ruxolitinib topical (Rx)

Brand and Other Names:Opzelura
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

topical cream

  • 1.5% (15mg/g)

Atopic Dermatitis

Indicated for topical short-term and noncontinuous long-term treatment of mild-to-moderate atopic dermatitis in nonimmunocompromised adults whose disease is not adequately controlled with topical prescription therapies or when those therapies are not advisable

Apply thin layer of cream to affected areas BID of up to 20% body surface area; not to exceed >60 g/week

Stop using when signs and symptoms (eg, itch, rash, redness) of atopic dermatitis resolve

If signs and symptoms do not improve within 8 weeks, re-examine patient

Dosing Considerations

Limitation of use

  • Not recommended for use in combination with therapeutic biologics, other Janus kinase (JAK) inhibitors, or potent immunosuppressants (eg, azathioprine, cyclosporine)

Dosage Forms & Strengths

topical cream

  • 1.5% (15mg/g)

Atopic Dermatitis

Indicated for topical short-term and noncontinuous long-term treatment of mild-to-moderate atopic dermatitis in nonimmunocompromised patients aged ≥12 years whose disease is not adequately controlled with topical prescription therapies or when those therapies are not advisable

<12 years: Safety and efficacy not established

≥12 years

  • Apply thin layer of cream to affected areas BID of up to 20% body surface area; not to exceed >60 g/week
  • Stop using when signs and symptoms (eg, itch, rash, redness) of atopic dermatitis resolve
  • If signs and symptoms do not improve within 8 weeks, re-examine patient

Dosing Considerations

Limitation of use

  • Not recommended for use in combination with therapeutic biologics, other Janus kinase (JAK) inhibitors, or potent immunosuppressants (eg, azathioprine, cyclosporine)
Next:

Interactions

Interaction Checker

and ruxolitinib topical

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (0)

                  Minor (0)

                    Previous
                    Next:

                    Adverse Effects

                    1-10%

                    Nasopharyngitis (3%)

                    Bronchitis (1%)

                    Ear infection (1%)

                    Eosinophil count increased (1%)

                    Urticaria (1%)

                    Diarrhea (1%)

                    Folliculitis (1%)

                    Tonsillitis (1%)

                    Rhinorrhea (1%)

                    <1%

                    Neutropenia

                    Allergic conjunctivitis

                    Pyrexia

                    Seasonal allergy

                    Herpes zoster

                    Otitis externa

                    Staphylococcal infection

                    Acneiform dermatitis

                    BLACK BOX WARNI

                    Previous
                    Next:

                    Warnings

                    Black Box Warnings

                    Serious infections

                    • Patients treated with oral JAK inhibitors for inflammatory conditions are at risk for developing serious infections that may lead to hospitalization or death
                    • Reported infections include:
                      • Active tuberculosis (TB), which may present with pulmonary or extrapulmonary disease
                      • Invasive fungal infections (eg, candidiasis, pneumocystosis)
                      • Bacterial, viral, and other infections due to opportunistic pathogens
                    • Avoid use in patients with an active, serious infection, including localized infections
                    • If a serious infection develops, interrupt therapy until infection is controlled
                    • Do not resume until the infection is controlled.
                    • Carefully consider the risks and benefits of treatment before initiating therapy in patients with chronic or recurrent infection
                    • Closely monitor for developing signs and symptoms of infection during and after treatment

                    Mortality

                    • Higher rate of all-cause mortality, including sudden cardiovascular death have been observed with oral JAK inhibitors used for inflammatory conditions
                    • Consider benefits and risks for the patient before initiating or continuing therapy

                    Malignancies

                    • Lymphoma and other malignancies observed with JAK inhibitors used for inflammatory conditions

                    Major adverse cardiovascular events (MACE)

                    • Higher rate of MACEs (eg, cardiovascular death, myocardial infarction, stroke) has been observed with JAK inhibitors used for inflammatory conditions

                    Thrombosis

                    • Increased incidence of thrombosis, including deep venous thrombosis (DVT), pulmonary embolism (PE), and arterial thrombosis, observed with oral JAK inhibitors for inflammatory conditions
                    • Many of these adverse reactions were serious and some resulted in death
                    • Promptly evaluate patients with symptoms of thrombosis

                    Contraindications

                    None

                    Cautions

                    Higher rate of all-cause mortality observed with oral JAK inhibitors used for inflammatory conditions

                    Malignancies, including lymphomas, observed in clinical trials of oral JAK inhibitors used to treat inflammatory conditions; patients who are current or past smokers are at additional increased risk

                    Major adverse cardiovascular events (MACE) such as cardiovascular death, nonfatal MI, and nonfatal stroke observed with JAK inhibitors used to treat inflammatory conditions; consider benefits and risks, particularly in patients who are current or past smokers and patients with other cardiovascular risk factors

