1. Pharmacokinetics of ingenol mebutate gel under maximum use conditions in large treatment areas
- Author
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Laerke Kyhl, Anders Hall, Dowling B Stough, Alicia D. Bucko, Michael Jarratt, and John Villumsen
- Subjects
Male ,Ingenol Mebutate Gel ,Pathology ,medicine.medical_specialty ,Ingenol mebutate ,Dermatology ,Administration, Cutaneous ,030207 dermatology & venereal diseases ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Pharmacokinetics ,medicine ,Humans ,Basal cell ,Aged ,Skin ,Aged, 80 and over ,Scalp ,integumentary system ,business.industry ,Pruritus ,Actinic keratosis ,Actinic keratoses ,Middle Aged ,medicine.disease ,Keratosis, Actinic ,Treatment Outcome ,ROC Curve ,chemistry ,Area Under Curve ,Face ,030220 oncology & carcinogenesis ,Arm ,Female ,Diterpenes ,business ,Gels ,Half-Life - Abstract
Actinic keratoses (AKs) exist on a continuum with squamous cell carcinoma and can occur as sub-clinical and clinically visible lesions in cancerized fields on sun-damaged skin. Ingenol mebutate effectively treats AKs on areas up to 25 cmPhase I, multicenter, open-label, uncontrolled, non-randomized trial. Patients received ingenol mebutate gel for three consecutive days on approximately 250 cmOf 61 patients, 10 (face =8; arm =2) had ingenol mebutate in whole blood at subnanomolar levels (0.235-0.462 nM). The assayed metabolites were below the lower limit of quantification. Local skin responses increased during Days 1-4 and declined thereafter, approaching baseline by Day 16. Most adverse events were pain/pruritus of mild or moderate intensity.Subnanomolar systemic exposure to ingenol mebutate was measured after application of the gel to approximately 250 cm
- Published
- 2017
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