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Pimecrolimus 구조식 이미지
카스 번호:
Elidel;ASM 981;Picrolimus;SDZ-ASM 981;Pimecrolimus;Unii-7kyv510875;PiMecroliMus(Elidel);Pimecrolimus (SDZ-ASM 981);PiMecroliMus(Elidel, SDZ-ASM-981);(9E)-3S-[(1E)-2-[(1R,3R,4S)-4R-chloro-3-methoxycyclohexyl]-1-methylethenyl]-8-ethyl-5S,6,8R,11,12S,13,14S,15R,16S,17,18R,19R,24,25,26,26aS-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-15,19
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Pimecrolimus 속성

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Pimecrolimus C화학적 특성, 용도, 생산


Pimecrolimus is an ascomycin macrolactam derivative, developed as a topical formulation (1% cream) for the treatment of mild to moderate atopic dermatitis for patients aged two years and over in whom the use of conventional therapies is inadvisable. Pimecrolimus is an inflammatory cytokine inhibitor that works by selectively targeting T-cells in the skin. It inhibits in vitro the production and release of pro-inflammatory cytokines after antigen-specific or non-specific stimulation in T cells and mast cells. Pimecrolimus binds specifically to cytosolic receptor macrophilin-12 at nanomolar concentrations leading to inhibition of the Ca2+/calmodulin-dependent phosphatase, calcineurin. Pimecrolimus is a chlorine derivative of the known FK-520, from which it can be synthesized. In a pig model of dinitrofluorobenzene-induced allergic contact dermatitis, pimecrolimus was shown to inhibit erythema and induration, had equivalent efficacy compared to clobetasol-17- propionate, but did not cause atrophogenic effects. In a mouse model of allergic contact dermatitis, pimecrolimus given orally was as potent as tacrolimus and more effective than cyclosporin. The agent also decreased the intensity of cutaneous manifestations in an atopic dermatitis model involving hypomagnesemic hairless mice. Both in adults and in pediatric patients with atopic dermatitis, treatment with pimecrolimus has demonstrated greater efficiency than conventional treatment in reducing the incidence of disease flares, as well as the use of second-line corticosteroids. Moreover, in a 26 week study, in pediatric patients (2-17 years), from 65% of subjects showing improvement, 85% were cleared of the disease. Oral pimecrolimus administration resulted in an elimination half-life of about 30 to 40 h. It is not metabolized or degraded during skin permeation after topical administration. However, following oral administration, it is metabolized via the liver CYP3A4 pathway and excreted mainly in the feces. Pimecrolimus is well tolerated; no systemic accumulation is seen and the most commonly reported side effect is reaction at the site of application. Moreover, pimecrolimus did not cause skin atrophy in contrast to corticosteroids. At this time, as a replacement therapy for topical corticosteroids, the only competing agent for pimecrolimus is topical tacrolimus (ointment). Preliminary studies demonstrated comparable efficacy and safety between these two agents.

화학적 성질

White Solid


Novartis (USA)


Pimecrolimus is a semi-synthetic, macrocyclic lactone derived from ascomycin by activation of the 32-hydroxy group with a triflate ester, and nucleophilic substitution with chloride under phase transfer conditions to provide the chloro analogue. Pimecrolimus has been targeted for treatment of inflammatory skin disorders. Like all tacrolimus analogues, pimecrolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Pimecrolimus is extensively cited in the literature with over 2,000 citations.


Macrolactam ascomycin derivative; inhibits production of pro-inflammatory cytokines by T cells and mast cells. Immunosuppresant


Pimecrolimus caused a strong and dose-dependent inhibition of anti-IgE–induced release of histamine from mast cells and basophils (maximally 73% and 82%, respectively, at 500 nmol/L pimecrolimus) and of mast cell tryptase (maximally 75%) and a less pronou


Pimecrolimus (SDZ ASM 981, Elidel) is another recently approved macrolide immunosuppressant that acts by inhibiting calcineurin and blocking the release of proinflammatory cytokines from T lymphocytes. The parent compound, ascomycin, was originally isolated from Streptomyces hygroscopicus var ascomyceticus. Like tacrolimus, pimecrolimus is approved for the topical treatment of moderate to severe atopic dermatitis that is refractory to other therapies.Transient local irritation is a common side effect.


Elidel (Novartis);Elide1.

Veterinary Drugs and Treatments

A relatively new addition to the human topical armamentarium, pimecrolimus cream may be of benefit in veterinary patients in the adjunctive treatment of atopic dermatitis, discoid lupus erythematosus, pemphigus erythematosus or foliaceous, pinnal vascular disease, alopecia areata, vitiligo and for perianal fistulas (terminal phase or maintenance treatment after cyclosporine therapy). Unlike topical corticosteroids, tacrolimus or pimecrolimus do not have atrophogenic or metabolic effects associated with long-term or large area treatment.
Pimecrolimus acts similarly as cyclosporine and tacrolimus, namely inhibiting T-lymphocyte activation primarily by inhibiting the phosphatase activity of calcineurin. It also inhibits the release of inflammatory cytokines and mediators from mast cells and basophils. Pimecrolimus may not have identical mechanisms of action as tacrolimus, as it did not impair the primary immune response (as did tacrolimus) in mice after a contact sensitizer was applied. Both drugs did impair the secondary response however. Any clinical significance associated with this difference is not yet clear.

Pimecrolimus 준비 용품 및 원자재


준비 용품

Pimecrolimus 공급 업체

글로벌( 167)공급 업체
공급자 전화 팩스 이메일 국가 제품 수 이점
Henan Tianfu Chemical Co.,Ltd.
0371-55170693 CHINA 20672 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-34979012 CHINA 661 60
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 CHINA 24191 60
career henan chemical co
+86-371-86658258 CHINA 30001 58
Shanghai Arbor Chemical Co., Ltd.
021-60451683 CHINA 906 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 CHINA 306 58
Hubei Jusheng Technology Co.,Ltd.
027-59599243 CHINA 28236 58
Casorganics US Corp
+17326109938 CHINA 176 58
(323) 306-3136
(626) 453-0409 United States 8407 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114 CHINA 6372 58

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