Deuruxolitinib

LEQSELVI ® is indicated for the treatment of adult patients with severe alopecia areata. Limitations of Use LEQSELVI is not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, cyclosporine, or other potent immunosuppressants. LEQSELVI is a Janus kinase (JAK) inhibitor indicated for the treatment of adults with severe alopecia areata.

Deuruxolitinib is a Janus kinase (JAK) inhibitor. JAKs mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function. JAK signaling involves recruitment of STATs (signal transducers and activators of transcription) to cytokine receptors, activation and subsequent localization of STATs to the nucleus leading to modulation of gene expression. In an in vitro kinase activity assay, deuruxolitinib had greater inhibitory potency for JAK1, JAK2 and TYK2 relative to JAK3. The relevance of inhibition of JAK enzymes to therapeutic effectiveness is not currently known.

For recommended testing, evaluations, and procedures prior to and during LEQSELVI treatment, see Full Prescribing Information. Recommended dosage is 8 mg twice daily. For treatment interruption for certain adverse reactions, see Full Prescribing Information.

LEQSELVI is contraindicated in patients who: Are CYP2C9 poor metabolizers. Are on concomitant moderate or strong CYP2C9 inhibitors. Using moderate or strong CYP2C9 inhibitors.

Boxed warning (serious infections, mortality, malignancy, major adverse cardiovascular events, and thrombosis): Increased risk of serious bacterial, fungal, viral and opportunistic infections, including tuberculosis (TB), that may lead to hospitalization or death. Interrupt treatment with LEQSELVI if a serious infection occurs until the infection is controlled. LEQSELVI treatment is not recommended in patients with active tuberculosis. Increased Risk of LEQSELVI-Associated Serious Adverse Reactions in CYP2C9 Poor Metabolizers or with Concomitant Use of Moderate or Strong CYP2C9 Inhibitors: LEQSELVI is contraindicated in patients who are CYP2C9 poor metabolizers or patients taking a moderate or strong CYP2C9 inhibitor. Gastrointestinal Perforations: Monitor patients who may be at increased risk for gastrointestinal perforation.

The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections Malignancy and Lymphoproliferative Disorders Thrombosis Gastrointestinal perforations Lipid Elevations, Anemia, Neutropenia and Lymphopenia Most common adverse reactions (≥1%) are: headache, acne, nasopharyngitis, blood creatine phosphokinase increased, hyperlipidemia, fatigue, weight increased, lymphopenia, thrombocytosis, anemia, skin and soft tissue infections, neutropenia, and herpes.

Effect of Other Drugs on LEQSELVI Strong CYP3A and moderate or strong CYP2C9 inducers: Avoid concomitant use of LEQSELVI with strong CYP3A and moderate or strong CYP2C9 inducers. Deuruxolitinib is a CYP2C9 and CYP3A substrate. Concomitant use with a strong CYP3A and moderate or strong CYP2C9 inducer decreases deuruxolitinib exposure (C max and AUC), which may reduce LEQSELVI efficacy. Moderate or strong CYP2C9 inhibitors: LEQSELVI is contraindicated in patients taking moderate or strong CYP2C9 inhibitors. Deuruxolitinib is a CYP2C9 substrate. Concomitant use with a moderate or strong CYP2C9 inhibitor is estimated to increase deuruxolitinib exposure (C max and AUC), which may increase the risk of LEQSELVI serious adverse reactions such as thrombosis. Strong CYP3A4 and moderate or strong CYP2C9 inducers: Avoid concomitant use. Moderate or strong CYP2C9 inhibitors: Contraindicated.

Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F and 86°F). Store in the original bottle to protect from moisture.