Ingenol mebutate gel applied topically for 2 to 3 days is effective for field treatment of actinic keratoses.Ingenol mebutate is a Cell Death Inducer. The physiologic effect of ingenol mebutate is by means of Increased Cellular Death.
|Source||Mol Cancer Ther (2015). Figure 4. Ingenol Mebutate|
|Cell Lines||SCC cells|
|Incubation Time||24 h|
|Results||In addition, we used either the PKC inhibitor AEB071 or a knockdown of PKCd, either alone or in combination with ingenol mebutate and analyzed the expression of ERK target genes. Either inhibition of PKC or knockdown of PKCd could prevent the upregulation of ERK target gene expression after ingenol mebutate treatment|
|Source||Mol Cancer Ther (2015). Figure 3. Ingenol Mebutate|
|Cell Lines||SCC13 cells|
|Incubation Time||24 h|
|Results||Similar to our findings with the PKC inhibitor, we detected a rescue of cell viability upon ingenol mebutate treatment when PKCd was knocked down. A knockdown PKCa followed by ingenol mebutate treatment led only to a partial rescue, while PKCd knockdown could rescue the ingenol mebutate–treated cells completely|
|Cell lines||T7 cell|
|Preparation method||Tumours were treated topically (on days 4 and 5 post tumour inoculation) with 30 μl of 0.25 % (w/v) ingenol mebutate or placebo gel (supplied by LEO Pharma A/S) using a positive displacement pipette, with the gel then spread over the tumour site.|
|Concentrations||30 μl of 0.25 % (w/v)|
|Incubation time||48 h|
|Animal models||BALB/c nu−/nu− mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||41 mg/ml in CHCl3|
Effective treatment of squamous cell carcinomas with ingenol mebutate gel in immunologically intact SKH1 mice.
Cozzi SJ, et al. Arch Dermatol Res. 2013 Jan;305(1):79-83. PMID: 22871992.
Ingenol mebutate gel for actinic keratosis.
Lebwohl M,et.al. N Engl J Med. 2012 Mar 15;1010-9. PMID: 22417254.
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