Authors:K. Imamura, A. Bonfils, A. Diani, and H. Uno. Wisconsin Primate Research
Center, Univ. Wisconsin, Madison, WI, USA, Hoechst Marion Roussel,
Romainvill, France, and Pharmacia-Upjohn, Kalamazoo, MI, USA.
"Our previous studies demonstrated that the treatment with either RU58841 (RU) or minoxidil (M) alone induced significant hair regrowth in the bald stumptail macaques. However, the rate of hair growth has not significantly progressed after 6 months.
This implies that M stimulates follicular cell proliferation but is unable to halt androgenetic follicular regression. On the contrary, RU prevents androgenetic follicular regression but appears to have no direct stimulating effect on follicular cell growth.
"The present study was aimed to evaluate the effect of combined RU 5% (RU-5) with M 2% (M-2) or M 5% (M-5) solution on hair regrowth by both photographic recording and micromorphometrical analysis of follicular growth (folliculogram). The vehicle, mixture of propylene glycol, alcohol, and water, was used for both compounds and was applied to the placebo group.
Each group has 3 monkeys. The data of hair growth for RU-5, M-2, and M-5 groups were used the results from our previous studies. The results revealed that the initial hair regrowth was noticed as early as 1 month after treatment in RU-5 + M-5 and 2 months in RU-5 + M-2 group.
The similar degree of hair growth noticed at 3 months after treatment with RU-5 and M-5 alone.
In M-2 group, the hairiness maintained but showed no noticeableregrowth. At 3 months, regrowth of long terminal hairs appeared in both RU-5 + M-2 and RU-5 + M-5 groups and these hairs maintained for 6 to 12 months.
The overall rate of anagen conversion conversion and follicular enlargement were higher in combined groups compared to RU-5 and M-5 alone and revealed no significant difference between RU-5 + M-2 and RU-5 + M-5.
The follicular growth was not found in M-2 group. Progressive effect of hair growth by combined treatment of antiandrogen with hypertrichotic agent showed most remarkably in early stage, but within one year the overall effects of hair regrowth revealed no significant difference compared to the rate in RU-5 or M-5 alone.
Long-term observation will be necessary to find the synergetic effects on the follicular growth."
http://www.calvizie.net/documento.asp?args=6.1.154
RU58841 + minoxidil
Модератор: Безволосый Тони
RU58841 + minoxidil
Drug Type Antiandrogen
Availability Not Yet Available
Notes
This is a french drug which is not yet FDA approved which has been shown to be a highly effective local topical antiandrogen. The company that makes the drug has shut down its dermatological division and is no longer pursuing new drugs from that division including RU58841. It is unknown whether they will license the treatment to other companies.
Technical RU 58841 (C17H18N3O3F3)
Molecular Weight = 369.352; C,55.28;H,4.91;N,11.38
http://www.regrowth.com/hairloss-remedy ... u58841.cfm
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vovach777
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http://www.farrellmanual.com/topical/ru.htm
RU58841 - рулит. Его мешанина с миноксидилом будет рулить.
Ждемс. На RU58841 одна надежда.
RU58841 - рулит. Его мешанина с миноксидилом будет рулить.
Ждемс. На RU58841 одна надежда.
доктор не упоминал его чёта в ряду новинок. 
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vovach777
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Будет продаваться как Эвкапил - дохтур тебе его на блюдечке с голубой каёмочкой предложит...
Наружние антиандрогены - это новинка. Эвкапил - такая же мешанина только в более профинансированом масштабе.
фарм промышленость отстает на 10 лет. Исследования - длительная штука. Эвкапил в этом плане очень смелый проект.
Наружние антиандрогены - это новинка. Эвкапил - такая же мешанина только в более профинансированом масштабе.
фарм промышленость отстает на 10 лет. Исследования - длительная штука. Эвкапил в этом плане очень смелый проект.
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vovach777
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http://www.hairsite4.com/dc/dcboard.php ... full#29802
Treatment of alopecia areata in the DEBR model using Cyclosporin A lipid vesicles.
Verma DD, Verma S, McElwee KJ, Freyschmidt-Paul P, Hoffman R, Fahr A.
Institute for Pharmaceutical Technology and Biopharmacy, Department of Pharmaceutical Sciences, Bouve College of Health Sciences, 312 Mugar Building, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA. ddverma@yahoo.com
Alopecia areata (AA) is a chronic cutaneous disease with a suspected autoimmune origin. We evaluated the efficacy of 0.5% Cyclosporin A (CyA) in a topically applied liposomal formulation as a potential treatment for AA using the Dundee Experimental Bald Rat (DEBR) model. The vehicle consisted of liposomes (75% phosphatidylcholine, 5% lysophosphatidylcholine, 5% sterol, natural oils) of 10% wt. in ethanol with and without 2% wt. terpenes (d-limonene: citral: cineole, 10:45:45) as a penetration enhancer (PE). Fifteen DEBR were allocated to 3 groups of 5. Groups I, II and III received CyA vesicles with PE, CyA vesicles without PE, and CyA in ethanol respectively. All rats were treated twice a day for 6 weeks within a 4 cm2 area on one bald flank with CyA while the contralateral flank received an equivalent control formulation. Rats in group I exhibited visible hair regrowth on the drug treated site after one week of drug application. Group II rats had visible hair regrowth by the end of the second week. The hair growth was progressive and reached a maximum density at the site of application after six weeks in both groups. Histological examination revealed a reduced inflammatory infiltrate and improved hair follicle morphology within the drug treated area as compared to the contralateral vehicle treated skin. Group III rats showed neither visible signs of hair growth nor reduction of hair follicle inflammation. The results of this proof of concept preliminary study suggest that CyA vesicle formulations with and without PE have promising potential as a topical treatment for AA in humans.
"RU 58841-myristate--prodrug development for topical treatment of acne and androgenetic alopecia.
Munster U, Nakamura C, Haberland A, Jores K, Mehnert W, Rummel S, Schaller M, Korting HC, Zouboulis ChC, Blume-Peytavi U, Schafer-Korting M.
Pharmakologie und Toxikologie, Institut fur Pharmazie, Freie Universitat Berlin, Germany.
Acne and androgenetic alopecia are linked to androgen effects and therefore should improve following topical application of antiandrogens. We present a new antiandrogen prodrug, RU 58841-myristate (RUM) for topical therapy. Almost devoid of affinity to the androgen receptor, as derived from investigations in the mouse fibroblast cell line 29 +/GR +, RUM is rapidly metabolised to the potent antiandrogen RU 58841 by cultured human foreskin fibroblasts and keratinocytes, male occipital scalp skin dermal papilla cells, and by cells of the sebaceous gland cell line SZ95. In order to improve a specific targeting of the hair follicle, RUM was loaded on solid lipid nanoparticles (SLN), which are already known to support dermal targeting effects. Physically stable RUM loaded SLN were produced by hot homogenization. Penetration/permeation studies carried out using the Franz diffusion cell proved only negligible permeation of reconstructed epidermis and excised porcine skin within 6 h, implying a more topical action of the drug. Targeting to the hair follicle using SLN was visualised by fluorescence microscopy, following the application of Nile Red labelled SLN to human scalp skin. Transmission electron microscopy (TEM) allowed to detect intact silver labelled SLN in porcine hair follicles of preparations applied to the skin for 24 h. RUM loaded SLN should be considered for topical antiandrogen therapy of acne and androgenetic alopecia.
PMID: 15700772 "