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Identification
NamePimecrolimus
Accession NumberDB00337  (APRD01182)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). It is currently available as a topical cream, once marketed by Novartis, (however Galderma will be promoting the molecule in Canada in early 2007) under the trade name Elidel. [Wikipedia]

Structure
Thumb
Synonyms
33-Epi-chloro-33-desoxyascomycin
Pimecrolimus
Pimecrolimusum
External Identifiers
  • ASM 981
  • SDZ ASM 981
  • SDZ ASM-981
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Elidelcream10 mg/gtopicalValeant Pharmaceuticals North America LLC2001-12-02Not applicableUs
Elidelcream1 %topicalValeant Canada Lp Valeant Canada S.E.C.2003-03-24Not applicableCanada
Elidelcream10 mg/gtopicalPhysicians Total Care, Inc.2003-10-30Not applicableUs
Elidelcream10 mg/gtopicalValeant Pharmaceuticals North America LLC2001-12-02Not applicableUs
Elidelcream10 mg/gtopicalValeant Pharmaceuticals North America LLC2001-12-02Not applicableUs
Elidelcream10 mg/gtopicalValeant Pharmaceuticals North America LLC2001-12-02Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AregenMeda Pharm
RizanEsteve
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7KYV510875
CAS number137071-32-0
WeightAverage: 810.46
Monoisotopic: 809.4480897
Chemical FormulaC43H68ClNO11
InChI KeyKASDHRXLYQOAKZ-XDSKOBMDSA-N
InChI
InChI=1S/C43H68ClNO11/c1-10-30-18-24(2)17-25(3)19-36(53-8)39-37(54-9)21-27(5)43(51,56-39)40(48)41(49)45-16-12-11-13-32(45)42(50)55-38(28(6)33(46)23-34(30)47)26(4)20-29-14-15-31(44)35(22-29)52-7/h18,20,25,27-33,35-39,46,51H,10-17,19,21-23H2,1-9H3/b24-18+,26-20+/t25-,27+,28+,29-,30+,31-,32-,33-,35+,36-,37-,38+,39+,43+/m0/s1
IUPAC Name
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-12-[(1E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0⁴,⁹]octacos-18-ene-2,3,10,16-tetrone
SMILES
[H][C@]1(CC[[email protected]](Cl)[C@@H](C1)OC)\C=C(/C)[C@@]1([H])OC(=O)[C@]2([H])CCCCN2C(=O)C(=O)[C@]2(O)O[C@@]([H])([[email protected]](C[[email protected]]2C)OC)[[email protected]](C[C@@H](C)C\C(C)=C\[C@@H](CC)C(=O)C[[email protected]](O)[[email protected]]1C)OC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as macrolide lactams. These are cyclic polyketides containing both a cyclic amide and a cyclic ester group.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassMacrolide lactams
Sub ClassNot Available
Direct ParentMacrolide lactams
Alternative Parents
Substituents
  • Macrolide lactam
  • Alpha-amino acid ester
  • Macrolide
  • Alpha-amino acid or derivatives
  • Cyclohexyl halide
  • Oxane
  • Piperidine
  • Tertiary carboxylic acid amide
  • Carboxamide group
  • Carboxylic acid ester
  • Hemiacetal
  • Ketone
  • Lactam
  • Lactone
  • Secondary alcohol
  • Cyclic ketone
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Azacycle
  • Oxacycle
  • Carboxylic acid derivative
  • Dialkyl ether
  • Ether
  • Alcohol
  • Alkyl chloride
  • Alkyl halide
  • Organic nitrogen compound
  • Organic oxygen compound
  • Organochloride
  • Organonitrogen compound
  • Organooxygen compound
  • Organic oxide
  • Hydrocarbon derivative
  • Carbonyl group
  • Organohalogen compound
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of mild to moderate atopic dermatitis.
PharmacodynamicsPimecrolimus 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 emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation.
Mechanism of actionPimecrolimus 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 Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. Also, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/lgE.
Related Articles
AbsorptionBecause 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.
Volume of distributionNot Available
Protein binding74%-87% (in vitro, bound to plasma proteins)
Metabolism

No drug metabolism was observed in human skin in vitro. Oral administration yielded metabolites produced from O-demethylation and oxygenation reactions.

Route of elimination80% of the drug is excreted in the feces.
