Brand Name
Litfulo
Generic Name
Ritlecitinib
View Brand Information FDA approval date: July 06, 2023
Classification: Kinase Inhibitor
Form: Capsule
What is Litfulo (Ritlecitinib)?
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. Limitations of Use : Not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, cyclosporine or other potent immunosuppressants .
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Brand Information
Litfulo (ritlecitinib)
1INDICATIONS 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.
2DOSAGE FORMS AND STRENGTHS
Capsules: 50 mg of ritlecitinib, size 3, opaque capsules with yellow body and blue cap. The body is printed with “RCB 50” and the cap is printed with “Pfizer” in black.
3CONTRAINDICATIONS
LITFULO is contraindicated in patients with known hypersensitivity to ritlecitinib or any of its excipients
4ADVERSE REACTIONS
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Serious Infections
- Malignancy and Lymphoproliferative Disorders
- Thromboembolic Events
- Hypersensitivity
- Laboratory Abnormalities
4.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety of LITFULO was evaluated in three randomized, placebo-controlled clinical trials and one long-term trial in subjects with alopecia areata, including alopecia totalis and alopecia universalis, who were 12 years of age and older. A total of 1628 subjects were treated with LITFULO representing 2085 subject-years of exposure. There were 1011 subjects with at least 1 year of exposure to LITFULO. In the placebo-controlled period of clinical trials in alopecia areata, a total of 668 subjects were exposed to LITFULO with 130 receiving 50 mg once daily for up to 24 weeks. The median age of subjects was 33 years, 105 (11.9%) subjects were 12 to <18 years old and 22 (2.5%) subjects were 65 years of age or older. The majority of subjects were White (70.7%) and female (63.6%).
Adverse reactions occurring at ≥1% in the treated groups and at a higher rate than placebo are presented in Table 2. A total of 2 (1.5%) subjects treated with LITFULO 50 mg were discontinued from the trials due to adverse reactions.
Specific Adverse Reactions
Exposure adjusted incidence rates were adjusted by clinical trial size for all adverse reactions reported in this section.
Overall Infections
In the placebo-controlled trials, for up to 24 weeks, overall infections were reported in 66 subjects (80.35 per 100 subject-years) treated with placebo and 43 subjects (74.53 per 100 subject-years) treated with LITFULO 50 mg. Across clinical trials, including the long-term trial, overall infections were reported in 645 subjects (50.71 per 100 subject-years) treated with LITFULO 50 mg or higher.
Serious Infections
In the placebo-controlled trials, for up to 24 weeks, 3 subjects reported serious infections across all ritlecitinib doses studied. Across clinical trials, including the long-term trial, serious infections were reported in 12 subjects (0.66 per 100 subject-years) treated with LITFULO 50 mg or higher. The most common serious infections were related to appendicitis, COVID-19 infection (including pneumonia), and sepsis.
Herpes Zoster
In the placebo-controlled trials, for up to 24 weeks, herpes zoster was reported in 4 subjects across all ritlecitinib doses studied and 0 subjects treated with placebo. Across clinical trials, including the long-term trial, herpes zoster was reported in 21 subjects (1.17 per 100 subject-years) treated with LITFULO 50 mg or higher. Opportunistic infections of multi-dermatomal herpes zoster were reported in 1 subject (0.50 per 100 subject-years) treated with the ritlecitinib higher dose in the placebo-controlled trials and 2 subjects (0.1 per 100 subject-years) treated with LITFULO 50 mg or higher in all clinical trials.
Malignancy
In the placebo-controlled trials, for up to 24 weeks, 1 malignancy (breast cancer) was reported in 1 subject (1.33 per 100 subject-years) treated with ritlecitinib higher dose and no malignancy was reported in subjects treated with placebo. Across clinical trials, including the long-term trial, malignancies excluding NMSC were reported in 7 subjects (0.37 per 100 subject-years) treated with LITFULO 50 mg or higher.
Thromboembolic Events
Across clinical trials, including the long-term trial, pulmonary embolism (PE) was reported in 1 subject (0.06 per 100 subject-years) treated with LITFULO. There was 1 report of retinal artery occlusion and 1 report of acute myocardial infarction.
Urticaria
In the placebo-controlled trials, for up to 24 weeks, urticaria was reported in 28 subjects treated in all ritlecitinib doses studied and 3 subjects treated with placebo. The rate of urticaria was 8.23 per 100 subject-years in subjects treated with ritlecitinib 50 mg and 4.03 per 100 subject-years in subjects treated with placebo. Across clinical trials, including the long-term trial, urticaria was reported in 76 subjects treated with LITFULO 50 mg or higher. Among all subjects treated with ritlecitinib 50 mg or higher in the integrated safety analysis, the rate of urticaria was 4.10 per 100 subject-years. The median time to onset of an initial event was 8 weeks; median duration of urticaria was 7 days. Most of the cases were mild to moderate in severity.
