; the bottle must remain tightly closed.
- The product contains sodium; consider the cumulative amount where sodium restriction is clinically important.
regorafenib preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg
regorafenib interactions
Give the oncology pharmacist a complete list of prescribed, over-the-counter and herbal products. Important examples include:
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, ketoconazole, posaconazole and voriconazole
May substantially alter exposure to regorafenib and its active metabolites; concomitant use should generally be avoided.
Grapefruit juice
Can inhibit CYP3A4 and alter regorafenib exposure, so it should be avoided.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort
Can substantially alter regorafenib and active-metabolite exposure and may reduce treatment effectiveness; avoid where possible.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.