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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Complement inhibitors
iptacopan
L04AJ08
Adult Dosing
- Paroxysmal Nocturnal Hemoglobinuria (PNH): 200 mg orally twice daily
- C3 Glomerulopathy (C3G): 200 mg orally twice daily
- Take with or without food; swallow whole
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 18 years of age
Indications
- Treatment of adults with paroxysmal nocturnal hemoglobinuria (PNH)
- Reduction of proteinuria in adults with primary C3 glomerulopathy (C3G)
Mechanism of Action
- Proximal complement inhibitor
- Binds to complement factor B, inhibiting the alternative complement pathway convertase (C3 convertase)
- Prevents downstream amplification of the complement cascade, C3 fragment opsonization, and terminal complement-mediated hemolysis
Contraindications
- Initiation in patients with active encapsulated bacterial infections (e.g., Neisseria meningitidis, Streptococcus pneumoniae, Haemophilus influenzae)
- Known hypersensitivity to iptacopan or any of its excipients
Adverse Reactions
- Headache
- Nasopharyngitis
- Diarrhea
- Abdominal pain
- Nausea
- Serious infections (including encapsulated bacterial infections)
- Elevated serum transaminases
Drug Interactions
- Strong CYP2C8 inhibitors may increase iptacopan exposure
- Moderate to strong CYP2C8 inducers may decrease iptacopan efficacy
- Concomitant use with strong OATP1B1/1B3 inhibitors may alter plasma concentrations
Curated Content: Needs Vetting Before Put to Clinical Use