17 alpha-propionate

Biological Activity

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.

Customer Product Validations & Biological Datas

	Source	J Microbiol Biotechnol (2016). Figure 4. 17 alpha-propionate
	Method	Western Blot
	Cell Lines	bacteria
	Concentrations	140 mg/l
	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.

Protocol

Cell Experiment
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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

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.