The atypical retinoid E-3-(3'-Adamantan-1-yl-4'-methoxybiphenyl-4-yl)-2-propenoic acid (ST1898) displays comedolytic activity in the rhino mouse model.
Retinoids represent the first-line therapy for the treatment of acne vulgaris. Their effect is comedolytic and anti-comedogenic, and associates with hyperplasia and deregulated differentiation of the epidermis, and decreased inflammation. We here tested the comedolytic effect of the novel atypical retinoid E-3-(3'-Adamantan-1-yl-4'-methoxybiphenyl-4-yl)-2-propenoic acid (ST1898) in the rhino mouse, as a model of comedogenic acne, and compared this effect to that of adapalene (Differin® gel), as reference compound. Topical administration of 0.1% ST1898 for three weeks exerted a comedolytic effect comparable to that of adapalene 0.1%. In ST1898-treated mice, epidermal hyperplasia was significantly reduced and the expression of keratinocyte differentiation markers was less perturbed compared to adapalene-treated animals. Moreover, keratin 6, which stains activated keratinocytes, was strongly and uniformly induced in interfollicular epidermis of adapalene-treated mice, while only faintly and focally expressed in ST1898-treated ones. Our data indicate that ST1898 has strong comedolytic activity but modest topical side effects.
Laboratory of Molecular and Cell Biology, IDI-IRCCS,  Via dei Monti di Creta 104, 00167 Rome, Italy.
Teresa
T
Odorisio
Naomi
N
De Luca
Loredana
L
Vesci
Pier Luigi
PL
Luisi
Pasquale
P
Stano
Giovanna
G
Zambruno
Claudio
C
Pisano
D000152:Acne Vulgaris / Q000188:drug therapy*; D000218:Adamantane / Q000031:analogs & derivatives* / Q000627:therapeutic use; D000068816:Adapalene; D000818:Animals; D002934:Cinnamates / Q000627:therapeutic use*; D003879:Dermatologic Agents / Q000627:therapeutic use; D004195:Disease Models, Animal; D005260:Female; D008297:Male; D051379:Mice; D009281:Naphthalenes / Q000627:therapeutic use
C578524:3-(3'-adamantan-1-yl-4'-methoxybiphenyl-4-yl)-2-propenoic acid; D002934:Cinnamates; D003879:Dermatologic Agents; D009281:Naphthalenes; D000068816:Adapalene; D000218:Adamantane