Roflumilast Topical

Roflumilast cream is used for the treatment of plaque psoriasis and atopic dermatitis, while roflumilast foam is used for the treatment of plaque psoriasis and seborrheic dermatitis, to improve itching and inflammation and control skin symptoms. Roflumilast is a once-daily, steroid-free cream or foam that can be used long-term anywhere on the body, including sensitive areas such as the face or skin folds, and hairy areas. Roflumilast is well tolerated, with very little stinging or burning.

Roflumilast brand name is Zoryve. Roflumilast is also available as a tablet for COPD (chronic obstructive pulmonary disease) under the brand name Daliresp.

Roflumilast mechanism of action (MOA) is by inhibiting the enzyme PDE4, an enzyme that plays an important role in controlling inflammation and immune responses in the body. By inhibiting PDE-4 (Phosphodiesterase-4), roflumilast helps to reduce redness, itch, scaling, and improve other skin symptoms.

Roflumilast is a phosphodiesterase 4 (PDE4) inhibitor.

Roflumilast FDA-approved indications are:

Plaque psoriasis

• 0.3% cream in patients 2 years and older.
• 0.3% foam in patients 12 years and older.

Atopic dermatitis (mild to moderate)

• 0.05% cream in patients 2 to 5 years.
• 0.15% cream in patients 6 years and older.

Seborrheic dermatitis

• 0.3% foam in patients 9 years and older.

Roflumilast cream (0.3%) for plaque psoriasis in patients 2 years of age and older. Roflumilast cream (0.3%) can be used for plaque psoriasis on the scalp and body, including sensitive areas such as the face, skin folds, and genitalia. The base is a non-greasy, moisturizing cream that absorbs quickly and spreads easily. It does not include sensitizing ingredients or irritants such as propylene glycol, polyethylene glycol, isopropyl alcohol, ethanol, or fragrances. This cream should not be applied to the eyes, mouth, or vagina.

Roflumilast cream (0.15%) for atopic dermatitis in patients 6 years of age and older with mild to moderate atopic dermatitis. Roflumilast cream helps clear atopic dermatitis, reduces itch, and can be used long-term to control dermatitis. This cream should not be applied to the eyes, mouth, or vagina.

Roflumilast cream (0.05%) for atopic dermatitis in pediatric patients 2 to 5 years of age.

Roflumilast foam for plaque psoriasis in patients 12 years and older for plaque psoriasis on scalp and body, including sensitive areas like the face, skin folds, and genitalia. Roflumilast foam is a once-daily, steroid-free topical treatment that can be used anywhere on the body, including hairy areas.

Roflumilast foam for seborrheic dermatitis in patients 9 years of age and older. Roflumilast foam is used to help rapidly clear seborrheic dermatitis and also reduce the symptoms of itch. This foam should not be applied to the eyes, mouth, or vagina.

Roflumilast Cream

• Apply a thin layer to affected areas once daily.
• Rub in completely until it disappears.
• Wash hands after application (unless treating hands).

Roflumilast Foam

• Apply a thin layer to affected areas once daily.
• Shake well before use.
• Turn the can upside down and dispense it into your hand.
• Apply to dry skin and rub in completely.
• Wash hands after application.

Do not use roflumilast cream or foam if you have certain liver problems, including moderate to severe liver impairment.

Roflumilast foam is flammable. Avoid fire, flame, and smoking when applying and right after you apply it.

Before you start treatment, tell your healthcare provider about all of your medical conditions, including if you:

• have liver problems.

Pregnancy

Tell your healthcare provider if you are pregnant or plan to become pregnant, as it is not known if roflumilast will harm your unborn baby.

Breastfeeding

Tell your healthcare provider if you are breastfeeding or planning to breastfeed. Talk to your healthcare provider about the best way to feed your baby during treatment with this cream.

Breastfeeding women using the cream or foam should use it on the smallest area of the skin and for the shortest time needed. Do not apply this cream or foam directly to the nipple or areola if you are breastfeeding to avoid contact with the product with your baby. Avoid direct skin contact of treated areas with your baby if roflumilast cream is applied to your chest.

Common roflumilast cream side effects

The most common roflumilast cream 0.3% side effects include

• Diarrhea (3.1%)
• Headache (2.4%)
• Insomnia (1.4%)
• Nausea (1.2%)
• Application site pain(1.0%)
• Upper respiratory infections (1.0%)
• Urinary tract infections (1.0%)

The most common roflumilast cream 0.15% side effects for atopic dermatitis are

• Headache (2.9%)
• Nausea (1.9%)
• Application site pain(1.5%)
• Diarrhea (1.5%)
• Vomiting (1.5%)

Common roflumilast foam side effects

The most common roflumilast foam side effects include:

• Nausea (1.3%)
• Headache (1.1%)
• Cold symptoms (1.5%)

These are not all of the possible side effects. 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 Arcutis Biotherapeutics, Inc. by calling 1-844-692-6729..

