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Ingenol Mebutate

Medically reviewed by Drugs.com. Last updated on Sep 8, 2020.

Pronunciation

(IN je nol MEB u tate)

Index Terms

  • Euphorbia peplus Derivative
  • Ingenol-3-angelate gel
  • PEP005

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Gel, External:

Picato: 0.015% (3 ea); 0.05% (2 ea) [contains benzyl alcohol, isopropyl alcohol]

Brand Names: U.S.

  • Picato

Pharmacologic Category

  • Topical Skin Product

Pharmacology

Ingenol mebutate appears to induce primary necrosis of actinic keratosis with a subsequent neutrophil-mediated inflammatory response with antibody-dependent cytotoxicity of residual disease cells; killing residual disease cells may prevent future relapse (Ramsay 2011; Siller 2010).

Absorption

Absorption through the skin is minimal (with proper use); expected systemic exposure is <0.1 ng/mL.

Use: Labeled Indications

Actinic keratosis: Topical treatment of actinic keratosis

Contraindications

Known hypersensitivity to ingenol mebutate or any component of the formulation.

Dosing: Adult

Actinic keratosis: Topical:

Face or scalp: Apply 0.015% gel once daily to affected area for 3 consecutive days (Lebwohl 2012); patients not achieving clearance or that experience recurrence after achieving clearance ≥8 weeks after initial treatment may benefit from a second treatment course.

Trunk or extremities: Apply 0.05% gel once daily to affected area for 2 consecutive days (Lebwohl 2012).

Dosing: Geriatric

Refer to adult dosing.

Administration

Apply topically to one contiguous affected area of skin using one unit-dose tube; one unit-dose tube will cover ~5 cm x 5 cm (~25 cm2 or ~2 inch x 2 inch). Spread evenly then allow gel to dry for 15 minutes. Do not cover with bandages or occlusive dressings. Wash hands immediately after applying and avoid transferring gel to any other areas. Avoid washing or touching the treatment area or doing activities that cause sweating for ≥6 hours, and following this period of time, patients may wash the area with a mild soap. Not for oral, ophthalmic, or intravaginal use. Avoid application near or around the mouth and lips. Avoid transfer of gel to the periocular area. If accidental exposure occurs, flush area with water and contact health care provider.

Storage

Store at 2°C to 8°C (36°F to 46°F); excursions are permitted to 0°C to 15°C (32°F to 59°F); do not freeze. Discard tubes after single use.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Percentages represent face/scalp and trunk/extremities incidences unless otherwise specified.

>10%:

Dermatologic: Erythema of skin (92% to 94%), desquamation (≤90%), exfoliation of skin (≤90%), crusted skin (74% to 80%), swelling of skin (face/scalp: 79%; trunk/extremities: 64%), localized vesiculation (face/scalp: ≤56%; trunk/extremities: ≤44%), pustules (face/scalp: ≤56%; trunk/extremities: ≤44%), dermal ulcer (≤32%), skin erosion (≤32%), application site pain (face/scalp: 15%, trunk/extremities: 2%)

1% to 10%:

Dermatologic: Application site pruritus (8%), application site irritation (trunk/extremities: 4%), skin infection (face/scalp: 3%; at application site)

Nervous system: Headache (face/scalp: 2%)

Ophthalmic: Periorbital edema (face/scalp: 3%)

Respiratory: Nasopharyngitis (trunk/extremities: 2%)

Frequency not defined:

Ophthalmic: Eyelid edema, eye pain

<1%, postmarketing, and/or case reports: Allergic contact dermatitis, anaphylaxis, cicatrix of skin (application site), conjunctivitis (chemical-induced), corneal injury (burn), herpes zoster infection, hypersensitivity reaction, injury to eye region, pigmentation alteration (application site), severe dermatological reaction, skin carcinoma (UK Drug Safety Feb 12, 2020), Stevens-Johnson syndrome

Warnings/Precautions

Concerns related to adverse effects:

• Dermatologic reactions: Severe reactions including erythema, crusting, swelling, vesiculation/pustulation, and erosion/ulceration may occur in the treated area. Do not apply ingenol mebutate gel until skin is healed from any prior drug or surgical treatment.

• Hypersensitivity: Hypersensitivity reactions, including anaphylaxis, as well as allergic reactions leading to hospitalization, and allergic contact dermatitis, have been reported. If anaphylaxis or other clinically significant hypersensitivity reaction occurs, discontinue immediately and manage as medically appropriate.

• Ocular toxicity: Avoid treatment in the periocular area. Severe eye pain, chemical conjunctivitis, corneal burning, eyelid edema, eyelid ptosis, and periorbital edema can occur after exposure. Patients should wash their hands well immediately after applying and avoid transferring to the eye area. If accidental exposure occurs, patient should flush area with water and contact health care provider.

Monitoring Parameters

Monitor for signs/symptoms of hypersensitivity reactions and for dermatologic toxicity.

Pregnancy Considerations

Systemic absorption is limited following topical administration; maternal use is not expected to result in fetal exposure.

Patient Education

What is this drug used for?

• It is used to treat a precancerous skin problem called actinic keratosis.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Skin discoloration

• Skin crusting, scaling, flaking, redness, or swelling

• Headache

• Stuffy nose

• Sore throat

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Skin infection

• Skin ulcers

• Severe skin reaction or irritation

• Dizziness

• Passing out

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.