Skip to main content

Retinoid Pharmacology

  • Chapter
Therapy of Skin Diseases

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 119.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 159.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 219.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  1. Kurlandsky SB, Duell EA, Kang S, Voorhees JJ, Fisher GJ (1996) Auto-regulation of retinoic acid biosynthesis through regulation of retinol esterification in human keratinocytes. J Biol Chem 271(26):15346È“15352

    Article  PubMed  CAS  Google Scholar 

  2. Petkovich PM (2001) Retinoic acid metabolism. J Am Acad Dermatol 45(5):S136–S142

    Article  PubMed  CAS  Google Scholar 

  3. Roos TC, Jugert FK, Merk HF, Bickers DR (1998) Retinoid metabolism in the skin. Pharmacol Rev 50(2):315–333

    PubMed  CAS  Google Scholar 

  4. Baron JM, Heise R, Blaner W, Neis M, Joussen S, Dreuw A, Marquardt Y, Saurat JH, Merk HF, Bickers DR, Jugert FK (2005) Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol 125(1):143–153

    Article  PubMed  CAS  Google Scholar 

  5. Duell EA, Astrom A, Griffiths CE, Chambon P, Voorhees JJ (1992) Human skin levels of retinoic acid and cytochrome P-450-derived 4-hydroxyretinoic acid after topical application of retinoic acid in vivo compared to concentrations required to stimulate retinoic acid receptor-mediated transcription in vitro. J Clin Invest 90(4):1269–1274

    Article  PubMed  CAS  Google Scholar 

  6. Heise R, Mey J, Neis M, Marquardt Y, Joussen S, Ott H, Wiederholt T, Kurschat P, Megahed M, Bickers DR, Merk HF, Baron JM (2006) Skin retinoid concentrations are modulated by CYP26AI expression restricted to basal keratino-cytes in normal human skin and differentiated 3D-skin models. J Invest Dermatol 126:2473–2480

    Article  PubMed  CAS  Google Scholar 

  7. Smith G, Wolf CR, Deeni YY, Dawe RS, Evans AT, Comrie MM, Ferguson J, Ibbotson SH (2003) Cutaneous expression of cytochrome P450 CYP2S1: individuality in regulation by therapeutic agents for psoriasis and other skin diseases. Lancet 361:1336–1343

    Article  PubMed  CAS  Google Scholar 

  8. van de Kerkhof PC (2006) Update on retinoid therapy of psoriasis in: an update on the use of retinoids in dermatology. Dermatol Ther 19(5):252–263

    Article  PubMed  Google Scholar 

  9. Karlsson T, Rollman O, Vahlquist A, Torma H (2004) Immunofluorescence localization of nuclear retinoid receptors in psoriasis versus normal human skin. Acta Derm Venereol 84(5):363–369

    Article  PubMed  CAS  Google Scholar 

  10. Fisher GJ, Voorhees JJ (1996) Molecular mechanisms of retinoid actions in skin. FASEB J 10(9):1002–1013

    PubMed  CAS  Google Scholar 

  11. Saurat JH, Didierjean L, Masgrau E, Piletta PA, Jaconi S, Chatellard-Gruaz D, Gumowski D, Masouye I, Salomon D, Siegenthaler G (1994) Topical retinaldehyde on human skin: biologic effects and tolerance. J Invest Dermatol 103(6):770–774

    Article  PubMed  CAS  Google Scholar 

  12. Sorg O, Tran C, Saurat JH (2001) Cutaneous vitamins A and E in the context of ultraviolet- or chemically-induced oxidative stress. Skin Pharmacol Appl Skin Physiol 14(6):363–372

    Article  PubMed  CAS  Google Scholar 

  13. Sorg O, Antille C, Kaya G, Saurat JH (2006) Retinoids in cosmeceuticals. Dermatol Ther 9(5):289–296

    Article  Google Scholar 

  14. Antille C, Tran C, Sorg O, Carraux P, Didierjean L, Saurat JH (2003) Vitamin A exerts a photoprotective action in skin by absorbing ultraviolet B radiation. J Invest Dermatol 121(5):1163–1167

    Article  PubMed  CAS  Google Scholar 

  15. Creidi P, Vienne MP, Ochonisky S, Lauze C, Turlier V, Lagarde JM, Dupuy P (1998) Profilometric evaluation of photodamage after topical retinaldehyde and retinoic acid treatment. J Am Acad Dermatol 39(6):960–965

