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Litfulo (Ritlecitinib Tosylate)
Ritlecitinib irreversibly inhibits JAK3 and TEC kinase family by blocking ATP binding site.
LITFULO (ritlecitinib tosylate) is a JAK3/TEC kinase inhibitor approved for severe alopecia areata in patients 12 years and older. The drug demonstrates dose-proportional pharmacokinetics with rapid absorption (Tmax 1 hour), moderate protein binding (14%), and short half-life (1.3-2.3 hours), requiring metabolism through multiple pathways. Key risks include CYP3A and CYP1A2 inhibition requiring dose adjustments of concomitant substrates, and contraindication in patients with hypersensitivity or severe hepatic impairment. Not recommended for combination use with other JAK inhibitors, biologic immunomodulators, cyclosporine, or potent immunosuppressants.
At a glance
| Generic name | Ritlecitinib Tosylate |
|---|---|
| Sponsor | Pfizer |
| Drug class | Kinase inhibitor |
| Target | Janus kinase 3 (JAK3) and tyrosine kinase expressed in hepatocellular carcinoma (TEC) kinase family |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 2023 |
Mechanism of action
Ritlecitinib is a kinase inhibitor that irreversibly inhibits JAK3 and the TEC kinase family by blocking the adenosine triphosphate (ATP) binding site. In cellular settings, ritlecitinib inhibits cytokine-induced STAT phosphorylation mediated by JAK3-dependent receptors and inhibits signaling of immune receptors dependent on TEC kinase family members. The relevance of inhibition of specific JAK or TEC family enzymes to therapeutic effectiveness is not currently known.
Approved indications
- Alopecia areata
Common side effects
- Headache
- Diarrhea
- Acne
- Rash
- Urticaria
- Folliculitis
- Pyrexia
- Dermatitis atopic
- Dizziness
- Blood creatine phosphokinase increased
- Herpes zoster
- Red blood cell count decreased
Drug interactions
- CYP3A substrates (where small concentration changes may lead to serious adverse reactions)
- CYP1A2 substrates (where small concentration changes may lead to serious adverse reactions)
- Strong CYP3A inducers (e.g., rifampin)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| FDA Orange Book | Patents + exclusivity |