Plaque Psoriasis (Roflumilast cream 0.3%) - DERMIS-1 Study (NCT04211363) and DERMIS-2 (NCT04211389)

• 41.5% of roflumilast patients had clear or almost clear skin in 8 weeks (vs. 5.8% on placebo). Measured using Investigator’s Global Assessment (IGA) score
• 67.5% of patients reported a 4-point reduction in itch by week 8 (measured using the Worst Itch-Numeric Rating Scale (WI-NRS) score)

Plaque Psoriasis (Roflumilast foam 0.3%) ARRECTOR trial (NCT05028582)

• Scalp psoriasis: 66.4% of roflumilast foam patients had clear or almost clear skin in 8 weeks (vs.27.8% on placebo). Measured using Scalp-IGA
• Body psoriasis: 45.5% of roflumilast foam patients had clear or almost clear skin in 8 weeks (vs 20.1% on placebo) measured using the Body-IGA score
• 63.1% of patients reported a 4-point reduction in scalp itch by week 8 (vs 30.1%) measured using the Scalp Itch-Numeric Rating Scale (SI-NRS)

Atopic Dermatitis (Roflumilast cream 0.15%) - INTEGUMENT-1 (NCT04773587)

• 33.6% of roflumilast patients had a successful improvement of itch within 4 weeks (measured using the WI-NRS score)
• Itch relief started within 24 hours of application.

Atopic Dermatitis (Zoryve cream 0.05%)- INTEGUMENT-PED (NCT04845620)

• 25.4% of Zoryve patients had a clear or almost clear skin plus a 2-grade improvement from baseline at week 4 (vs 10.7% on placebo). Measured using vIGA-AD (validated Investigator Global Assessment for Atopic Dermatitis)

Seborrheic Dermatitis (Roflumilast foam 0.15%)– STRATUM [NCT04973228]

• 79.5% of roflumilast patients had clear or almost clear skin in 8 weeks vs. 58% placebo ( measured using IGA score)
• 50.7% achieved complete clearance by week 8.

Roflumilast Cream Dose for Atopic Dermatitis or Plaque Psoriasis: Apply once daily to affected areas

Roflumilast Foam Dose for Seborrheic Dermatitis or Plaque Psoriasis: Apply once daily to affected areas.General dosing information: For topical use only. Not for ophthalmic, oral, or intravaginal use.

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

Using roflumilast cream or foam with medicines that are systemic CYP3A4 inhibitors or dual inhibitors that inhibit both CYP3A4 and CYP1A2 simultaneously may increase the active ingredient roflumilast systemic exposure and may increase side effects. It is important to weigh up the potential for increased adverse reactions against benefit if these products are used together with Roflumilast cream or foam.

Using roflumilast cream with oral contraceptives containing gestodene and ethinyl estradiol may increase roflumilast systemic exposure and may result in increased side effects. The risk of such concurrent use should be weighed carefully against the benefit.

This list is not complete. Not all possible drug interactions are listed here.

Review the Zoryve Cream Package Insert or Zoryve Foam Package Insert for more detailed information about this medicine. Discuss any medical questions you have with your doctor or other health care provider. This is not all the information you need to know about this medicine for safe and effective use, and it does not take the place of talking to your doctor about your treatment.

Cream storage

• Store at room temperature from 68°F to 77°F (20°C to 25°C).

Foam storage

• Store at room temperature between 68°F to 77°F (20°C to 25°C).
• This foam is flammable. Keep away from heat and flame.
• The contents foam are under pressure. Do not puncture or burn the can. Do not expose to heat or store at temperatures above 120°F (49°C).
• Do not freeze. Store the can upright.

Active ingredient: roflumilast

Zoryve Cream inactive ingredients: ceteareth-10 phosphate, cetearyl phosphate, cetostearyl alcohol, diethylene glycol monoethyl ether, hexylene glycol, isopropyl palmitate, methylparaben, propylparaben, purified water, sodium hydroxide, and white petrolatum. Hydrochloric acid may have been added to adjust pH.

Zoryve Foam inactive ingredients: ceteareth-10 phosphate, cetearyl phosphate, cetostearyl alcohol, diethylene glycol monoethyl ether, hexylene glycol, isopropyl palmitate, methylparaben, propylparaben, purified water, sodium hydroxide, and white petrolatum. Hydrochloric acid may have been added to adjust pH. Propellants: butane, isobutane, and propane.

Zoryve Arcutis Biotherapeutics, Inc. Westlake Village, CA 91361.