                    Thromboses, including DVT, PE, and arterial thrombosis, were observed with oral JAK inhibitors for inflammatory conditions compared with patients treated with placebo; there was no clear relationship between platelet count elevations and thrombotic events; use with caution in patients who may be at increased risk of thrombosis

                    Oral ruxolitinib has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein cholesterol, and triglycerides

                    Serious infections

                    • Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens reported with oral JAK inhibitors
                    • Serious lower respiratory tract infections reported in the clinical development program with topical ruxolitinib
                    • Avoid use in patients with an active, serious infection, including localized infections
                    • Consider risks and benefits of treatment before initiating in patients with or who have the following:
                      • Chronic or recurrent infection
                      • A history of a serious or an opportunistic infection
                      • Previous exposure to tuberculosis
                      • Resided or traveled in areas of endemic tuberculosis or endemic mycoses
                      • Underlying conditions that may predispose them to infection
                    • Tuberculosis (TB)
                      • No cases of active TB were reported with topical ruxolitinib; however, active TB cases were reported with oral JAK inhibitors used to treat inflammatory conditions
                      • Consider evaluating for latent and active TB infection before administration
                      • During use, monitor for developing signs and symptoms of TB
                    • Viral reactivation
                      • Viral reactivation, including cases of herpes virus reactivation (eg, herpes zoster), were reported with JAK inhibitors used to treat inflammatory conditions
                      • If herpes zoster develops, consider interrupting treatment until episode resolves
                    • Hepatitis B and C
                      • Impact of JAK inhibitors used to treat inflammatory conditions on chronic viral hepatitis reactivation is unknown
                      • Patients with history of hepatitis B or C infection were excluded from clinical trials
                      • Hepatitis B viral load (HBV-DNA titer) increases, with or without associated elevations in ALT and AST, were reported in patients with chronic hepatitis B taking oral ruxolitinib
                      • Do not initiate in patients with active hepatitis B or C

                    Thrombocytopenia, anemia, and neutropenia

                    • Thrombocytopenia, anemia, and neutropenia reported
                    • Consider benefits and risks for patients with history of these events before initiating therapy
                    • Monitor complete blood cell count as clinically indicated
                    • Discontinue therapy if signs and/or symptoms of clinically significant thrombocytopenia, anemia, and/or neutropenia occur

                    Drug interaction overview

                    • Drug interaction studies were not conducted
                    • Ruxolitinib is a substrate of CYP3A4
                    • Strong CYP3A4 inhibitors
                      • Avoid coadministration
                      • Strong CYP3A4 inhibitors may increase ruxolitinib systemic exposure and adverse reactions
                    Previous
                    Next:

                    Pharmacology

                    Mechanism of Action

                    Janus kinase (JAK) pathways inhibitor; JAK consists of a group of intracellular tyrosine kinases that transmit signals from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function, including inflammation associated with atopic dermatitis

                    JAKs phosphorylate and recruit signal transducers and activators of transcription (STATs) which modulate intracellular activity including gene expression

                    JAK inhibitors modulate the JAK signaling pathway, which in turn prevents the phosphorylation and activation of STATs

                    Absorption

                    Peak plasma concentration: 449 nM (adults); 110 nM (adolescents)

                    AUC: 3,215 h·nM (adults); 801 h·nM (adolescents)

                    Distribution

                    Protein bound: ~97%

                    Metabolism

                    Primarily metabolized by CYP3A4 and CYP2C9 (lesser extent) in vitro

                    Elimination

                    Half-life: 116 hr

                    Excretion: Urine (74%) and feces (22%); <1% excreted as unchanged drug

                    Previous
                    Next:

                    Administration

                    Topical Administration

                    For topical use only

                    Not for ophthalmic, oral, or intravaginal use

                    Storage

                    Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

                    Previous
                    Next:

                    Images

                    No images available for this drug.
                    Previous
                    Next:

                    Patient Handout

                    A Patient Handout is not currently available for this monograph.
                    Previous
                    Next:

                    Formulary

                    FormularyPatient Discounts

                    Adding plans allows you to compare formulary status to other drugs in the same class.

                    To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                    Adding plans allows you to:

                    • View the formulary and any restrictions for each plan.
                    • Manage and view all your plans together – even plans in different states.
                    • Compare formulary status to other drugs in the same class.
                    • Access your plan list on any device – mobile or desktop.

                    The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                    Tier Description
                    1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                    2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                    3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                    4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    NC NOT COVERED – Drugs that are not covered by the plan.
                    Code Definition
                    PA Prior Authorization
                    Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                    QL Quantity Limits
                    Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                    ST Step Therapy
                    Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                    OR Other Restrictions
                    Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                    Additional Offers
                    Email to Patient

                    From:

                    To:

                    The recipient will receive more details and instructions to access this offer.

                    By clicking send, you acknowledge that you have permission to email the recipient with this information.

                    Email Forms to Patient

                    From:

                    To:

                    The recipient will receive more details and instructions to access this offer.

                    By clicking send, you acknowledge that you have permission to email the recipient with this information.

                    Previous
                    Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.