PMID: 8583361Aug 1, 1995Paper

In-vivo activity of retinoid esters in skin is related to in-vitro hydrolysis rate

The Journal of Pharmacy and Pharmacology
S ChenK M Tramposch

Abstract

BMS-181163 (4-acetamidophenyl retinoate, previously reported as BMY-30123), the acetamidophenyl ester of all-trans-retinoic acid (tRA), is topically active in various retinoid-sensitive animal models, but was recently shown to be ineffective for the treatment of acne in patients. To determine whether BMS-181163 functions as a prodrug of tRA in mice but not in man, the relative rates of ester hydrolysis in mouse and human skin homogenates were determined. In-vitro hydrolysis assays showed that BMS-181163 was substantially hydrolysed in mouse skin homogenates and minimally in human skin preparations. In addition, a series of phenyl esters of tRA and several known active synthetic retinoids (Ch-80: (E)-4-[3-oxo-3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1 - propenyl] benzoic acid; CD-271: 6-[3-(1-adamantyl)-4-methyoxyphenyl]-2-naphthoic acid; and TTNPB: (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1- propenyl] benzoic acid) was prepared and hydrolysis rates and in-vivo (rhino mouse utriculi reduction) activities were compared. The hydrolysis rates of the six test retinoid phenyl esters, ranging from 0.06 to 2.0 h-1 were found to correlate with the in-vivo activity. Those esters (BMS-181163 and ac...Continue Reading

References

Jun 1, 1979·The Journal of Pharmacy and Pharmacology·Y W Yip, L W Po
May 1, 1992·The Journal of Pharmacy and Pharmacology·K M TramposchR J Bonney
Sep 1, 1989·Journal of the American Academy of Dermatology·J J LeydenL Lufrano
Oct 1, 1986·Journal of the American Academy of Dermatology·A M KligmanJ J Leyden
Apr 1, 1969·Kango kyoshitsu. [Nursing classroom]·K Fujita
Jun 1, 1984·The Journal of Investigative Dermatology·R E AshtonN J Lowe

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