Opzelura

[Manufacturer]: Incyte Company

[Specification] Each gram (1.5%) of white to off-white cream contains 15mg ruxolitinib.

[Trademark] Opzelura

[Chinese name] Ruxolitinib

[English name] ruxolitinib cream

[Properties] A white to off-white oil-in-water topical cream containing 1.5% ruxolitinib in a 60g aluminum tube

[Storage] Store at a temperature of 20℃-25℃, with an excursion of 15℃-30℃ allowed.

[Indications and uses]

It is used to treat patients with mild to moderate atopic dermatitis (AD) over 12 years old, and patients with vitiligo over 12 years old.

[Dosage and Administration]

Instruct patients to apply a thin layer of this product on the affected area not exceeding 20% ​​of the body surface area twice a day. The weekly dosage should not exceed 60g.

This product is for topical use only and is not for ophthalmic, oral or intravaginal use.

Discontinue use when the signs and symptoms of atopic dermatitis (e.g., itching, rash, redness) subside. If signs and symptoms do not improve within 8 weeks, the patient should be re-examined by a health care provider.

[Contraindications]

It is not recommended to use this product in combination with therapeutic biologics, other JAK inhibitors, or potent immunosuppressants (such as azathioprine or cyclosporine).

[Adverse reactions]

Common adverse reactions include: pain or swelling of the nose or throat (nasopharyngitis), diarrhea, bronchitis, ear infection, increased eosinophil (a type of white blood cell) count, hives, folliculitis, tonsillitis, and runny nose. In addition, the drug also carries a black box warning, reminding patients that the use of JAK inhibitors to treat inflammation may cause serious infections, mortality, malignant tumors, major adverse cardiovascular events and thrombosis.

[Warnings and Precautions]

Severe infection: Patients taking oral JAK inhibitors to treat inflammation are at risk for serious infection, which may result in hospitalization or death. Therefore, patients should be closely monitored for signs and symptoms of infection during and after treatment with this product. Avoid use in patients with active, serious infections, including localized infections. If serious infection occurs, this product needs to be discontinued immediately until the infection is controlled. Clinically reported infections include:

Active pulmonary tuberculosis, which may manifest as pulmonary or extrapulmonary disease

Invasive fungal infections, including candidiasis and pneumocystis disease

Bacterial, viral, and other infections caused by opportunistic pathogens

Mortality: Higher all-cause mortality, including sudden cardiovascular death, was observed in patients treated with oral JAK inhibitors for inflammation.

Malignancies: Lymphoma and other malignancies have been observed in patients treated with JAK inhibitors for inflammation.

Major adverse cardiovascular events: Higher rates of MACE (including cardiovascular death, myocardial infarction, and stroke) were observed in patients treated with JAK inhibitors for inflammation.

Thrombus: The incidence of thrombosis, including deep vein thrombosis, pulmonary embolism, and arterial thrombosis, was increased in patients treated with oral JAK inhibitors for inflammation compared with placebo. Patients with thrombotic symptoms should be promptly evaluated.

Low blood cell counts: This product may cause a low platelet count (thrombocytopenia), a low red blood cell count (anemia), and a low white blood cell count (neutropenia). If needed, your healthcare provider will do blood tests to check your blood counts during your treatment with this product and may stop your treatment if signs or symptoms of low blood counts occur. Tell healthcare provider right away if any of the following symptoms occur or worsen: unusual bleeding; shortness of breath; congestion; fever; tiredness.

Elevated cholesterol: If a patient has high levels of fat in the blood (high cholesterol or triglycerides), healthcare professionals need to take immediate action.

[General description]

Atopic dermatitis is a severe chronic, relapsing skin disease. The main symptoms are itching, dry skin and inflammation, which can appear anywhere on the body. Symptoms of moderate to severe atopic dermatitis are severe itching that causes visible damage to the skin. Like other chronic inflammatory diseases, atopic dermatitis is mediated by the immune system and is associated with complex interactions between immune cells and inflammatory cytokines.

[Mechanism of action]

Opzelura™ (ruxolitinib) cream is a Janus kinase (JAK) inhibitor that can selectively inhibit JAK1/JAK2. JAKs belong to a family of cytoplasmic tyrosine kinases whose function is to mediate the signal transduction of many cytokines (such as interferons) that are important for hematopoietic and immune functions. It modulates the activity of inflammatory factors associated with atopic dermatitis pathology and may directly modulate itch.

[Patient information]

1. Inform the patient to strictly follow the doctor’s instructions to take medication.

2. Advise patients to contact medical staff immediately if they experience any of the above adverse reactions (warnings and precautions).

3. Advise patients to proactively inform them of any other drugs they are taking, including prescription drugs, over-the-counter drugs, etc.