idelalisib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
idelalisib: clinical details
Prescribing considerations
- Treatment should be supervised by a clinician experienced in anticancer therapy.
- Confirm the licensed disease context and review previous therapy, molecular findings and alternatives.
- Do not initiate with an ongoing systemic bacterial, fungal or viral infection.
- Reconcile all medicines for CYP3A and transporter interactions.
- Counsel patients to report infection, respiratory symptoms and diarrhoea promptly.
Contraindications and cautions
- Hypersensitivity to idelalisib or an excipient.
- Use caution with hepatic impairment, active hepatitis, previous inflammatory bowel disease or substantial immunosuppression.
- Safety and efficacy are not established in people younger than 18 years.
Monitoring
- Full blood count, particularly absolute neutrophil count.
- ALT, AST and bilirubin.
- Infection and CMV status in patients with previous CMV exposure.
- New respiratory symptoms, diarrhoea or colitis, rash, and neurological or behavioural change.
Clinical pharmacology
Idelalisib selectively inhibits the PI3K p110-delta catalytic subunit, suppressing Akt-pathway signalling and malignant B-cell proliferation, survival, homing and retention. It is metabolised mainly by aldehyde oxidase; its inactive primary metabolite strongly inhibits CYP3A.
Formulation and product differences
- The film-coated tablet contains sunset yellow FCF (E110), which may cause allergic reactions.
- The tablet should be swallowed whole and is essentially sodium-free.
idelalisib preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg, 150 mg
idelalisib interactions
A full review of prescribed, non-prescribed and herbal products is essential.
Rifampicin, phenytoin, carbamazepine and St John’s wort
These CYP3A inducers can substantially reduce idelalisib exposure and should generally be avoided.
Sensitive CYP3A substrates
Exposure to medicines including alfuzosin, amiodarone, quetiapine, simvastatin, midazolam and triazolam may increase markedly, potentially causing serious toxicity.
Fentanyl, alfentanil, methadone or buprenorphine/naloxone
Concentrations may increase, requiring monitoring for sedation and respiratory depression.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.