【Manufacturer】Incyte Corporation
【Specifications】Cream:1.5% Ruxolitinib
【Trademark】Opzelura
【Generic Name】Ruxolitinib
【Storage】Store at 20°C to 25°C, with an allowable excursion range of 15°C to 30°C.
【Opzelura(Ruxolitinib Indications】
1. Atopic Dermatitis
Opzelura is indicated for the topical short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis in non-immunocompromised adult and pediatric patients 12 years of age and older, whose disease is not adequately controlled with topical prescription therapies, or when those therapies are not advisable.
2. Non-Segmental Vitiligo
Opzelura is indicated for the topical treatment of non-segmental vitiligo in adult and pediatric patients 12 years of age and older.
3. Usage Limitations
It is not recommended to use Opzelura in combination with therapeutic biologics, other JAK inhibitors, or potent immunosuppressants such as azathioprine or cyclosporine.
【Opzelura(Ruxolitinib ) Recommended Dosage and Administration】
A. Important Administration Information
Do not use more than 60 grams per week or exceed 100 grams every two weeks.
Opzelura is for topical use only and is not intended for ocular, oral, or intravaginal use.
B. Recommended Dosage for Atopic Dermatitis
Instruct patients to apply a thin layer of Opzelura to the affected areas twice daily, up to 20% of the body surface area. Discontinue use when signs and symptoms of atopic dermatitis (such as itching, rash, and redness) resolve. If symptoms and signs do not improve within 8 weeks, patients should seek medical re-evaluation.
C. Recommended Dosage for Non-Segmental Vitiligo
Instruct patients to apply a thin layer of Opzelura to the affected areas twice daily, up to 10% of the body surface area. Achieving significant repigmentation may require treatment with Opzelura for more than 24 weeks. If patients do not observe repigmentation within 24 weeks, they should seek medical re-evaluation.
【Opzelura(Ruxolitinib，Warnings and Precautions】
A. Serious Infections
Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported in patients receiving oral Janus kinase inhibitors. Severe lower respiratory tract infections were reported in the clinical development program of topical Ruxolitinib. Avoid use of Opzelura in patients with active serious infections, including localized infections. Consider the risks and benefits of treatment prior to initiating Opzelura in patients with chronic or recurrent infections, a history of serious or opportunistic infections, exposure to tuberculosis, or who have resided or traveled in areas of endemic tuberculosis or endemic mycoses; or have underlying conditions that may predispose them to infection. Closely monitor patients for the development of signs and symptoms of infection during and after Opzelura treatment. If a patient develops a serious infection, opportunistic infection, or sepsis, interrupt Opzelura. Do not resume therapy until the infection is controlled.
Tuberculosis: No cases of active tuberculosis (TB) were reported in Opzelura clinical trials. Cases of active TB have been reported in clinical trials of oral Janus kinase inhibitors used for the treatment of inflammation. Consider evaluating patients for latent and active TB infection prior to initiating Opzelura. Monitor patients for the development of signs and symptoms of TB during Opzelura use.
Viral Reactivation: Cases of viral reactivation, including herpes virus reactivation (e.g., herpes zoster), have been reported in clinical trials of Janus kinase inhibitors used for the treatment of inflammatory conditions, including Opzelura. If a patient develops herpes zoster, consider interrupting Opzelura treatment until the episode resolves.
Hepatitis B and C: The impact of Janus kinase inhibitors used for the treatment of inflammation, including Opzelura, on chronic viral hepatitis reactivation is not known. Patients with a history of hepatitis B or C infection were excluded from clinical trials. Increases in hepatitis B virus (HBV) DNA titers have been reported in chronic HBV-infected patients receiving oral Ruxolitinib, with or without associated elevations in alanine aminotransferase and aspartate aminotransferase. Opzelura is not recommended in patients with active hepatitis B or C.
B. Mortality
In a large, randomized, postmarketing safety study of an oral JAK inhibitor in patients 50 years of age and older with at least one cardiovascular risk factor, a higher rate of all-cause mortality, including sudden cardiovascular death, was observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. Consider the benefits and risks for the individual patient prior to initiating or continuing therapy with Opzelura.
C. Malignancy and Lymphoproliferative Disorders
Malignancies, including lymphoma, have been observed in clinical trials of oral JAK inhibitors used for the treatment of inflammatory conditions. Patients who are current or past smokers are at additional increased risk. In a large, randomized, postmarketing safety study of an oral JAK inhibitor in RA patients, a higher rate of malignancies (excluding non-melanoma skin cancer) was observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. A higher rate of lymphoma was observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. A higher rate of lung cancer was observed in current or past smokers treated with the JAK inhibitor compared to those treated with TNF blockers.
In this study, current or past smokers had an additional increased risk of malignancies. Consider the benefits and risks for the individual patient prior to initiating or continuing therapy with Opzelura, particularly in patients with a known malignancy (other than successfully treated non-melanoma skin cancer), patients who develop a malignancy during treatment, and patients who are current or past smokers.
