The Japanese have done it again! This time with with a completely new approach…here’s a brief summary:
Discovery of TASP0382088: a potent and selective transforming growth factor-Beta type I receptor inhibitor as a topical drug for alopecia[/]
Medicinal Chemistry Laboratories, Taisho Pharmaceutical Co., Ltd., Saitama, Japan
Hideaki Amada,*, Hajime Asanuma, Takeshi Koami, Atsushi Okada, Mayumi Endo, Yasuji Ueda, Takumi Naruse, and Akiko Ikedab
Published in: July 2013
TGF-Beta is well known to exhibit significant growth inhibitory activities against various cells, such as epithelial cells, vascular endothelial cells, hematocytes or lymphocytes. Regarding hair follicles, it has been reported that TGF-Beta hyper-expression induces growth suppression/apoptosis in hair follicle cells, shifting the hair cycle from anagen to catagen, and TGF-Beta has been strongly implicated in the progression of alopecia. In addition, it has been reported that TGF-Beta/Smad2 signaling pathway has a strong relation ship with hair growth suppression based on research involving transgenic mice overexpressing Smad2 in the epidermis under the control of keratin 14 promoter. Based on these findings, compounds that inhibit ALK5 and block the TGF-Beta;/Smad signaling pathway might have the potential to ameliorate alopecia.
In this study, they overcame all the solubility problems and came up with a lotion form that did not affect the potency of this molecule and increased solubility by 3 fold!
“The potency of compound II was maintained in both the enzyme and cellular assays, and II was more than three times more soluble in the lotion
base than I”
Interesting stuff Thought I should share it with you guys…