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.
Cell Experiment | |
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Cell lines | PBMC |
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). |
Concentrations | 10^-2 mol/L |
Incubation time | 24 h |
Animal Experiment | |
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Animal models | Female Golden hamsters |
Formulation | 0.05 mL of acetone containing 4 μg of testosterone propionate (TP) |
Dosages | 100−200−400 μg/animal |
Administration | s.c. |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
Molecular Weight | 402.52 |
Formula | C24H34O5 |
CAS Number | 19608-29-8 |
Purity | >99% |
Solubility | 10 mM in DMSO |
Storage | at -20°C |
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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