Overview
11 DESCRIPTION LITFULO (ritlecitinib) capsules are formulated with ritlecitinib tosylate, a kinase inhibitor. Ritlecitinib tosylate is a white to off white to pale pink solid which is freely soluble in water. The chemical name is 1-{(2S,5R)-2-Methyl-5-[(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}prop-2-en-1-one 4 methylbenzene-1-sulfonic acid.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action LITFULO is a kinase inhibitor. Ritlecitinib irreversibly inhibits Janus kinase 3 (JAK3) and the tyrosine kinase expressed in hepatocellular carcinoma (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. Additionally, ritlecitinib 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. 12.
Indications
- 1 INDICATIONS AND USAGE LITFULO is a kinase inhibitor indicated for the treatment of severe alopecia areata in adults and adolescents 12 years and older. Limitations of Use : Not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, cyclosporine or other potent immunosuppressants. LITFULO is a kinase inhibitor indicated for the treatment of severe alopecia areata in adults and adolescents 12 years and older.
Common Doses
- 50 mg
Dosage
2 DOSAGE AND ADMINISTRATION • For recommended testing, evaluations and immunizations prior to LITFULO initiation, see Full Prescribing Information. ( 2.1 ) • Recommended dosage is 50 mg orally once daily. ( 2.2 ) • For dosage interruption for certain adverse reactions, see Full Prescribing Information. ( 2.4 ) 2.1 Recommended Evaluations and Immunizations Prior to Treatment Initiation Perform the following evaluations prior to LITFULO initiation: • Tuberculosis (TB) infection evaluation: LITFULO initiation is not recommended in patients with active TB.
Black Box Warning
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), and THROMBOSIS WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), and THROMBOSIS See full prescribing information for complete boxed warning. • Increased risk of serious bacterial, fungal, viral, and opportunistic infections that may lead to hospitalization or death, including tuberculosis (TB). Interrupt treatment if serious infection occurs until the infection is controlled. LITFULO should not be given to patients with active tuberculosis.
Contraindications
- 4 CONTRAINDICATIONS LITFULO is contraindicated in patients with known hypersensitivity to ritlecitinib or any of its excipients [see Warnings and Precautions (5.6) ] . LITFULO is contraindicated in patients with known hypersensitivity to ritlecitinib or any of its excipients. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Serious Infections [see Warnings and Precautions (5.1) ] • Malignancy and Lymphoproliferative Disorders [see Warnings and Precautions (5.3) ] • Thromboembolic Events [see Warnings and Precautions (5.5) ] • Hypersensitivity [see Warnings and Precautions (5.6) ] • Laboratory Abnormalities [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS • Certain CYP3A substrates: Additional monitoring and dose adjustment of CYP3A substrate should be considered. ( 7.1 ) • Certain CYP1A2 substrates: Additional monitoring and dose adjustment of CYP1A2 substrate should be considered. ( 7.1 ) • Certain CYP3A inducers: Coadministration with strong inducers of CYP3A is not recommended. ( 7.2 ) 7.1 Effects of LITFULO on Other Drugs Table 3 includes clinically significant drug interactions affecting other drugs. Table 3.