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Christopher G Parker, Christian A Kuttruff, Andrea Galmozzi, Lars Jørgensen, Chien-Hung Yeh, Daniel J Hermanson, Yujia Wang, Marta Artola, Steven J McKerrall, Christopher M Josyln, Bjarne Nørremark, Georg Dünstl, Jakob Felding, Enrique Saez, Phil S Baran, Benjamin F Cravatt
The diterpenoid ester ingenol mebutate (IngMeb) is the active ingredient in the topical drug Picato, a first-in-class treatment for the precancerous skin condition actinic keratosis. IngMeb is proposed to exert its therapeutic effects through a dual mode of action involving (i) induction of cell death that is associated with mitochondrial dysfunction followed by (ii) stimulation of a local inflammatory response, at least partially driven by protein kinase C (PKC) activation. Although this therapeutic model has been well characterized, the complete set of molecular targets responsible for mediating IngMeb activity remains ill-defined...
December 27, 2017: ACS Central Science
Marc Z Handler, Bradley S Bloom, David J Goldberg
BACKGROUND: No studies have examined the use of topical ingenol mebutate for improvement of photoaged skin. OBJECTIVE: To evaluate clinical results of ingenol mebutate gel applied to photoaged skin and to quantify improvement at 7, 30, and 60 days after application. MATERIALS AND METHODS: Twenty-five subjects were enrolled in the study. Picato (ingenol mebutate) (LEO Pharma, Parsippany, NJ) gel was applied to an area with a known actinic keratosis daily for 3 days...
August 30, 2017: Dermatologic Surgery: Official Publication for American Society for Dermatologic Surgery [et Al.]
Malene Bertelsen, Martin Stahlhut, Gunnar Grue-Sørensen, Xifu Liang, Gitte Bach Christensen, Kresten Skak, Karen Margrethe Engell, Thomas Högberg
INTRODUCTION: Ingenol mebutate gel (Picato(®), LEO Pharma A/S) is approved for the field treatment of actinic keratosis and is characterized by high sustained clearance of actinic lesions. The inherent propensity of ingenol mebutate towards chemical rearrangement necessitates refrigeration of the final product. We sought to identify novel ingenol derivatives with enhanced chemical stability and similar or improved in vitro potency and in vivo efficacy. METHODS: A number of ingenol esters were synthesized with full regiocontrol from ingenol...
December 2016: Dermatology and Therapy
Giovanni Appendino
Despite a more recent isolation and chemical characterization when compared to phorbol, along with its chemical instability, limited distribution in Nature, and scarce availability, ingenol is the only Euphorbia diterpenoid that has undergone successful pharmaceutical development, with ingenol 3-angelate (ingenol mebutate, Picato(®)) entering the pharmaceutical market in 2012 for the treatment of actinic keratosis. The phytochemical, chemical, and biological literature on members of the ingenane class of diterpenoids is reviewed from their first isolation in 1968 through 2015, highlighting unresolved issues both common to phorboids (biogenesis, relationship between molecular targets, and in vivo activity) and specific to ingenol derivatives (two-dimensional representation, in-out stereoisomerism, versatility of binding mode to PKC, and inconsistencies in the structural elucidation of some classes of derivatives)...
2016: Progress in the Chemistry of Organic Natural Products
Carey Kim, Pantea Hashemi, Michael Caglia, Kenneth Shulman
BACKGROUND: Epidermodysplasia verruciformis (EV) is a rare genetic disorder characterized by widespread human papillomavirus (HPV) associated lesions and an increase susceptibility to cutaneous malignancies. A host of medications traditionally used to treat warty lesions have been used with variable results and limited success. To our knowledge, we describe the first reported case of a patient with Imiquimod resistant EV successfully treated with topical ingenol mebutate (Picato). CASE: A patient with a 5 year history of EV failed to respond to a 6 week course of 5% imiquimod on the forehead and was subsequently treated with a 3 day course of 0...
March 2016: Journal of Drugs in Dermatology: JDD
Guochun Jiang, Erica A Mendes, Philipp Kaiser, Daniel P Wong, Yuyang Tang, Ivy Cai, Anne Fenton, Gregory P Melcher, James E K Hildreth, George R Thompson, Joseph K Wong, Satya Dandekar
Although anti-retroviral therapy (ART) is highly effective in suppressing HIV replication, it fails to eradicate the virus from HIV-infected individuals. Stable latent HIV reservoirs are rapidly established early after HIV infection. Therefore, effective strategies for eradication of the HIV reservoirs are urgently needed. We report that ingenol-3-angelate (PEP005), the only active component in a previously FDA approved drug (PICATO) for the topical treatment of precancerous actinic keratosis, can effectively reactivate latent HIV in vitro and ex vivo with relatively low cellular toxicity...
July 2015: PLoS Pathogens
Guangjian Mei, Xin Liu, Chuang Qiao, Wei Chen, Chuang-chuang Li
A type II intramolecular oxidopyrylium-mediated [5+2] cycloaddition reaction allows the efficient and diastereoselective formation of various highly functionalized and synthetically challenging bridged seven-membered ring systems (such as bicyclo[4.4.1]undecane, bicyclo[4.3.1]decane, bicyclo[5.4.1]dodecane, and bicyclo[6.4.1]]tridecane). This simple, thermal, direct transformation has a broad substrate scope and is high yielding, with high functional-group tolerance and unique endo selectivity. The highly strained tricyclic cores of ingenol mebutate (picato) and cyclocitrinol are synthesized efficiently and diastereoselectively using this methodology...
February 2, 2015: Angewandte Chemie
Kyriaki Tzogani, Nithyanandan Nagercoil, Robert James Hemmings, Bekkai Samir, Jean Gardette, Pierre Demolis, Tomas Salmonson, Francesco Pignatti
BACKGROUND: The European Commission has recently issued a marketing authorisation valid throughout the European Union for ingenol mebutate (Picato) in the cutaneous treatment of non-hyperkeratotic, non-hypertrophic actinic keratosis in adults. OBJECTIVES: The objective of this paper is to summarise the scientific review of the application leading to regulatory approval in the EU. The full scientific assessment report and product information, including the summary of product characteristics, are available on the EMA website (www...
July 2014: European Journal of Dermatology: EJD
Brooke Fidler, Tamara Goldberg
Ingenol mebutate gel (Picato) for actinic keratoses.
January 2014: P & T: a Peer-reviewed Journal for Formulary Management
William Abramovits, Marcial Oquendo, Kimberly D Vincent, Aditya K Gupta
No abstract text is available yet for this article.
March 2013: Skinmed
(no author information available yet)
No abstract text is available yet for this article.
April 30, 2012: Medical Letter on Drugs and Therapeutics
L Penide, J Alvarez, F González, J Medina, P Picato
Anesthesia for imaging by nuclear magnetic resonance presents special problems due to the effect of the large magnetic field and high frequency radio waves on monitoring and respiratory systems. These systems in turn affect image quality. Special materials should be designed specifically for this context or existing materials should be modified.
September 1994: Revista Española de Anestesiología y Reanimación
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