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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Selective immunosuppressants
tolebrutinib
L04AA62
Forms & Strengths
- Oral tablets: 15 mg
- Oral tablets: 30 mg
- Oral tablets: 60 mg
Adult Dosing
- Multiple sclerosis (non-relapsing/secondary progressive): 60 mg orally once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients (<18 years) have not been established
Indications
- Treatment of non-relapsing secondary progressive multiple sclerosis (investigational/under regulatory review)
Mechanism of Action
- Selective, brain-penetrant covalent inhibitor of Bruton's tyrosine kinase (BTK)
- Modulates B-cell activation and CNS microglia-driven neuroinflammation
Contraindications
- Hypersensitivity to tolebrutinib or any formulation excipients
- Severe hepatic impairment
- Active severe infections
Adverse Reactions
- Headache
- Nasopharyngitis
- Transient serum transaminase elevations (hepatotoxicity)
- Upper respiratory tract infections
- Diarrhea
Drug Interactions
- Strong CYP3A4 inhibitors may increase tolebrutinib exposure
- Strong CYP3A4 inducers may decrease tolebrutinib efficacy
- Concomitant immunosuppressive agents may increase infection risk
Curated Content: Needs Vetting Before Put to Clinical Use