17 alpha-propionate is a new potent topical antiandrogen potentially useful in acne vulgaris. CB-03-01 1% cream was very well tolerated, and was significantly better than placebo regarding TLC (P = 0·0017), ILC (P = 0·0134) and ASI (P = 0·0090), and also clinically more effective than comparator. The product also induced a faster attainment of 50% improvement in all the above parameters.
|Preparation method||Because of the extent of these experiments, the drugs were divided into two groups: dexamethasone, budesonide, beclomethasone dipropionate and fluticasone (first group); and dexamethasone, CsA, FK506 (tacrolimus) and mycophenolate (second group).|
|Incubation time||24 h|
|Animal models||Female Golden hamsters|
|Formulation||0.05 mL of acetone containing 4 μg of testosterone propionate (TP)|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
|Source||J Microbiol Biotechnol (2016). Figure 4. 17 alpha-propionate|
|Incubation Time||6 h|
|Results||As shown in Fig. 4, propionate-oxidizing bacteria relevant band B3 was enhanced with the pH decrease rom 7.1 to 6.0, indicating that this propionate degrader (band B3) is slightly acid tolerant.|
Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist.
Celasco G,et.al. Arzneimittelforschung. 2004;881-6. PMID: 15646372.
Biotransformation of the topical glucocorticoids budesonide and beclomethasone 17 alpha,21-dipropionate in human liver and lung homogenate.
Andersson P, et al. J Pharm Pharmacol. 1984 Nov;36(11):763-5. PMID: 6150981.
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