    Article  PubMed  CAS  Google Scholar 

  16. Ortonne JP (2006) Retinoid therapy of pigmentary disorders. Dermatol Ther 19(5):280–288

    Article  PubMed  Google Scholar 

  17. Vahlquist A, Lee JB, Michaelsson G, Rollman O (1982) Vitamin A in human skin: II Concentrations of carotene, retinol and dehydroretinol in various components of normal skin. J Invest Dermatol 79(2):94–97

    Article  PubMed  CAS  Google Scholar 

  18. Stuettgen D (1962) Zur Lokalbehandlung von Keratosen mit Vitamin A-Säure. Dermatologica 124:65–80

    Article  PubMed  CAS  Google Scholar 

  19. Thielitz A, Krautheim A, Gollnick H (2006) Update in retin-oid therapy of acne. Dermatol Ther 19(5):272–279

    Article  PubMed  Google Scholar 

  20. Krautheim A, Gollnick HP (2004) Acne: topical treatment. Clin Dermatol 22(5):398–407

    Article  PubMed  Google Scholar 

  21. Bianchi L, Orlandi A, Campione E, Angeloni C, Costanzo A, Spagnoli LG, Chimenti S (2004) Topical treatment of basal cell carcinoma with tazarotene: a clinicopathological study on a large series of cases. Br J Dermatol 151(1):148–156

    Article  PubMed  CAS  Google Scholar 

  22. Rafal ES, Griffiths CE, Ditre CM, Finkel LJ, Hamilton TA, Ellis CN, Voorhees JJ (1992) Topical tretinoin (retinoic acid) treatment for liver spots associated with photodamage. N Engl J Med 326(6):368–374

    Article  PubMed  CAS  Google Scholar 

  23. Uno H, Cappas A, Dong S, Kligman AM (1991) The effect of topical tretinoin on the facial macula of the macaque. J Invest Dermatol 96:632

    Article  Google Scholar 

  24. Yoshimura K, Tsukamoto K, Okazaki M, Virador VM, Lei TC, Suzuki Y, Uchida G, Kitano Y, Harii K (2001) Effects of all-trans retinoic acid on melanogenesis in pigmented skin equivalents and monolayer culture of melanocytes. J Dermatol Sci 27(suppl 1):S68–S75

    Article  PubMed  CAS  Google Scholar 

  25. Kasraee B, Fallahi MR, Ardekani GS, Ebrahimi S, Doroudchi G, Omrani GR, Handjani F, Amini M, Tanideh N, Haddadi M, Nikbakhsh M, Jahanbani S, Tran C, Sorg O, Saurat JH (2006) Retinoic acid synergistically enhances the melanocy-totoxic and depigmenting effects of monobenzylether of hydroquinone in black guinea pig skin. Exp Dermatol 15(7):509–514

    Article  PubMed  CAS  Google Scholar 

  26. Kaymak Y, Ilter N (2006) The effectiveness of intermittent isotretinoin treatment in mild or moderate acne. J Eur Acad Dermatol Venereol 20(10):1256–1260

    Article  PubMed  CAS  Google Scholar 

  27. The European Agency for the Evaluation of Medicinal Products. Committee for Proprietary Medicinal Products. Summary information on a referral opinion following an arbitration pursuant to article 29 of Directive 2001/83/EC for isotretinoin. CPMP/8211/03, 17 October 2003

    Google Scholar 

  28. Baumann L, Vujevich J, Halem M, Martin LK, Kerdel F, Lazarus M, Pacheco H, Black L, Bryde J (2005) Open-label pilot study of alitretinoin gel 0.1% in the treatment of pho-toaging. Cutis 76(1):69–73

    PubMed  Google Scholar 

  29. Scheinfeld N (2006) Schools of pharmacology: retinoid update. J Drugs Dermatol 5(9):921–922

    PubMed  Google Scholar 

  30. Saurat JH (1999) Retinoids and psoriasis: novel issues in retinoid pharmacology and implications for psoriasis treatment. J Am Acad Dermatol 41(3 Pt 2):S2–S6

    Article  PubMed  CAS  Google Scholar 

  31. Pearce DJ, Klinger S, Ziel KK, Murad EJ, Rowell R, Feldman SR (2006) Low-dose acitretin is associated with fewer adverse events than high-dose acitretin in the treatment of psoriasis. Arch Dermatol 142(8):1000–1004

