Currently Enrolling Trials
Opzelura is a topical cream formulation of ruxolitinib, a Janus kinase (JAK) inhibitor.
Opzelura is specifically indicated for the topical short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis in non-immunocompromised patients 12 years of age and older whose disease is not adequately controlled with topical prescription therapies or when those therapies are not advisable.
Opzelura is supplied as a cream for topical use. A thin layer of Opzelura should be applied twice daily to affected areas of up to 20% body surface area. Do not use more than 60 grams per week. Stop using when signs and symptoms (e.g., itch, rash, and redness) of atopic dermatitis resolve. If signs and symptoms do not improve within 8 weeks, patients should be reexamined by their healthcare provider.
Mechanism of Action
Opzelura is a topical cream formulation of ruxolitinib, a Janus kinase (JAK) inhibitor. It inhibits JAK1 and JAK2 which 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. The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.
Adverse effects associated with the use of Opzelura may include, but are not limited to, the following:
- ear infection
- eosinophil count increased
The Opzelura drug label comes with the following Black Box Warning: Serious infections leading to hospitalization or death, including tuberculosis and bacterial, invasive fungal, viral, and other opportunistic infections, have occurred in patients receiving Janus kinase inhibitors for inflammatory conditions. Higher rate of all-cause mortality, including sudden cardiovascular death have been observed in patients treated with Janus kinase inhibitors for inflammatory conditions. Lymphoma and other malignancies have been observed in patients treated with Janus kinase inhibitors for inflammatory conditions. Higher rate of MACE (including cardiovascular death, myocardial infarction, and stroke) has been observed in patients treated with Janus kinase inhibitors for inflammatory conditions. Thrombosis, including deep venous thrombosis, pulmonary embolism, and arterial thrombosis, some fatal, have occurred in patients treated with Janus kinase inhibitors for inflammatory conditions.
Clinical Trial Results
The FDA approval was based on data from the TRuE-AD (Topical Ruxolitinib Evaluation in Atopic Dermatitis) clinical trial program, consisting of two randomized, double-blind, vehicle-controlled Phase 3 studies (TRuE-AD1 and TRuE-AD 2) evaluating the safety and efficacy of Opzelura in more than 1,200 adolescents and adults with mild to moderate AD. Results from the studies showed patients experienced significantly clearer skin and itch reduction when treated with Opzelura cream 1.5% twice daily (BID), compared to vehicle (non-medicated cream). Significantly more patients treated with Opzelura achieved Investigator’s Global Assessment (IGA) Treatment Success (IGA-TS, primary endpoint) at Week 8 (defined as an IGA score of 0 [clear] or 1 [almost clear] with at least a 2-point improvement from baseline): 53.8% in TRuE-AD1 and 51.3% in TRuE-AD2, compared to vehicle (15.1% in TRuE-AD1, 7.6% in TRuE-AD2. Significantly more patients treated with Opzelura experienced a clinically meaningful reduction in itch from baseline at Week 8, as measured by a ≥4-point reduction in the itch Numerical Rating Scale (itch NRS4): 52.2% in TRuE-AD1 and 50.7% in TRuE-AD2, compared to vehicle (15.4% in TRuE-AD1, 16.3% in TRuE-AD2), among patients with an NRS score of at least 4 at baseline.