Ingenol mebutate

개요Ingenol mebutate (also known as PEP005) was approved in January 2012 by the US FDA for the topical treatment of actinic keratoses (AK). Ingenol mebutate also received approval in 2012 in the European Union, Australia, and Brazil for the same indication. Ingenol mebutate, a diterpene ester natural product, is the active agent in the sap of the plant Euphorbia peplus, which has long been used as a traditional remedy for skin lesions. Ingenol mebutate has a novel mechanism of action involving initial plasma membrane disruption, rapid loss of mitochondrial membrane potential, and cell death by primary necrosis within 1 h; a subsequent tumor-specific immune response results in antibodydependent cellular toxicity that eliminates residual cells. Ingenol mebutate is obtained by extraction from the dried, milled aerial parts of Euphorbia peplus followed by a series of purification steps.

용도Ingenol 3-Angelate is known to exhibit antitumor activities which induces plasma membrane and mitochondrial disruption and necrotic cell death.