    Article  PubMed  CAS  Google Scholar 

  32. Bikowski JB (2005) Mechanisms of the comedolytic and anti-inflammatory properties of topical retinoids. J Drugs Dermatol 4(1):41–47

    PubMed  Google Scholar 

  33. Jain S (2004) Topical tretinoin or adapalene in acne vulgaris: an overview. J Dermatolog Treat 15(4):200–207

    Article  PubMed  CAS  Google Scholar 

  34. Shroot B, Michel S, Allec J, Chatelus A, Wagner N (1998) A new concept of drug delivery for acne. Dermatology 196(1):165–170

    Article  PubMed  CAS  Google Scholar 

  35. Ioannides D, Rigopoulos D, Katsambas A (2002) Topical adapalene gel 0.1% vs. isotretinoin gel 0.05% in the treatment of acne vulgaris: a randomized open-label clinical trial. Br J Dermatol 147(3):523–527

    Article  PubMed  CAS  Google Scholar 

  36. Pariser DM, Thiboutot DM, Clark SD, Jones TM, Liu Y, Graeber M (2005) The efficacy and safety of adapalene gel 0.3% in the treatment of acne vulgaris: a randomized, multicenter, investigator-blinded, controlled comparison study versus adapalene gel 0.1% and vehicle. Cutis 76(2):145–151

    PubMed  Google Scholar 

  37. Thiboutot DM, Shalita AR, Yamauchi PS, Dawson C, Arsonnaud S, Kang S; on behalf of the Differin Study Group (2005) Combination therapy with adapalene gel 0.1% and doxycycline for severe acne vulgaris: a multicenter, investigator-blind, randomized, controlled study. Skin Med 4(3):138–146

    Article  Google Scholar 

  38. Altinyazar HC, Koca R, Tekin NS, Esturk E (2005) Adapalene vs. metronidazole gel for the treatment of rosa-cea. Int J Dermatol 44(3):252–255

    CAS  Google Scholar 

  39. Nagpal S, Chandraratna RA (2000) Recent developments in receptor-selective retinoids. Curr Pharm Des 6(9):919–913

    Article  PubMed  CAS  Google Scholar 

  40. Nagpal S, Thacher SM, Patel S, Friant S, Malhotra M, Shafer J, Krasinski G, Asano AT, Teng M, Duvic M, Chandraratna RA (1996) Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acid recep-tor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ 7(12):1783–1791

    PubMed  CAS  Google Scholar 

  41. Esgleyes-Ribot T, Chandraratna RA, Lew-Kaya DA, Sefton J, Duvic M (1994) Response of psoriasis to a new topical retinoid, AGN 190168. J Am Acad Dermatol 30(4):581–590

    Article  PubMed  CAS  Google Scholar 

  42. Krueger GG, Drake LA, Elias PM, Lowe NJ, Guzzo C, Weinstein GD, Lew-Kaya DA, Lue JC, Sefton J, Chandraratna RA (1998) The safety and efficacy of tazarotene gel, a topical acetylenic retinoid, in the treatment of psoriasis. Arch Dermatol 134(1):57–60

    Article  PubMed  CAS  Google Scholar 

  43. Behrens S, Grundmann-Kollmann M, Schiener R, Peter RU (2000) Kerscher MCombination phototherapy of psoriasis with narrow-band UVB irradiation and topical tazarotene gel. J Am Acad Dermatol 42(3):493–495

    Article  PubMed  CAS  Google Scholar 

  44. Tzaneva S, Honigsmann H, Tanew A, Seeber A (2002) A comparison of psoralen plus ultraviolet A (PUVA) mono-therapy, tacalcitol plus PUVA and tazarotene plus PUVA in patients with chronic plaque-type psoriasis. Br J Dermatol 147(4):748–753

    Article  PubMed  CAS  Google Scholar 

  45. Dummer R, Cozzio A, Meier S, Beyeler M, Laetsch B, Doebbeling U, Urosevic (2006) Standard and experimental therapy in cutaneous T-cell lymphomas. J Cutan Pathol 33(suppl 1):52–57

    Article  PubMed  Google Scholar 

  46. Budgin JB, Richardson SK, Newton SB, Wysocka M, Zaki MH, Benoit B, Rook AH (2005) Biological effects of bex-arotene in cutaneous T-cell lymphoma. Arch Dermatol 141(3):315–321

