"Excema Therapy Elidel (Pimecrolimus) Shows Lower Rate of Skin Permeation Than With Protopic (Tacrolimus)"
PROVIDENCE, RI -- May 10,l 2004 -- New data presented have shed further light on the pharmacological profile of Elidel® (pimecrolimus) Cream 1%, by showing that it permeates through the skin into the bloodstream up to six times less than Protopic (tacrolimus), another treatment for atopic dermatitis in the same therapeutic class. The study[1, presented at the Society for Investigative Dermatology meeting in Providence, Rhode Island, USA, shows that Elidel cream is characterised by extremely low levels of permeation through the skin, in contrast to Protopic. These in vitro data are in line with clinical data in patients showing that systemic absorption of pimecrolimus after topical application is minimal, even in patients with extensive body surface involvement (i.e. up to 92%2). As a result of this low permeation through skin, the risk of systemic effects associated with topical application of Elidel is considered to be minimal.
In the latest research, scientists applied Elidel cream 1% and Protopic ointment 0.1% and 0.03% to samples of human skin, and measured the penetration and permeation of the active compounds in vitro. The permeation rate through the skin of pimecrolimus was found to be around six times lower than that of tacrolimus from 0.1% Protopic ointment (i.e. 0.67 ± 0.35 vs. 4.1 ± 0.7 ng/ml/hr). When Elidel was compared with Protopic 0.03% (2.9 ± 0.3 ng/ml/hr), pimecrolimus permeation was still lower by a factor of 4.3.
The concentration of the two drugs in t he skin - where their therapeutic activity occurs - was similar for Elidel 1% and Protopic 0.1% (4.4 ± 2.6 and 3.6 ± 0.6 µg/g respectively), whereas Protopic 0.03% yielded around two-fold lower levels (1.7 ± 0.4 µg/g).
Zoe Draelos, MD, Clinical Associate Professor of Dermatology at Wake Forest University School of Medicine, North Carolina, USA, said, "Evidence from more than 8,000 patients in clinical trials, and post-marketing safety reports covering more than five million patient-months, have already confirmed the favorable safety profile of Elidel cream. This study provides further reassurance by demonstrating that permeation of pimecrolimus through human skin in vitro is very low."
"This information is particularly important in the treatment of young children and for patients with extensive body surface involvement, who are at risk of systemic effects from topical steroids. In these patients, Elidel represents a valuable therapeutic alternative due to its very low systemic absorption properties."
About Elidel
Elidel is the only steroid-free prescription cream for eczema. Elidel is currently available and approved for the short-term and intermittent long-term treatment of mild to moderate eczema in patients as young as two years old that do not respond well to, or may have side effects with, conventional treatments. Elidel is the number one prescribed brand for eczema.
Elidel is manufactured and marketed by Novartis.
Contraindications and Adverse Events
In clinical trials with Elidel, the most common side effect on the skin was a mild to moderate, temporary feeling of warmth or burning (occurring in 8% of children aged 2-7 years and in 26% of adults). This side effect was temporary and its occurrences were comparable to those experienced by patients on vehicle cream. Other common side effects included headache and cold symptoms, such as stuffy nose, sore throat, cough and rarely viral skin infections. Elidel did not elicit skin atrophy, sometimes seen with long-term topical corticosteroid use.
Developed by the Novartis Research Institute, Elidel may be used on all skin surfaces, including delicate areas such as the face, neck and skin folds. The active ingredient is pimecrolimus, which is derived from ascomycin, a natural substance produced by the fungus Streptomyces hygroscopicus var. ascomyceticus. Pimecrolimus selectively blocks the production and release of cytokines from T-cells. These cytokines in the skin cause the inflammation, redness and itching associated with eczema.
About Eczema
Currently, eczema affects up to 17 percent of the U.S. population. Mild to moderate sufferers age two and older make up the vast majority of this eczema patient population. As conventional therapies can be inadvisable and/or ineffective for many of these eczema patients, Elidel serves as a valuable treatment option for this large population.
References: 1 Billich A, Aschauer H, Stuetz A. In vitro skin penetration/permeation of pimecrolimus and tacrolimus from their marketed formulations (Elidel and Protopic). 2 Harper J, Lakhanpaul M, Wahn U, Pariser D, Gottlieb AB, Kaufmann R, Eichenfield L, Langely R, Scott G, Ebelin M-E, Burtin P. Pimecrolimus (Elidel®, SDZ ASM 981 Cream 1%) blood levels are consistently low in children with extensive atopic dermatitis. Abstract at EADV 2001
SOURCE: Novartis Pharmaceuticals Corporation
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