axitinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
axitinib: clinical details
Prescribing considerations
- Treatment should be supervised by a clinician experienced in anti-cancer therapy.
- Control hypertension before treatment and review cardiovascular and thromboembolic risk.
- Consider hepatic function; the selected SmPC advises against use in severe hepatic impairment.
- Plan interruption around surgery and resume only when wound healing is clinically adequate.
- Review all medicines, supplements and herbal products for CYP3A4/5 interactions.
- Assess pregnancy potential, contraception, breastfeeding and fertility implications.
Contraindications and cautions
- Hypersensitivity to axitinib or any product excipient.
- The selected lactose-containing product must not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
Monitoring
- Blood pressure before treatment and regularly thereafter
- Thyroid function before treatment and periodically
- Urinary protein before treatment and periodically
- Liver enzymes and bilirubin before and during treatment
- Haemoglobin and haematocrit where clinically indicated
- Symptoms of heart failure, bleeding, thrombosis, gastrointestinal perforation or fistula, PRES and wound-healing complications
Clinical pharmacology
Axitinib selectively inhibits VEGFR-1, VEGFR-2 and VEGFR-3. It is absorbed orally, highly protein-bound and metabolised mainly by CYP3A4/5, with lesser contributions from CYP1A2, CYP2C19 and UGT1A1.
Formulation and product differences
- The selected product is a film-coated tablet intended to be swallowed whole.
- It contains lactose monohydrate and is essentially sodium-free.
- The selected tablet is red, oval and marked “A7TI” on one side and “3” on the other.
axitinib preparations and strengths
axitinib interactions
Axitinib is mainly metabolised through CYP3A4/5. A full medication and herbal-product review is required.
Strong CYP3A4/5 inhibitors, including ketoconazole, itraconazole, clarithromycin, erythromycin and ritonavir
May increase axitinib concentrations and toxicity; an alternative with little or no CYP3A4/5 inhibition is preferred.
Strong CYP3A4/5 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and dexamethasone
May substantially reduce axitinib exposure and effectiveness; an alternative is preferred.
St John’s wort
May lower axitinib exposure through enzyme induction and should be avoided unless the oncology team specifically advises otherwise.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.