Roxadustat
Regulatory sources consulted
Approved indications
- Treatment of adult patients with symptomatic anaemia associated with chronic kidney disease (CKD).
Contraindications
Absolute
- Hypersensitivity to the active substance or to any of the excipients.
- Pregnancy.
- Breast-feeding.
Clinical warnings
- Major warning · Cardiovascular events and mortality: An increased risk of mortality and serious cardiovascular events (e.g., myocardial infarction, stroke) has been observed in some studies, particularly in non-dialysis-dependent patients. Assess individual risks and benefits. — EMA
- Major warning · Vascular thrombosis: Venous and arterial thromboembolic events have been reported, including vascular access thrombosis. Use with caution in patients with risk factors for thromboembolism. — EMA
- Seizures: Seizures have been reported. Use with caution in patients with a history of seizure disorders. — EMA
Drug interactions
- HighGemfibrozilC10AB04
Mechanism: Potent inhibition of CYP2C8 and OATP1B1, which increases roxadustat exposure (AUC x2.7).
Recommendation: If co-administration is necessary, limit the roxadustat dose to 2.5 mg/kg or 200 mg (whichever is lower) and monitor hemoglobin response.
EMA SPC
- HighPhosphate bindersV03AE
Mechanism: Polyvalent cations (e.g., sevelamer, calcium) chelate roxadustat in the GI tract, drastically reducing its absorption and AUC (up to -67%).
Recommendation: Administer roxadustat at least 1 hour before or 1 hour after the administration of phosphate binders or other medicinal products containing polyvalent cations.
EMA SPC
Adverse events
Common (≥1%)
hyperkalaemia · nausea · diarrhoea · peripheral oedema · hypertension · headache
Rare but serious
sepsis · deep vein thrombosis · pulmonary embolism · seizures
Pregnancy and lactation
FDA category: X
Roxadustat is contraindicated during pregnancy and breast-feeding. Women of childbearing potential must use highly effective contraception during treatment and for at least one week after the last dose.
Recent literature (PubMed)
Estudio fase 3 (ROCKIES) en 2133 pacientes con ERC en diálisis demostró que roxadustat oral no fue inferior a epoetina alfa parenteral para aumentar la hemoglobina en 52 semanas, con un perfil de eventos adversos comparable.
Revisión detallada de la farmacocinética y farmacodinamia de roxadustat. Describe su vida media de 9.6-16h, alta unión a proteínas (99%), y un modelo de efecto en dos pasos: un aumento rápido de EPO seguido de un aumento gradual de hemoglobina.
Revisión que discute la evidencia clínica sobre los efectos adversos de roxadustat, incluyendo riesgo cardiovascular, hiperpotasemia e infecciones. Subraya la necesidad de seguimiento a largo plazo para confirmar su perfil de seguridad.
Artículo de revisión que explora los efectos pleiotrópicos y potenciales usos de roxadustat más allá de la anemia renal, basados en su mecanismo de acción sobre el HIF. También discute posibles efectos fuera de diana.
Revisión enfocada en los aspectos farmacéuticos de roxadustat, incluyendo formulaciones, polimorfismo y métodos analíticos. De interés para el desarrollo de productos, pero con menor relevancia clínica directa.