Thyroid receptor agonists for the treatment of androgenetic alopecia

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 1, 2010, Pages 306-308

  Li, Jie Jack ^a   Mitchell, Lorna H ^a   Dow, Robert L ^a  

^a PFIZER INC   (United States)

Author keywords

Androgenetic alopecia; Photo irritation; Skin penetration; Thyromimetics; Topical drug

Indexed keywords

PF 00277343; THYROMIMETIC AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG METABOLISM; DRUG STRUCTURE; HAIR GROWTH; MACACA; MALE TYPE ALOPECIA; MOUSE; NONHUMAN; PHOTOTOXICITY; SKIN PENETRATION;

ADMINISTRATION, TOPICAL; ALOPECIA; ANIMALS; BALB 3T3 CELLS; HAIR; HUMANS; MACACA; MICE; NEUTRAL RED; RECEPTORS, THYROID HORMONE; SKIN ABSORPTION; TRIAZINES;

MACACA ARCTOIDES;

EID: 72049126590     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.109     Document Type: Article

References (15)

1. Safer J.D., Fraser L.M., Ray S., and Holick M.F. Thyroid 11 (2001) 717
2. van Beek N., Bodo E., Kromminga A., Gaspar E., Meyer K., Zmijewski M.A., Slominski A., Wenzel B.E., and Paus R. J. Clin. Endocrin. Metab. 93 (2008) 4381
3. Billoni N., Buan B., Gautier B., Gaillard O., Mahe Y.F., and Bernard B.A. Br. J. Dermatol. 142 (2000) 645
4. Bodo E., Kromminga A., Biro T., Borbiro I., Gaspar E., Zmijewski M.A., van Beek N., Langbein L., Slominski A.T., and Paus R. J. Invest. Dermatol. 12 (2009) 1126
5. Dow R.L., Schneider S.R., Paight E.S., Hank R.F., Chiang P., Cornelius P., Lee E., Newsome W.P., Swick A.G., Spitzer J., Hargrove D.M., Patterson T.A., Pandit J., Chrunyk B.A., LeMotte P.K., Danley D.E., Rosner M.H., Ammirati M.J., Simons S.P., Schulte G.K., Tate B.F., and DaSilva-Jardine P. Bioorg. Med. Chem. Lett 13 (2003) 379
6. Chian, Y.-C. P.; Cornelius, P.; Doherty, N. S.; Dow, R. L. EP1262177, 2002.
7. 2). Ten mice were used in each experimental group. The treatment regimen was twice daily (BID) application for 4 weeks, 5 days/week from Monday to Friday. Local irritation was recorded before each application and hair growth scores were recorded every other day. After 4 weeks of treatment, mice were further observed for one more week during which hair growth and skin irritation were scored every other day. The scale used for scoring hair growth was: 0 = no hair growth, pink skin; 1 = skin color changes from pink to gray or black without visible hair growth, indicating the onset of anagen; 2 = sparse or diffuse short hair growth; 3 = dense, normal coat hair. A reference androgen receptor antagonist (RU-58841) was included in every study.
8. Thomas V.H., Bhattachar S., Hitchingham L., Zocharski P., Naath M., Surendran N., Stoner C.L., and El-Kattan A. Exp. Opin. Drug Metab. Toxicol. 2 (2006) 591
9. See:. Antille C., Tran C., Sorg O., and Saurat J.-H. Exp. Dermatol. 13 (2004) 558
10. Nam C., An S., Lee E., Moon S., Kang J., and Chang I. ATLA, Altern. Lab. Anim. 32 (2004) 693
11. Spielmann, H.; Alternatives to Animal Testing II, Proceedings of the International Scientific Conference, 2nd, Brussels, 1999, pp 15-24.
12. A similar paper has recently been published:. Li Y., Chang M.-q., Gao F., and Gao W.-t. J. Chem. Res (2008) 640
13. Janey J.M. Buchwald-Hartwig Amination. In: Li J.J., and Corey E.J. (Eds). Name Reactions for Functional Group Transformations (2007), Wiley & Sons, Hoboken, NJ 564-609
14. see. Buck E., Song Z.J., Tschaen D., Dormer P.G., Volante R.P., and Reider P.J. Org. Lett. 4 (2002) 1623
15. Uno H., Cappas A., and Brigham P. J. Am. Acad. Dermatol. 16 (1987) 657