D. Non-Melanoma Skin Cancer
Non-melanoma skin cancers, including basal cell carcinoma and squamous cell carcinoma, have occurred in patients treated with Opzelura. Perform periodic skin examinations during Opzelura treatment and as appropriate following treatment. Exposure to sunlight and UV light should be limited by wearing protective clothing and using broad-spectrum sunscreen.
E. Major Adverse Cardiovascular Events (MACE)
In a large, randomized, postmarketing safety study of an oral JAK inhibitor in RA patients 50 years of age and older with at least one cardiovascular risk factor, a higher rate of major adverse cardiovascular events (MACE) (defined as cardiovascular death, non-fatal myocardial infarction (MI), and non-fatal stroke) was observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. Current or past smokers are at additional increased risk. Consider the benefits and risks for the individual patient prior to initiating or continuing therapy with Opzelura, particularly in patients who are current or past smokers and those with other cardiovascular risk factors. Inform patients about the symptoms of serious cardiovascular events and what to do if they occur. Patients who experience a myocardial infarction or stroke should discontinue Opzelura.
F. Thrombosis
Thromboembolic events have been observed in Opzelura clinical trials. Thrombosis, including deep vein thrombosis (DVT), pulmonary embolism (PE), and arterial thrombosis, has been reported in patients receiving Janus kinase inhibitors used for the treatment of inflammatory conditions. Many of these adverse reactions were serious and some resulted in death. In a large, randomized, postmarketing safety study of an oral JAK inhibitor in RA patients 50 years of age and older with at least one cardiovascular risk factor, a higher rate of overall thrombosis, DVT, and PE was observed in patients treated with the JAK inhibitor compared to those treated with TNF blockers. Avoid use of Opzelura in patients at increased risk of thrombosis. If symptoms of thrombosis occur, discontinue Opzelura and evaluate and treat the patient appropriately.
G. Thrombocytopenia, Anemia, and Neutropenia
Thrombocytopenia, anemia, and neutropenia have been reported in Opzelura clinical trials. Consider the benefits and risks for patients with a known history of these events prior to initiating Opzelura. Monitor complete blood counts as clinically indicated. If clinically significant thrombocytopenia, anemia, and neutropenia develop, discontinue Opzelura.
H. Elevated Lipid Parameters
Treatment with oral Ruxolitinib has been associated with increases in lipid parameters, including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides.
【Opzelura(Ruxolitinib）Conteaindications】
No information available.
【Opzelura(Ruxolitinib Drug Interactions】
No drug interaction studies have been conducted with Opzelura. Ruxolitinib is a known substrate of cytochrome P450 3A4 (CYP3A4). CYP3A4 inhibitors may increase systemic concentrations of Ruxolitinib, while CYP3A4 inducers may decrease systemic concentrations of Ruxolitinib.
1. Strong CYP3A4 Inhibitors
Avoid concomitant use of Opzelura with strong CYP3A4 inhibitors due to the potential for increased systemic exposure of Ruxolitinib and increased risk of adverse reactions with Opzelura.
【Opzelura(Ruxolitinib Adverse Reactions】
1. Opzelura may cause serious side effects, including: hives, difficulty breathing, swelling of the face, lips, tongue, or throat, severe dizziness, abnormal laboratory results, unusual bleeding, shortness of breath, bruising, fever, and fatigue. If you experience any of the above symptoms, seek medical attention immediately.
2. The most common side effects of Opzelura include: pain or swelling of the nose or throat, diarrhea, bronchitis, ear infection, increased white blood cell (eosinophil) count, hives, inflamed hair follicles (folliculitis), swollen tonsils (tonsillitis), and runny nose.
【Opzelura(Ruxolitinib Use in Specific Population】
1. Pregnancy
Available pregnancy data from Opzelura clinical trials are insufficient to assess the drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of Ruxolitinib to pregnant rats and rabbits during organogenesis resulted in adverse developmental outcomes at doses associated with maternal toxicity.
2. Lactation
There are no data on the presence of Ruxolitinib in human milk, the effects on the breastfed child, or the effects on milk production. Ruxolitinib is present in the milk of lactating rats. When a drug is present in animal milk, it is likely that the drug is present in human milk. Due to the potential for serious adverse reactions in adults, including the risk of serious infections, thrombocytopenia, anemia, and neutropenia, advise women not to breastfeed during treatment with Opzelura and for approximately four weeks (about 5-6 elimination half-lives) after the last dose.
3. Pediatric Use
Atopic Dermatitis: The safety and efficacy of Opzelura for the topical treatment of mild to moderate atopic dermatitis have been established in pediatric patients 12 to 17 years of age. Evidence supporting the use of Opzelura in this age group is derived from TRuE-AD1 and TRuE-AD2, which included 92 pediatric subjects 12 to 17 years of age with mild to moderate atopic dermatitis. No clinically meaningful differences in safety or efficacy were observed between adult and pediatric subjects. The safety and efficacy of Opzelura in pediatric patients younger than 12 years of age with atopic dermatitis have not been established.
