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QuickView for Pimecrolimus (compound)


PubChem
Name: pimecrolimus
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
DrugBank
Identification
Name: pimecrolimus
Name (isomeric): DB00337
Drug Type: small molecule
Synonyms:
SDZ ASM 981; ASM 981
Brand: Elidel
Category: Enzyme Inhibitors, Immunosuppressive Agents, Dermatologic Agents
CAS number: 137071-32-0
Pharmacology
Indication: For treatment of mild to moderate atopic dermatitis.
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
Interactions
Drug interaction:
CladribinePimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as cladribine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
BleomycinPimecrolimus may enhance the adverse/toxic effect of immunosuppressants like bleomycin. This combination is contraindicated
ChlorambucilPimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as chlorambucil. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
CarmustinePimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as carmustine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
ClofarabinePimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as clofarabine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants.
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Targets