Name: | pimecrolimus |
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PubChem Compound ID: | 6447131 |
Molecular formula: | C43H68ClNO11 |
Molecular weight: | 810.453 g/mol |
Synonyms: |
137071-32-0; Pimecrolimus; 15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-((1E)-2-((1R,3R,4S)-4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,1; 33-epi-Chloro-33-desoxyascomycin; SDZ-ASM 981; Elidel; 15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-(2-(4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetrameth
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Name: | pimecrolimus |
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Name (isomeric): | DB00337 |
Drug Type: | small molecule |
Synonyms: |
SDZ ASM 981; ASM 981
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Brand: | Elidel |
Category: | Enzyme Inhibitors, Immunosuppressive Agents, Dermatologic Agents |
CAS number: | 137071-32-0 |
Indication: | For treatment of mild to moderate atopic dermatitis. |
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Pharmacology: |
Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotion...
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Mechanism of Action: |
Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleuki...
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Absorption: | Because of the low systemic absorption of pimecrolimus following topical application the calculation of standard pharmacokinetic measures such as AUC, Cmax, half-life, etc. cannot be reliably done. |
Protein binding: | 74%-87% (in vitro, bound to plasma proteins) |
Biotransformation: | No drug metabolism was observed in human skin in vitro. Oral administration yielded metabolites produced from O-demethylation and oxygenation reactions. |
Route of elimination: | 80% of the drug is excreted in the feces. |
Toxicity: | Side effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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