everolimus: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
everolimus: clinical details
Prescribing considerations
- Initiation and maintenance require clinicians experienced in transplantation or TSC, with access to whole-blood everolimus concentration monitoring.
- Review infections, total immunosuppressive burden, pneumonitis risk, wound healing, previous hepatitis B, hepatic impairment and interacting medicines.
- Avoid live vaccines and minimise ultraviolet exposure in immunosuppressed transplant recipients.
- Discuss reproductive plans and potential effects on fertility.
Contraindications and cautions
- Hypersensitivity to everolimus, related rapamycin derivatives such as sirolimus, or formulation excipients.
- Selected formulations contain lactose and are unsuitable for specified rare hereditary disorders of galactose metabolism or absorption.
Monitoring
- Whole-blood everolimus trough concentration, particularly after initiation, formulation changes or changes in interacting medicines.
- Full blood count.
- Renal function and urinary protein.
- Fasting glucose and blood lipids.
- Liver function and clinical status in hepatic impairment.
- Clinical evidence of infection, pneumonitis, mouth ulceration, wound-healing problems, angioedema and malignancy.
Clinical pharmacology
Everolimus forms an FKBP-12 complex that selectively inhibits mTORC1. It is metabolised mainly through CYP3A4 and is a P-glycoprotein substrate, accounting for substantial interaction potential and the role of therapeutic drug monitoring.
Formulation and product differences
- Certican tablets are licensed for adult transplantation and should be swallowed whole.
- Votubia dispersible tablets are licensed for specified TSC manifestations and must be administered as a water suspension.
- Votubia tablets and dispersible tablets are not interchangeable or to be combined. Certican and Votubia products should not be substituted without specialist direction.
everolimus preparations and strengths
Dispersible tablet
Route: Oral
Strengths: 1 mg, 2 mg, 3 mg, 5 mg
Tablet
Route: Oral
Strengths: 2.5 mg, 5 mg, 10 mg
everolimus interactions
Interactions affecting CYP3A4 or P-glycoprotein are particularly important. Check prescription, non-prescription and herbal products with the specialist team.
Strong CYP3A4/P-glycoprotein inhibitors, including clarithromycin, azole antifungals and some HIV antivirals
Can substantially increase everolimus exposure and toxicity; combinations are generally avoided or require specialist management.
Moderate inhibitors, including erythromycin, fluconazole, verapamil, diltiazem and cannabidiol
Can increase everolimus concentrations, prompting closer adverse-effect and blood-level monitoring.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.