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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Sphingosine-1-phosphate (S1P) receptor modulators
ponesimod
L04AE04
Forms & Strengths
- Oral tablets: 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg, 10 mg
- Titration pack: 14-day starter pack containing 2 mg to 10 mg tablets
Adult Dosing
- Maintenance dose: 20 mg orally once daily
- Initiation titration: Day 1-2: 2 mg once daily
- Day 3-4: 3 mg once daily
- Day 5-6: 4 mg once daily
- Day 7: 5 mg once daily
- Day 8: 6 mg once daily
- Day 9: 7 mg once daily
- Day 10: 8 mg once daily
- Day 11: 9 mg once daily
- Day 12-14: 10 mg once daily
- Day 15 and thereafter: 20 mg once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of relapsing forms of multiple sclerosis (RMS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease in adults
Mechanism of Action
- Sphingosine 1-phosphate (S1P) receptor modulator
- Selectively binds to S1P receptor subtype 1 (S1P1)
- Blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood
- Reduces central nervous system infiltration of autoreactive lymphocytes
Contraindications
- In the last 6 months, experienced myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III/IV heart failure
- Presence of Mobitz type II second- or third-degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial heart block, unless the patient has a functioning pacemaker
- Baseline QTc interval of 500 ms or greater
- Treatment with Class Ia or Class III antiarrhythmic drugs
- Severe active infections or active chronic infections such as hepatitis or tuberculosis
- Known hypersensitivity to ponesimod or any of its excipients
Adverse Reactions
- Upper respiratory tract infection
- Hepatic transaminase elevation
- Hypertension
- Diarrhea
- Bradycardia and AV conduction delays upon initiation
- Macular edema
- Increased risk of infections (including cryptococcal infections)
- Decreased forced expiratory volume in 1 second (FEV1)
Drug Interactions
- Antiarrhythmic drugs (Class Ia and Class III): Contraindicated due to additive effects on cardiac conduction and QT prolongation
- Beta-blockers, non-dihydropyridine calcium channel blockers, and other heart rate-lowering drugs: May cause additive bradycardia; use with caution and consider cardiology consultation
- Live attenuated vaccines: Avoid administration during and for 1 to 4 weeks after discontinuation of ponesimod
- Strong CYP3A4 inducers (e.g., rifampin): Co-administration decreases ponesimod exposure; avoid concomitant use
- Immunosuppressive or immunomodulating therapies: Potential for additive immune system effects; caution with switching or co-administering
Curated Content: Needs Vetting Before Put to Clinical Use