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Related Experiment Videos

Cis-trans interconversion of acitretin in man.

J M Geiger1, C J Brindley

  • 1Department of Clinical Research, F. Hoffmann-La Roche & Co. Ltd., Basel, Switzerland.

Skin Pharmacology : the Official Journal of the Skin Pharmacology Society
|January 1, 1988
PubMed
Summary

Acitretin stereoisomers interconvert in the body, leading to higher cis-acitretin levels than expected. This unexpected isomer interaction may explain the reduced therapeutic effect observed in skin conditions like psoriasis.

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Area of Science:

  • Pharmacology
  • Dermatology
  • Medicinal Chemistry

Background:

  • Acitretin, a retinoid, is used to treat dermatological conditions.
  • The primary metabolite of trans-acitretin is its cis isomer, cis-acitretin.
  • Oral retinoids are generally effective for conditions such as psoriasis.

Purpose of the Study:

  • To investigate the interconversion of cis-acitretin and trans-acitretin in humans.
  • To assess the plasma concentrations and therapeutic effects of administering cis-acitretin orally.
  • To explore potential reasons for observed differences in therapeutic activity between stereoisomers.

Main Methods:

  • Administration of a single oral dose of cis-acitretin to human subjects.
  • Monitoring plasma concentrations of cis-acitretin (Ro 13-7652) and trans-acitretin (Ro 10-1670).
  • Evaluating therapeutic effects on dermatoses, including psoriasis.

Main Results:

  • Demonstrated in vivo interconversion of cis-acitretin to trans-acitretin after oral administration.
  • Achieved significantly higher plasma concentrations of both cis-acitretin and trans-acitretin following cis-acitretin administration compared to trans-acitretin administration.
  • Observed a lack of clear therapeutic effect in dermatoses despite high plasma retinoid levels.

Conclusions:

  • Oral administration of cis-acitretin leads to significant systemic exposure of both cis and trans isomers.
  • The therapeutic efficacy of orally administered acitretin may be influenced by interactions between its cis and trans isomers formed in vivo.
  • Further research is needed to elucidate the mechanisms behind the differential therapeutic activity of acitretin stereoisomers.

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