Everolimus

How it works

It binds the intracellular protein FKBP-12 to inhibit the mammalian target of rapamycin (mTOR) signalling pathway, suppressing cell proliferation, growth and angiogenesis.

Prescribing in practice

• It causes immunosuppression with increased infection risk and can produce non-infectious pneumonitis, which should be suspected with new respiratory symptoms and may require treatment interruption.
• Initiate under specialist supervision with therapeutic drug monitoring in transplant settings and dose adjustment for hepatic impairment.
• It is a substrate of CYP3A4 and P-glycoprotein, so concurrent strong inducers or inhibitors and grapefruit can markedly alter exposure.

Monitoring

Monitor blood glucose, lipids, full blood count, renal and hepatic function, and where applicable everolimus blood concentrations.

Counselling the patient

• Report new or worsening cough or breathlessness, and any signs of infection.
• Avoid grapefruit and grapefruit juice while taking this medicine.
• Mouth ulcers are common; good oral hygiene and a non-alcoholic mouthwash can help.

Evidence & guidelines

NICE technology appraisal guidance supports everolimus in defined oncology indications, based on pivotal trials demonstrating progression-free survival benefit.