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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Calcineurin inhibitors
voclosporin
L04AD03
Adult Dosing
- Lupus nephritis: 23.7 mg (3 capsules) orally twice daily
- Administer consistently with or without food, avoiding grapefruit
- Reduce dose to 7.9 mg twice daily if eGFR drops significantly
Pediatric Dosing
- Safety and efficacy in pediatric patients (<18 years) have not been established
Indications
- Active lupus nephritis (LN) in combination with a background immunosuppressive therapy regimen
Mechanism of Action
- Calcineurin inhibitor that suppresses calcineurin activity
- Inhibits IL-2 expression and T-cell proliferation and differentiation
- Decreases cytokine release and prevents podocyte damage in the kidney
Contraindications
- Concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, itraconazole)
- Severe hepatic impairment
- Known hypersensitivity to voclosporin
Adverse Reactions
- Hypertension
- Diarrhea
- Headache
- Anemia
- Cough
- Urinary tract infection
- Nephrotoxicity
- Increased risk of malignancies and serious infections
Drug Interactions
- Strong and moderate CYP3A4 inhibitors (significantly increase voclosporin exposure)
- Strong and moderate CYP3A4 inducers (significantly decrease voclosporin efficacy)
- P-glycoprotein inhibitors and inducers
- Nephrotoxic drugs (additive risk of renal impairment)
Curated Content: Needs Vetting Before Put to Clinical Use