Decreased Lymphocyte Counts
Across clinical trials, including the long-term trial confirmed ALC <500/mm
Decreased Platelet Count
In the placebo-controlled trials, for up to 24 weeks, treatment with LITFULO was associated with a decrease in platelet count. Maximum effects on platelets were observed within 4 weeks, after which platelet count remained stable at a lower level with continued therapy. Across clinical trials, including the long-term trial, 1 subject (<0.1%) had a confirmed platelet count <100,000/mm
Creatine Phosphokinase (CPK) Elevations
In the placebo-controlled trials, for up to 24 weeks, events of blood CPK increased were reported in 2 (1.5%) subjects treated with LITFULO 50 mg and 0 subjects treated with placebo.
Liver Enzyme Elevations
In the placebo-controlled trials, for up to 24 weeks, events of increases in liver enzymes ≥3 times the upper limit of normal (ULN) were observed in subjects treated with LITFULO
5OVERDOSAGE
LITFULO was administered in clinical trials up to a single oral dose of 800 mg. Adverse reactions were comparable to those seen at lower doses and no specific toxicities were identified. Pharmacokinetics (PK) data up to and including a single oral dose of 800 mg in healthy adult volunteers indicate that more than 90% of the administered dose is expected to be eliminated within 48 hours.
There is no specific antidote for overdose with LITFULO. Treatment should be symptomatic and supportive, and monitor patients for signs and symptoms of adverse reactions
In case of an overdose, call Poison Control Center at 1-800-222-1222 for latest recommendations.
6DESCRIPTION
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.
The molecular formula for ritlecitinib tosylate is C
LITFULO is supplied for oral administration as a 50 mg immediate-release capsule. Each capsule contains 50 mg ritlecitinib (equivalent to 80.13 mg ritlecitinib tosylate) and the following inactive ingredients: crospovidone, glyceryl dibehenate, lactose monohydrate, microcrystalline cellulose, and hypromellose (HPMC) capsule shells. The yellow/blue, opaque capsule shells contain Brilliant blue FCF – FD&C Blue, hypromellose, titanium dioxide, and yellow iron oxide.
7CLINICAL STUDIES
The efficacy and safety of LITFULO were evaluated in one randomized, double-blind, placebo-controlled trial (Trial AA-I) in subjects 12 years of age and older with alopecia areata with ≥50% scalp hair loss, including alopecia totalis (AT) and alopecia universalis (AU).
Trial AA-I evaluated a total of 718 subjects who were randomized to one of the following treatment regimens for 48 weeks: 1) 200 mg once daily for 4 weeks followed by 50 mg once daily for 44 weeks; 2) 200 mg once daily for 4 weeks followed by 30 mg once daily for 44 weeks; 3) 50 mg once daily for 48 weeks; 4) 30 mg once daily for 48 weeks; 5) 10 mg once daily for 48 weeks; 6) placebo for 24 weeks followed by 200 mg once daily for 4 weeks and 50 mg once daily for 20 weeks; or 7) placebo for 24 weeks followed by 50 mg once daily for 24 weeks.
The recommended dose of LITFULO is 50 mg once daily and the results for this dose are discussed below.
Across all treatment groups 62% of subjects were female, 68% were White, 26% were Asian, and 4% were Black or African American. The majority of subjects (85%) were adults (≥18 years of age) with a mean age of 33.7 years. A total of 105 (15%) subjects 12 to <18 years of age and 20 (3%) subjects 65 years of age and older were enrolled. The mean baseline Severity of Alopecia Tool (SALT) score ranged from 88.3 to 93.0 across treatment groups; among subjects without AT/AU at baseline, the mean SALT score ranged from 78.3 to 87.0. The majority of subjects had abnormal eyebrows (83%) and eyelashes (75%) at baseline across treatment groups. The median duration since alopecia areata diagnosis was 6.9 years and the median duration of the current alopecia areata episode was 2.5 years. Randomization was stratified by AT/AU status with 46% of subjects classified as AT/AU based upon a baseline SALT score of 100.
8HOW SUPPLIED/STORAGE AND HANDLING
LITFULO capsules are packaged in child-resistant, white, high-density polyethylene (HDPE) bottles with polypropylene (PP) cap with a foil heat induction seal liner. The bottles contain 1g of desiccant in a high-density polyethylene (HDPE) canister. Do not eat the desiccant.
9PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Medication Guide).
10PRINCIPAL DISPLAY PANEL - 50 mg Capsule Bottle Label Sample
PROFESSIONAL SAMPLE – NOT FOR SALE
NDC 63539-334-28
Pfizer
Litfulo™
50 mg*
Do not crush, split, or chew the capsules
28 Capsules