    Article  PubMed  CAS  Google Scholar 

  47. Smit JV, de Jong EM, van Hooijdonk CA, Otero ME, Boezeman JB, van de Kerkhof PC (2004) Systemic treatment of psoriatic patients with bexarotene decreases epidermal proliferation and parameters for inflammation, and improves differentiation in lesional skin. J Am Acad Dermatol 51(2):257–264

    Article  PubMed  Google Scholar 

  48. Duvic M, Martin AG, Kim Y et al (2001) Phase 2 and 3 clinical trial of oral bexarotene (Targretin capsules) for the treatment of refractory or persistent early-stage cutaneous T-cell lymphoma. Arch Dermatol 137:581–593

    PubMed  CAS  Google Scholar 

  49. Assaf C, Bagot M, Dummer R, Duvic M, Gniadecki R, Knobler R, Ranki A, Schwandt P, Whittaker S (2006) Minimizing adverse side-effects of oral bexarotene in cutaneous T-cell lymphoma: an expert opinion. Br J Dermatol 155(2):261–266

    Article  PubMed  CAS  Google Scholar 

  50. Thacher SM, Vasudevan J, Chandraratna RA (2000) Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des 6(1):25–58

    Article  PubMed  CAS  Google Scholar 

  51. Bardazzi F, Bianchi F, Parente G, Guareschi E, Landi C (2005) A pilot study on the use of topical tazarotene to treat squamous cell carcinoma in situ. J Am Acad Dermatol 52(6):1102–1104

    Article  PubMed  Google Scholar 

  52. Peris K, Ferrari A, Fargnoli MC, Piccolo D, Chimenti S (2005) Dermoscopic monitoring of tazarotene treatment of superficial basal cell carcinoma. Dermatol Surg 31(2):217–220

    Article  PubMed  CAS  Google Scholar 

  53. Lucker GP, Verfaille CJ, Heremans AM, Vanhoutte FP, Boegheim JP, Steijlen PP (2005) Topical liarozole in ich-thyosis: a double-blind, left-right comparative study followed by a long-term open maintenance study. Br J Dermatol 152(3):566–569

    Article  PubMed  CAS  Google Scholar 

  54. Nohynek GJ, Meuling WJ, Vaes WH, Lawrence RS, Shapiro S, Schulte S, Steiling W, Bausch J, Gerber E, Sasa H, Nau H (2006) Repeated topical treatment, in contrast to single oral doses, with Vitamin A-containing preparations does not affect plasma concentrations of retinol, retinyl esters or retinoic acids in female subjects of child-bearing age. Toxicol Lett 163(1):65–76

    Article  PubMed  CAS  Google Scholar 

  55. Loureiro KD, Kao KK, Jones KL, Alvarado S, Chavez C, Dick L, Felix R, Johnson D, Chambers CD (2005) Minor malformations characteristic of the retinoic acid embryopa-thy and other birth outcomes in children of women exposed to topical tretinoin during early pregnancy. Am J Med Genet A 136(2):117–121

    PubMed  Google Scholar 

  56. Anadolu RY, Sen T, Tarimci N, Birol A, Erdem C (2004) Improved efficacy and tolerability of retinoic acid in acne vulgaris: a new topical formulation with cyclodextrin complex psi. J Eur Acad Dermatol Venereol 18(4):416–421

    Article  PubMed  CAS  Google Scholar 

  57. Dreno B, Bettoli V, Ochsendorf F, Perez-Lopez M, Mobacken H, Degreef H, Layton A (2006) An expert view on the treatment of acne with systemic antibiotics and/or oral isotretin-oin in the light of the new European recommendations. Eur J Dermatol 16(5):565–571

    PubMed  Google Scholar 

  58. Saini R, Tutrone WD, Weinberg JM (2005) Advances in therapy for psoriasis: an overview of infliximab, etanercept, efalizumab, alefacept, adalimumab, tazarotene, and pime-crolimus. Curr Pharm Des 11(2):273–280

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Jens M. Baron .

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2010 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Baron, J.M. (2010). Retinoid Pharmacology. In: Krieg, T., Bickers, D.R., Miyachi, Y. (eds) Therapy of Skin Diseases. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-78814-0_8

Download citation

  • DOI: https://doi.org/10.1007/978-3-540-78814-0_8

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-78813-3

  • Online ISBN: 978-3-540-78814-0

  • eBook Packages: MedicineMedicine (R0)

Publish with us

Policies and ethics