Ruxolitinib cream

Ruxolitinib cream (brand name Opzelura) is used to treat atopic dermatitis (eczema) and nonsegmental vitiligo. It is applied twice a day to the affected areas.

Ruxolitinib works by blocking specific proteins called JAK1 and JAK2 that send "grow and multiply" signals to blood cells and immune cells. By stopping these signals, ruxolitinib cream decreases harmful inflammation in skin conditions such as atopic dermatitis and nonsegmental vitiligo by suppressing inflammatory cytokines. It belongs to the drug class called kinase inhibitors.

Oral ruxolitinib first gained FDA approval on November 16, 2011, under the brand name Jakafi. Ruxolitinib cream was FDA-approved on September 21, 2021, under the brand name Opzelura. There is no generic ruxolitinib cream or tablets.

FDA approvals and uses

Topical ruxolitinib is FDA-approved for:

• Mild to moderate atopic dermatitis in non-immunocompromised adults and children 2 years of age and older whose disease is not adequately controlled with topical prescription therapies or when those therapies are not advisable (short-term and non-continuous chronic treatment only)
• Nonsegmental vitiligo in adults and children 12 years of age and older.

The use of ruxolitinib cream along with therapeutic biologics, other JAK inhibitors, or strong immunosuppressants such as azathioprine or cyclosporine is not recommended.

It is not known if this medicine is safe and effective in children less than 2 years of age with atopic dermatitis or in children less than 12 years of age with nonsegmental vitiligo.

Important: Ruxolitinib cream is for use on the skin only. Do not use in your eyes, mouth, or vagina.

Ruxolitinib cream is for use on the skin only. Do not use ruxolitinib cream in your eyes, mouth, or vagina. Use it exactly as your healthcare provider tells you. Ask your healthcare provider if you have questions about applying ruxolitinib cream.

• Apply a thin layer of ruxolitinib cream 2 times a day to affected areas.

If you are using ruxolitinib cream for atopic dermatitis:

• Do not use ruxolitinib cream with tight bandages that cover and seal the skin (occlusive dressings).
• Adults and children 12 years of age and older: do not use more than one 60-gram tube each week or more than one 100-gram tube every 2 weeks.
• Children 2 to 11 years of age: do not use more than one 60-gram tube every 2 weeks.
• Stop using ruxolitinib cream when your signs and symptoms of atopic dermatitis, such as itching, rash, and redness, go away, or as directed by your healthcare provider. Tell your healthcare provider if your symptoms do not improve within 8 weeks of treatment.

If you are using ruxolitinib cream for nonsegmental vitiligo:

• Do not use more than one 60-gram tube each week or more than one 100-gram tube every 2 weeks.
• Tell your healthcare provider if your treated skin does not improve within 24 weeks of treatment.

Wash your hands after applying ruxolitinib cream, unless your hands are being treated. If someone else applies ruxolitinib cream, they should wash their hands after applying it.

Common side effects

The most common side effects of ruxolitinib cream for atopic dermatitis are:

• common cold (nasopharyngitis)
• diarrhea
• bronchitis
• ear infection
• increase in a type of white blood cell (eosinophil) count, or decrease in a type of white blood cell (neutrophil) count (neutropenia)
• hives (urticaria)
• inflamed hair pores (folliculitis)
• swelling of the tonsils (tonsillitis)
• runny nose (rhinorrhea)
• upper respiratory tract infection
• COVID-19
• pain, irritation, discomfort, or itching at the application site
• fever (pyrexia).

The most common side effects of ruxolitinib cream for nonsegmental vitiligo are:

• acne at the application site
• itching at the application site
• common cold (nasopharyngitis)
• headache
• urinary tract infection
• redness at the application site
• fever.

Serious side effects and warnings

Ruxolitinib (either oral or topical) can cause the following serious side effects:

• Serious infections. Ruxolitinib belongs to a class of medicines called Janus kinase (JAK) inhibitors, which affect your immune system and can lower its ability to fight infections. Some people have had serious infections while taking oral JAK inhibitors, including tuberculosis (TB) and infections caused by bacteria, fungi, or viruses that can spread throughout the body. Some people have been hospitalized or died from these infections. Some people have had serious infections of their lungs while using ruxolitinib cream. Ruxolitinib cream should not be used if you have an active, serious infection. Tell your healthcare provider if you develop any symptoms of infection, such as: fever, sweating, or chills muscle aches cough or shortness of breath blood in your phlegm weight loss warm, red, or painful skin or sores on your body diarrhea or stomach pain burning when you urinate or urinating more often than usual feeling very tired.
• Increased risk of death due to any reason (all causes). Increased risk of death has occurred in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking an oral JAK inhibitor.
• Cancer and immune system problems. Ruxolitinib may increase your risk of certain cancers by changing the way your immune system works. Lymphoma and other cancers, including lung cancer, have happened in people taking oral JAK inhibitors, especially in current or past smokers. Some people have had non-melanoma skin cancers while using ruxolitinib cream. Your healthcare provider will regularly check your skin during treatment. Limit time in sunlight, wear protective clothing, and use a broad-spectrum sunscreen. Tell your healthcare provider if you have ever had any type of cancer.
• Increased risk of major cardiovascular events. Increased risk of major cardiovascular events such as heart attack, stroke, or death, has occurred in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking oral JAK inhibitors, especially in current or past smokers. Get emergency help right away if you have any symptoms of a heart attack or stroke while taking ruxolitinib, including: discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back severe tightness, pain, pressure, or heaviness in your chest, throat, neck, or jaw pain or discomfort in your arms, back, neck, jaw, or stomach shortness of breath with or without chest discomfort breaking out in a cold sweat nausea or vomiting feeling lightheaded weakness in one part or on one side of your body slurred speech.
• Blood clots. Blood clots in the veins of your legs (deep vein thrombosis, DVT) or lungs (pulmonary embolism, PE) can happen in some people using ruxolitinib and may be life-threatening. These have happened more often in people 50 years of age and older with at least 1 heart disease risk factor taking oral JAK inhibitors. Tell your healthcare provider right away if you have any signs or symptoms of blood clots during treatment, including: swelling, pain, or tenderness in one or both legs sudden, unexplained chest or upper back pain shortness of breath or difficulty breathing.
• Low blood cell counts. Ruxolitinib may cause low platelet counts (thrombocytopenia), low red blood cell counts (anemia), and low white blood cell counts (neutropenia, lymphopenia, and leukopenia). If needed, your healthcare provider will do a blood test to check your blood cell counts during treatment and may stop your treatment if signs or symptoms of low blood cell counts happen. Tell your healthcare provider right away if you develop or have worsening of any of these symptoms: unusual bleeding bruising tiredness shortness of breath fever.
• Potential risks related to JAK inhibition. Increases in cholesterol have happened in people taking oral JAK inhibitors. Tell your healthcare provider if you have high levels of fat in your blood (high cholesterol or triglycerides). Low blood sugar (hypoglycemia) in people with diabetes has also happened after taking oral JAK inhibitors.

These are not all the possible side effects of ruxolitinib. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects to Incyte Corporation at 1-855-463-3463.

Before applying topical ruxolitinib, tell your healthcare provider about all of your medical conditions, including if you:

• have an infection, an infection that will not go away or keeps coming back, or symptoms of an infection
• have diabetes, chronic lung disease, HIV, or a weak immune system
• have or have had low white or red blood cell counts
• have or had tuberculosis (TB), or have been in close contact with someone who has TB
• have had shingles (herpes zoster)
• have or have had hepatitis B or C
• live in, have lived in, or have traveled to areas where certain fungal infections are common (such as the Ohio and Mississippi River valleys and the Southwest)
• have high levels of fat in your blood (high cholesterol or triglycerides)
• have had cancer
• are a current or past smoker
• have had a blood clot, heart attack, other heart problems, or stroke
• are pregnant or plan to become pregnant. It is not known if ruxolitinib will harm your unborn baby. There is a pregnancy exposure registry for individuals who use ruxolitinib cream during pregnancy; you and your healthcare provider can report an exposure to Incyte Corporation at 1-855-463-3463.
• are breastfeeding or plan to breastfeed. It is not known if ruxolitinib passes into your breast milk. Do not breastfeed during treatment with ruxolitinib and for about 4 weeks after the final dose.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Dose of ruxolitinib cream for atopic dermatitis

• Apply a thin layer 2 times a day to affected areas of up to 20% body surface area.
• Do not use with occlusive dressings.
• Maximum: adults and children 12 years and older: one 60-gram tube per week or one 100-gram tube per 2 weeks children 2 to 11 years: one 60-gram tube per 2 weeks.

Dose of ruxolitinib cream for nonsegmental vitiligo

• Apply a thin layer 2 times a day to affected areas of up to 10% body surface area.
• Maximum: one 60-gram tube per week or one 100-gram tube per 2 weeks.

If you miss a dose of ruxolitinib, apply your next dose at your regular time. Do not apply 2 doses at the same time.

If you apply too much ruxolitinib, call your healthcare provider or go to the nearest hospital emergency room right away.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking ruxolitinib with certain other medicines may affect how ruxolitinib works. Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Store ruxolitinib cream at room temperature, 68°F to 77°F (20°C to 25°C).

Keep out of the reach of children.

Active ingredient: ruxolitinib phosphate 1.5%

Inactive ingredients (Opzelura): cetyl alcohol, dimethicone 350, edetate disodium, glyceryl stearate SE, light mineral oil, medium chain triglycerides, methylparaben, phenoxyethanol, phosphoric acid, polyethylene glycol 200, polysorbate 20, propylene glycol, propylparaben, stearyl alcohol, purified water, white petrolatum, and xanthan gum.

Available in 60-gram and 100-gram tubes.

Ruxolitinib cream is made by Incyte Corporation under the brand Opzelura. Incyte is located at 1801 Augustine Cut-off, Wilmington, DE 19803.