selumetinib hydrogen sulfate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
selumetinib hydrogen sulfate: clinical details
Prescribing considerations
- Initiate under a clinician experienced in diagnosing and treating NF1-related tumours.
- Confirm that the patient can safely swallow hard capsules whole before prescribing this formulation.
- Review cardiac, ophthalmic and hepatic history and all medicines, supplements and herbal products.
- Clinical evidence is limited in people older than 65 years and in those with impaired baseline left-ventricular function.
Contraindications and cautions
- Hypersensitivity to selumetinib or any excipient.
- Severe hepatic impairment.
Monitoring
- Echocardiographic LVEF before treatment and approximately every 3 months, or more often when clinically indicated.
- Ophthalmological assessment before treatment and promptly for any new visual disturbance.
- Liver tests before treatment, at least monthly for the first 6 months, then as clinically indicated.
- Assess blood pressure, haemoglobin, creatinine, albumin and creatine phosphokinase according to clinical status.
- Monitor anticoagulation more frequently when anticoagulants or antiplatelet medicines are used.
Clinical pharmacology
Selumetinib is a selective MEK1/2 inhibitor that suppresses RAF–MEK–ERK signalling. It is highly protein bound and is metabolised predominantly through CYP3A4, with lesser CYP2C19 and other enzyme contributions; an active N-desmethyl metabolite contributes to activity.
Formulation and product differences
- The selected product is a hard capsule that must remain intact; opening, chewing or dissolving may alter release and absorption.
- The capsule contains the vitamin E excipient TPGS, which is relevant to bleeding risk and medicine interactions.
- This hard-capsule formulation is unsuitable for patients unable or unwilling to swallow it whole.
selumetinib hydrogen sulfate preparations and strengths
Capsule
Route: Oral
Strengths: 10 mg, 25 mg
selumetinib hydrogen sulfate interactions
Check prescribed, over-the-counter and herbal products with the specialist team before use.
Strong or moderate CYP3A4 or CYP2C19 inhibitors, including clarithromycin, itraconazole, fluconazole and omeprazole
These may increase selumetinib exposure and toxicity, so alternatives are generally preferred.
Grapefruit juice
It may increase selumetinib exposure and should be avoided.
CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin and St John's wort
These may reduce selumetinib exposure and effectiveness and should generally be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.