Ingenol mebutate

A topical medication used in dermatology

Ingenol mebutate
File:Ingenol mebutate.svg
INN
Drug class
Routes of administration	Topical
Pregnancy category
Bioavailability	N/A
Metabolism	N/A
Elimination half-life	N/A
Excretion	N/A
Legal status	Rx-only
CAS Number	75567-37-2
PubChem	6441245
DrugBank	DB05051
ChemSpider	4948575
KEGG	D09764

Ingenol mebutate is a topical medication used primarily for the treatment of actinic keratosis, a precancerous condition of the skin. It is derived from the sap of the plant Euphorbia peplus, commonly known as petty spurge or milkweed. Ingenol mebutate is marketed under the brand name Picato.

Mechanism of Action

Ingenol mebutate works by inducing cell death in rapidly proliferating cells, such as those found in actinic keratosis. It achieves this through two primary mechanisms:

• Induction of Apoptosis: Ingenol mebutate triggers apoptosis, or programmed cell death, in abnormal keratinocytes. This is achieved by activating protein kinase C (PKC), which leads to the disruption of mitochondrial membranes and the activation of caspases, enzymes that play a crucial role in the apoptotic process.

• Immune Response Activation: The compound also stimulates a local inflammatory response, which recruits immune cells to the site of application. This helps in clearing the damaged cells and promotes healing of the skin.

Clinical Use

Ingenol mebutate is applied topically to the skin. The treatment regimen typically involves applying the gel once daily for two to three consecutive days, depending on the location of the lesions. For lesions on the face and scalp, a two-day treatment is recommended, while lesions on the trunk and extremities require a three-day treatment.

Side Effects

Common side effects of ingenol mebutate include:

• Local skin reactions such as redness, flaking, and crusting
• Swelling and blistering at the site of application
• Itching and irritation

These side effects are generally mild to moderate and resolve within a few weeks after treatment.

Pharmacokinetics

Ingenol mebutate is absorbed minimally into the systemic circulation when applied topically. Its pharmacokinetic profile is characterized by rapid absorption and clearance, with the majority of the compound remaining localized at the site of application.

History and Development

Ingenol mebutate was developed from the sap of Euphorbia peplus, a plant traditionally used in folk medicine for treating skin lesions. The compound was isolated and its therapeutic potential was explored, leading to its approval for medical use.

Related Pages

• Actinic keratosis
• Euphorbia peplus
• Topical medication