Sebetralstat: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Sebetralstat: clinical details
Prescribing considerations
- Confirm HAE and ensure the patient has an emergency plan for laryngeal attacks.
- Not established for children under 12 years.
- Use is not recommended in severe hepatic impairment.
- Review CYP3A4 inhibitors and inducers, transporter substrates and narrow-therapeutic-index medicines.
- Advise against driving or operating machinery if fatigue occurs.
- Subject to additional monitoring; report suspected adverse reactions through the Yellow Card scheme.
Contraindications and cautions
- Hypersensitivity to sebetralstat or any excipient.
Monitoring
- No medicine-specific routine laboratory monitoring is established.
- For metformin users at increased risk of lactic acidosis, consider renal function and blood lactate monitoring.
- Review attack response, tolerability and interacting medicines.
Clinical pharmacology
Sebetralstat competitively and reversibly inhibits plasma kallikrein, reducing bradykinin formation. It is rapidly absorbed, primarily metabolised by CYP3A4 and mainly eliminated after hepatic metabolism through the faecal route.
Formulation and product differences
- The selected product is a yellow, oval, film-coated oral tablet supplied in child-resistant blister wallets.
Sebetralstat preparations and strengths
Tablet
Route: Oral
Strengths: 300 mg
Sebetralstat interactions
Review all prescribed, non-prescribed and herbal products before sebetralstat is supplied or used.
Strong CYP3A4 inhibitors, including itraconazole, ketoconazole, ritonavir or clarithromycin
May substantially increase sebetralstat exposure, requiring review of the attack plan.
Strong or moderate CYP3A4 inducers, including phenytoin, carbamazepine, phenobarbital, rifampicin or efavirenz
May markedly reduce sebetralstat exposure and potentially reduce its effect.
Metformin
Sebetralstat may increase metformin exposure through renal transporter inhibition. Consider renal function and lactate monitoring in people at higher risk of lactic acidosis.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.