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Ascomycin



Ascomycin
Systematic (IUPAC) name
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Identifiers
CAS number 11011-38-4
ATC code  ?
PubChem 6437370
Chemical data
Formula C43H69NO12 
Mol. mass 792.007
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Ascomycin, also called Immunomycin, FR-900520, FK520, is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It can be used to treat autoimmune diseases and skin diseases, and can help prevent rejection after an organ transplant.

Additional recommended knowledge

Ascomycin acts by binding to immunophilins, especially macrophilin-12. It appears that Ascomycin inhibits the production of Th1 (interferon- and IL-2) and Th2 (IL-4 and IL-10) cytokines. Additionally, ascomycin preferentially inhibits the activation of mast cells, an important cellular component of the atopic response. Ascomycin produces a more selective immunomodulatory effect in that it inhibits the elicitation phase of allergic contact dermatitis but does not impair the primary immune response when administered systemically.

Ascomycin is produced by the fermentation of Streptomyces hygroscopicus.

Related compounds

Tacrolimus, Pimecrolimus

References

  • Griffiths CE. Ascomycin: an advance in the management of atopic dermatitis. Br J Dermatol. 2001. Apr;144(4):679-81.
  • Kawai, M., et al., Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues. FEBS Lett. 1993. 316(2): 107-13.
  • Zuberbier T, Chong SU, Grunow K, Guhl S, Welker P, Grassberger M, Henz BM. The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils. J Allergy Clin Immunol. 2001. Aug;108(2): 275-80.
  • Mollison KW, Fey TA, Krause RA, Thomas VA, Mehta AP, Luly JR. Comparison of FK-506, rapamycin, ascomycin, and cyclosporine in mouse models of host-versus-graft disease and heterotopic heart transplantation. Ann N Y Acad Sci. 1993. Jun 23; 685:55-7.
  • Morisaki M, Arai T., Related Articles, Identity of immunosuppressant FR-900520 with ascomycin. J Antibiot (Tokyo). 1992. Jan;45(1):126-8.
  • Paul C., Graeber M, Stuetz A., Ascomycins: promising agents for the treatment of inflammatory skin diseases. Expert Opin Investig Drugs. 2000. Jan;9(1):69-77.#Mrowietz U., Macrolide immunosuppressants. Eur J Dermatol. 1999. Jul-Aug;9(5):346-51.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Ascomycin". A list of authors is available in Wikipedia.
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