Non-Segmental Vitiligo: The safety and efficacy of Opzelura for the topical treatment of non-segmental vitiligo have been established in pediatric patients 12 to 17 years of age. Evidence supporting the use of Opzelura in this age group is derived from TRuE-V1 and TRuE-V2, which included 55 pediatric subjects 12 to 17 years of age with non-segmental vitiligo. No clinically meaningful differences in safety or efficacy were observed between adult and pediatric subjects. The safety and efficacy of Opzelura in pediatric patients younger than 12 years of age with non-segmental vitiligo have not been established.
4. Geriatric Use
Of the 1249 subjects with atopic dermatitis in Opzelura clinical trials, 115 (9%) were 65 years of age and older. No clinically meaningful differences in safety or efficacy were observed between subjects younger than 65 years of age and those 65 years of age and older.
Of the 831 subjects with non-segmental vitiligo in Opzelura clinical trials, 65 (8%) were 65 years of age and older. Opzelura clinical trials in subjects with non-segmental vitiligo did not include sufficient numbers of subjects 65 years of age and older to determine whether they respond differently from younger adult subjects.
【Opzelura(Ruxolitinib General Description】
Phosphorylated Ruxolitinib is a Janus kinase inhibitor with a molecular weight of 404.36 g/mol. Phosphorylated Ruxolitinib has the following structural formula:
The structural formula of phosphorylated Ruxolitinib
Phosphorylated Ruxolitinib is a white to off-white to pale yellow to pale pink powder.
Opzelura (Ruxolitinib) cream is a white to off-white, oil-in-water, dissolvable topical emulsion.
Each gram of Opzelura contains 15 mg of Ruxolitinib (equivalent to 19.8 mg of Ruxolitinib phosphate) in a cream base consisting of cetyl alcohol, dimethicone 350, disodium EDTA, glyceryl stearate SE, light mineral oil, medium-chain triglycerides, methylparaben, phenoxyethanol, polyethylene glycol 200, polysorbate 20, propylene glycol, propylparaben, stearyl alcohol, purified water, white petrolatum, and xanthan gum.
【Opzelura(Ruxolitinib Mechanism of Action】
Ruxolitinib, a Janus kinase (JAK) inhibitor, inhibits JAK1 and JAK2, which mediate the signaling of many cytokines and growth factors important for hematopoiesis and immune function. JAK signaling involves the 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. The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.
【Opzelura(Ruxolitinib Patient Information】
1. Infections: Inform patients that the risk of infections, including serious infections, may increase while using Opzelura. Advise patients to seek medical attention immediately if they develop any signs or symptoms of infection. Inform patients that Janus kinase inhibitors increase the risk of herpes zoster.
2. Malignancy and Lymphoproliferative Disorders: Inform patients that Janus kinase inhibitors may increase the risk of lymphoma and other malignancies, including skin cancer. Instruct patients to inform their healthcare provider if they have any type of cancer. Advise patients to have periodic skin examinations while using Opzelura. Recommend that patients limit exposure to sunlight and UV light by wearing protective clothing and using broad-spectrum sunscreen.
3. Major Adverse Cardiovascular Events: Inform patients that major adverse cardiovascular events (MACE), including non-fatal myocardial infarction, non-fatal stroke, and cardiovascular death, have been reported in clinical studies of Janus kinase inhibitors for the treatment of inflammatory conditions. Instruct all patients, particularly current or past smokers or those with other cardiovascular risk factors, to be alert for the development of signs and symptoms of cardiovascular events.
4. Thrombosis: Inform patients that deep vein thrombosis (DVT) and pulmonary embolism (PE) events have been reported in clinical studies of Janus kinase inhibitors for the treatment of inflammatory conditions. Instruct patients to seek medical attention immediately if they develop any signs or symptoms of DVT or PE.
5. Thrombocytopenia, Anemia, and Neutropenia: Advise patients of the risk of thrombocytopenia, anemia, and neutropenia with Opzelura. Instruct patients to inform their healthcare provider if they develop any signs or symptoms of thrombocytopenia, anemia, or neutropenia.
6. Administration Instructions: Inform patients that Opzelura is for topical use only.
7. Dosage: Advise patients not to use more than 60 grams per week or exceed 100 grams every two weeks.
8. Lactation: Advise patients not to breastfeed during treatment with Opzelura and for approximately four weeks after the last dose.
Information Source:
[1]https://www.rxlist.com/opzelura-drug.htm#description
[2]https://www.fda.gov/drugs/resources-information-approved-drugs/fda-disco-burst-edition-fda-approval -Opzelura
[3] https://ndclist.com/ndc/52652-8001
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