The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood.

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Presentation transcript:

The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils  Torsten Zuberbier, MDa, Sie-Uen Chong, a, Karl Grunow, MDa, Sven Guhl, a, Pia Welker, PhDa, Maximilian Grassberger, PhDb, Beate M. Henz, MDa  Journal of Allergy and Clinical Immunology  Volume 108, Issue 2, Pages 275-280 (August 2001) DOI: 10.1067/mai.2001.116865 Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 1 Anti-IgE–induced (2000 IU/mL) histamine release from human dermal mast cells preincubated with pimecrolimus (Pim ; mean ± SEM, n = 10, histamine release of controls = 13% ± 1.6% of total histamine, P < .01 for concentrations of ≥10 nmol/L pimecrolimus), cyclosporin A (CsA ), and dexamethasone (Dexa ; mean ± SEM; n = 3; histamine release of controls = 7.6% ± 1.5% of total histamine). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 2 Effect of the pimecrolimus (Pim ) antagonist rapamycin (RA ) on pimecrolimus during anti-IgE–induced (2000 IU/mL) histamine release (mean ± SEM; n = 5; histamine release of controls = 10.4% ± 1.9 of total histamine; P > .05). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 3 Dose-dependent effect of pimecrolimus (Pim ) on anti-IgE–induced (2000 IU/mL) tryptase release from dermal mast cells (mean ± SEM; n = 3). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 4 Dose-dependent influence of pimecrolimus (Pim ) and cyclosporin A (CsA ; 100 nmol/L) on anti-IgE–induced (2000 IU/mL) LTC4 release from dermal mast cells (mean ± SEM; n = 3; LTC4 release of controls = 63 ± 21 pg/mL). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 5 Dose-dependent effect of pimecrolimus (Pim ) on calcium ionophore A23187 (0.2 μmol/L) plus PMA–induced (20 ng/mL) TNF-α release from purified dermal mast cells (mean ± SEM; n = 4; TNF-α release of controls = 508 ± 134 pg/mL). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions

Fig. 6 Dose-dependent effect of pimecrolimus (Pim ) on anti-IgE–induced (200 IU/mL) histamine release from human basophils (mean ± SEM; n = 3; histamine release of controls = 28.3% ± 5.4% of total histamine). Journal of Allergy and Clinical Immunology 2001 108, 275-280DOI: (10.1067/mai.2001.116865) Copyright © 2001 Mosby, Inc. Terms and Conditions