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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

Dermatop     [2-(17-ethoxycarbonyloxy-11- hydroxy-10,13...

Synonyms: Peitel, Dermatop (TN), Hoe-777, AGN-PC-00J0T5, AG-G-92143, ...
 
 
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Disease relevance of Hoe 777

 

High impact information on Hoe 777

  • CONCLUSIONS: Prednicarbate and hydrocortisone aceponate are intermediate potent glucocorticoids that are superior to betamethasone 17-valerate because of the improved benefit/risk ratio [1].
  • Fibroblast migration was dosage dependently inhibited from 10(-9) M to 10(-5) M for desoximetasone, while incubation with prednicarbate did not cause a reduction of the chemotactic response at concentrations lower than 10(-7) M [6].
  • To reduce the risk of dermal atrophy, we aimed at BMV incorporation into solid lipid nanoparticles (SLN) for epidermal targeting using various lipids and emulsifiers corresponding to previous work on PC [2].
  • PURPOSE: To investigate pharmacokinetic differences between the nonhalogenated double ester prednicarbate (PC) and the fluorinated monoester betamethasone 17-valerate (BM17V) their metabolism in human keratinocytes and fibroblasts as well as their permeation and biotransformation in reconstructed epidermis and excised human skin was compared [7].
  • PURPOSE: Evaluation of skin layer-specific prednicarbate (PC) biotransformation, possibly explaining the improved benefit/risk ratio of this topical corticosteroid in atopic dermatitis (1,2) [8].
 

Chemical compound and disease context of Hoe 777

 

Biological context of Hoe 777

 

Anatomical context of Hoe 777

  • In transfected COS-7 cells we related the transcriptional potencies of PC, its metabolites and conventional GC to their receptor binding properties [12].
 

Gene context of Hoe 777

  • The remarkable anti-inflammatory effects of PC are in strong contrast to its reported low glucocorticoid receptor (GR) binding affinity [12].
  • Interestingly, bovine serum albumin (BSA) commonly used in receptor media in permeation studies to facilitate solubility of highly lipophilic substances strongly inhibited the metabolism of topically applied prednicarbate in reconstructed epidermis [13].
 

Analytical, diagnostic and therapeutic context of Hoe 777

References

  1. Prednicarbate activity and benefit/risk ratio in relation to other topical glucocorticoids. Schäfer-Korting, M., Korting, H.C., Kerscher, M.J., Lenhard, S. Clin. Pharmacol. Ther. (1993) [Pubmed]
  2. Glucocorticoid entrapment into lipid carriers--characterisation by parelectric spectroscopy and influence on dermal uptake. Sivaramakrishnan, R., Nakamura, C., Mehnert, W., Korting, H.C., Kramer, K.D., Schäfer-Korting, M. Journal of controlled release : official journal of the Controlled Release Society. (2004) [Pubmed]
  3. Allergic contact dermatitis from prednicarbate. Dunkel, F.G., Elsner, P., Burg, G. Contact Derm. (1991) [Pubmed]
  4. Efficacy and safety of silver textile in the treatment of atopic dermatitis (AD). Juenger, M., Ladwig, A., Staecker, S., Arnold, A., Kramer, A., Daeschlein, G., Panzig, E., Haase, H., Heising, S. Current medical research and opinion. (2006) [Pubmed]
  5. Allergic contact dermatitis to prednicarbate presenting as lupus erythematosus. Sánchez-Pérez, J., Pérez Gala, S., Delgado Jiménez, Y., Fraga, J., García Diez, A. Contact Derm. (2006) [Pubmed]
  6. Influence of corticosteroids on chemotactic response and collagen metabolism of human skin fibroblasts. Hein, R., Mauch, C., Hatamochi, A., Krieg, T. Biochem. Pharmacol. (1988) [Pubmed]
  7. Skin penetration and metabolism of topical glucocorticoids in reconstructed epidermis and in excised human skin. Gysler, A., Kleuser, B., Sippl, W., Lange, K., Korting, H.C., Höltje, H.D., Korting, H.C. Pharm. Res. (1999) [Pubmed]
  8. Prednicarbate biotransformation in human foreskin keratinocytes and fibroblasts. Gysler, A., Lange, K., Korting, H.C., Schäfer-Korting, M. Pharm. Res. (1997) [Pubmed]
  9. Small reduction of capsaicin-induced neurogenic inflammation in human forearm skin by the glucocorticoid prednicarbate. Tafler, R., Herbert, M.K., Schmidt, R.F., Weis, K.H. Agents Actions (1993) [Pubmed]
  10. Prednicarbate (Dermatop): profile of a corticosteroid. Gupta, A.K., Chow, M. Journal of cutaneous medicine and surgery. (2004) [Pubmed]
  11. Studies on the pharmacokinetics and metabolism of prednicarbate after cutaneous and oral administration. Barth, J., Lehr, K.H., Derendorf, H., Möllmann, H.W., Höhler, T., Hochhaus, G. Skin Pharmacol. (1993) [Pubmed]
  12. Transcriptional activity of potent glucocorticoids: relevance of glucocorticoid receptor isoforms and drug metabolites. Spika, I., Hammer, S., Kleuser, B., Korting, H.C., Schäfer-Korting, M. Skin Pharmacol. Appl. Skin Physiol. (2003) [Pubmed]
  13. The impact of skin viability on drug metabolism and permeation -- BSA toxicity on primary keratinocytes. Haberland, A., Schreiber, S., Maia, C.S., Rübbelke, M.K., Schaller, M., Korting, H.C., Kleuser, B., Schimke, I., Schäfer-Korting, M. Toxicology in vitro : an international journal published in association with BIBRA. (2006) [Pubmed]
  14. Solid lipid nanoparticles as drug carriers for topical glucocorticoids. Maia, C.S., Mehnert, W., Schäfer-Korting, M. International journal of pharmaceutics. (2000) [Pubmed]
  15. Comparison of various pharmaceutical preparations of prednicarbate after repeated topical administration to the skin of rats. Vogel, H.G., Petri, W. Arzneimittel-Forschung. (1985) [Pubmed]
  16. Atopic dermatitis -- topical therapy: do patients apply much too little? Niemeier, V., Kupfer, J., Schill, W.B., Gieler, U. The Journal of dermatological treatment. (2005) [Pubmed]
 
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