pralsetinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
pralsetinib: clinical details
Prescribing considerations
- Confirm RET fusion-positive disease using a validated method and initiate under an experienced anticancer prescriber.
- Control pre-existing hypertension before initiation.
- Assess for active and latent tuberculosis; treat either before starting pralsetinib.
- Review CYP3A4/P-gp interactions, QT-prolonging medicines, contraception and fertility preservation.
- Advise immediate reporting of new respiratory symptoms, bleeding or features of liver injury.
Contraindications and cautions
- Hypersensitivity to pralsetinib or any product excipient.
Monitoring
- Blood pressure at baseline, after the first week, at least monthly and when clinically indicated.
- ALT and AST before treatment, every 2 weeks during the first 3 months, then monthly and as clinically indicated.
- Full blood count and other biochemistry according to toxicity risk and clinical status.
- Baseline QTc and electrolytes; correct potassium, magnesium and calcium abnormalities. Repeat ECG and electrolytes after the first week, after the first month and periodically thereafter.
- Investigate new respiratory symptoms promptly for pneumonitis, interstitial lung disease, infection and other causes.
- Monitor for haemorrhage and tuberculosis symptoms.
Clinical pharmacology
Pralsetinib selectively inhibits oncogenic RET fusion kinases. It is principally metabolised by CYP3A4 and UGT1A4, is highly protein-bound and is predominantly eliminated in faeces.
Formulation and product differences
- The selected product is a 100 mg hard capsule.
- Capsules should be swallowed whole and stored in the original package to protect them from moisture.
pralsetinib interactions
The cancer team or pharmacist should review prescription, non-prescription and herbal products before treatment.
Strong CYP3A4 or combined CYP3A4/P-gp inhibitors, including itraconazole, voriconazole, posaconazole, ketoconazole, ritonavir and saquinavir
May increase pralsetinib exposure and the risk or severity of adverse effects; combination should generally be avoided.
Strong CYP3A4 inducers, including rifampicin, rifabutin, carbamazepine, phenytoin, phenobarbital and St John's wort
May lower pralsetinib exposure and reduce its effect; combination should generally be avoided.
Grapefruit and Seville oranges
May increase pralsetinib exposure and should be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.