Half lifeNot Available
ClearanceNot Available
ToxicitySide effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.6208
Blood Brain Barrier-0.9554
Caco-2 permeable-0.5764
P-glycoprotein substrateSubstrate0.8064
P-glycoprotein inhibitor IInhibitor0.8064
P-glycoprotein inhibitor IIInhibitor0.7014
Renal organic cation transporterNon-inhibitor0.8556
CYP450 2C9 substrateNon-substrate0.9117
CYP450 2D6 substrateNon-substrate0.8856
CYP450 3A4 substrateSubstrate0.7519
CYP450 1A2 substrateNon-inhibitor0.8678
CYP450 2C9 inhibitorNon-inhibitor0.8671
CYP450 2D6 inhibitorNon-inhibitor0.9026
CYP450 2C19 inhibitorNon-inhibitor0.8248
CYP450 3A4 inhibitorNon-inhibitor0.8672
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9326
Ames testNon AMES toxic0.6495
CarcinogenicityNon-carcinogens0.9183
BiodegradationNot ready biodegradable0.9937
Rat acute toxicity2.6919 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9787
hERG inhibition (predictor II)Non-inhibitor0.6886
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Creamtopical1 %
Creamtopical10 mg/g
Prices
Unit descriptionCostUnit
Elidel 100 Gram Tube 1% 100 gm Tube315.76USD tube
Elidel 60 Gram Tube 1% 60 gm Tube200.05USD tube
Elidel 30 Gram Tube 1% 30 gm Tube101.44USD tube
Elidel 1% cream3.21USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2200966 No2006-12-192015-10-26Canada
US5912238 Yes1996-12-152016-12-15Us
US6352998 Yes1996-04-262016-04-26Us
US6423722 Yes1998-12-262018-12-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00152 mg/mLALOGPS
logP4.36ALOGPS
logP6.81ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area158.13 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity214.03 m3·mol-1ChemAxon
Polarizability87.79 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Viktor Gyollai, Csaba Szabo, “Methods of preparing pimecrolimus.” U.S. Patent US20060142564, issued June 29, 2006.

US20060142564
General References
  1. Grassberger M, Baumruker T, Enz A, Hiestand P, Hultsch T, Kalthoff F, Schuler W, Schulz M, Werner FJ, Winiski A, Wolff B, Zenke G: A novel anti-inflammatory drug, SDZ ASM 981, for the treatment of skin diseases: in vitro pharmacology. Br J Dermatol. 1999 Aug;141(2):264-73. [PubMed:10468798 ]
External Links
ATC CodesD11AH02
AHFS Codes
  • 84:92.00
PDB EntriesNot Available
FDA labelDownload (230 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbataceptThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Abatacept.
AdalimumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Adalimumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Alemtuzumab.
AltretamineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Altretamine.
AmsacrineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Amsacrine.
AnakinraThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Anakinra.
Anti-thymocyte Globulin (Rabbit)The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Anti-thymocyte Globulin (Rabbit).
AprepitantThe metabolism of Pimecrolimus can be decreased when combined with Aprepitant.
AtazanavirThe metabolism of Pimecrolimus can be decreased when combined with Atazanavir.
AzacitidineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Azacitidine.
AzathioprineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Azathioprine.
BasilThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Basil.
BasiliximabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Basiliximab.
BelataceptThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Belatacept.
BelimumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Belimumab.
BetamethasoneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Betamethasone.
BleomycinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Bleomycin.
BlinatumomabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Blinatumomab.
BoceprevirThe metabolism of Pimecrolimus can be decreased when combined with Boceprevir.
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Brentuximab vedotin.
BudesonideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Budesonide.
BusulfanThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Busulfan.
CabazitaxelThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cabazitaxel.
CanakinumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Canakinumab.
CapecitabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Capecitabine.
CarboplatinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Carboplatin.
CarmustineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Carmustine.
CeritinibThe metabolism of Pimecrolimus can be decreased when combined with Ceritinib.
Certolizumab pegolThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Certolizumab pegol.
ChlorambucilThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Chlorambucil.
CisplatinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cisplatin.
CladribineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cladribine.
ClarithromycinThe metabolism of Pimecrolimus can be decreased when combined with Clarithromycin.
ClofarabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Clofarabine.
CobicistatThe metabolism of Pimecrolimus can be decreased when combined with Cobicistat.
ConivaptanThe metabolism of Pimecrolimus can be decreased when combined with Conivaptan.
CorticotropinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Corticotropin.
Cortisone acetateThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cortisone acetate.
CrizotinibThe metabolism of Pimecrolimus can be decreased when combined with Crizotinib.
CyclophosphamideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cyclophosphamide.
CyclosporineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cyclosporine.
CytarabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cytarabine.
DacarbazineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dacarbazine.
DactinomycinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dactinomycin.
DarunavirThe metabolism of Pimecrolimus can be decreased when combined with Darunavir.
DasatinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dasatinib.
DaunorubicinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Daunorubicin.
DelavirdineThe metabolism of Pimecrolimus can be decreased when combined with Delavirdine.
DexamethasoneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dexamethasone.
DiltiazemThe metabolism of Pimecrolimus can be decreased when combined with Diltiazem.
DinutuximabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dinutuximab.
DocetaxelThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Docetaxel.
DoxorubicinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Doxorubicin.
DronedaroneThe metabolism of Pimecrolimus can be decreased when combined with Dronedarone.
EculizumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Eculizumab.
EpirubicinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Epirubicin.
ErythromycinThe metabolism of Pimecrolimus can be decreased when combined with Erythromycin.
EstramustineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Estramustine.
EtanerceptThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Etanercept.
EtoposideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Etoposide.
EverolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Everolimus.
FingolimodThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fingolimod.
FloxuridineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Floxuridine.
FluconazoleThe metabolism of Pimecrolimus can be decreased when combined with Fluconazole.
FludarabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fludarabine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fludrocortisone.
FluorouracilThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fluorouracil.
FosamprenavirThe metabolism of Pimecrolimus can be decreased when combined with Fosamprenavir.
GemcitabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Gemcitabine.
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Gemtuzumab ozogamicin.
Glatiramer AcetateThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Glatiramer Acetate.
golimumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with golimumab.
HydrocortisoneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Hydrocortisone.
HydroxyureaThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Hydroxyurea.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ibrutinib.
IdarubicinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Idarubicin.
IdelalisibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Idelalisib.
IfosfamideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ifosfamide.
ImatinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Imatinib.
ImiquimodThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Imiquimod.
IndinavirThe metabolism of Pimecrolimus can be decreased when combined with Indinavir.
InfliximabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Infliximab.
IrinotecanThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Irinotecan.
IsavuconazoniumThe metabolism of Pimecrolimus can be decreased when combined with Isavuconazonium.
ItraconazoleThe metabolism of Pimecrolimus can be decreased when combined with Itraconazole.
KetoconazoleThe metabolism of Pimecrolimus can be decreased when combined with Ketoconazole.
L-PhenylalanineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with L-Phenylalanine.
LeflunomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Leflunomide.
LenalidomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Lenalidomide.
LomustineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Lomustine.
MechlorethamineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mechlorethamine.
MelphalanThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Melphalan.
MercaptopurineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mercaptopurine.
MethotrexateThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Methotrexate.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Methylprednisolone.
MifepristoneThe metabolism of Pimecrolimus can be decreased when combined with Mifepristone.
MitomycinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mitomycin.
MitoxantroneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mitoxantrone.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mycophenolate mofetil.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Mycophenolic acid.
NatalizumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Natalizumab.
NefazodoneThe metabolism of Pimecrolimus can be decreased when combined with Nefazodone.
NelarabineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Nelarabine.
NelfinavirThe metabolism of Pimecrolimus can be decreased when combined with Nelfinavir.
NilotinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Nilotinib.
ObinutuzumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Obinutuzumab.
OsimertinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Osimertinib.
OxaliplatinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Oxaliplatin.
PaclitaxelThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Paclitaxel.
PalbociclibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Palbociclib.
PanobinostatThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Panobinostat.
PazopanibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pazopanib.
PegaspargaseThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pegaspargase.
PemetrexedThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pemetrexed.
PentostatinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pentostatin.
PomalidomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pomalidomide.
PosaconazoleThe metabolism of Pimecrolimus can be decreased when combined with Posaconazole.
PralatrexateThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pralatrexate.
PrednisoloneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Prednisolone.
PrednisoneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Prednisone.
ProcarbazineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Procarbazine.
Repository corticotropinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Repository corticotropin.
RilonaceptThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Rilonacept.
RitonavirThe metabolism of Pimecrolimus can be decreased when combined with Ritonavir.
RituximabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Rituximab.
RuxolitinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ruxolitinib.
SaquinavirThe metabolism of Pimecrolimus can be decreased when combined with Saquinavir.
SecukinumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Secukinumab.
SiltuximabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Siltuximab.
SirolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sirolimus.
SorafenibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sorafenib.
StreptozocinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Streptozocin.
SunitinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sunitinib.
TacrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tacrolimus.
TelaprevirThe metabolism of Pimecrolimus can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Pimecrolimus can be decreased when combined with Telithromycin.
TemozolomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Temozolomide.
TemsirolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Temsirolimus.
TeniposideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Teniposide.
TeriflunomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Teriflunomide.
ThalidomideThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Thalidomide.
ThiotepaThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Thiotepa.
TioguanineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tioguanine.
TocilizumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tocilizumab.
TofacitinibThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tofacitinib.
TopotecanThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Topotecan.
TositumomabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tositumomab.
TrabectedinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Trabectedin.
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with ado-trastuzumab emtansine.
TretinoinThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tretinoin.
TriamcinoloneThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Triamcinolone.
UstekinumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Ustekinumab.
VedolizumabThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vedolizumab.
VerapamilThe metabolism of Pimecrolimus can be decreased when combined with Verapamil.
VinblastineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vinblastine.
VincristineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vincristine.
VindesineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vindesine.
VinorelbineThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vinorelbine.
VoriconazoleThe metabolism of Pimecrolimus can be decreased when combined with Voriconazole.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Tfiiic-class transcription factor binding
Specific Function:
Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2). Activ...
Gene Name:
MTOR
Uniprot ID:
P42345
Molecular Weight:
288889.05 Da
References
  1. Reitamo S, Remitz A, Kyllonen H, Saarikko J: Topical noncorticosteroid immunomodulation in the treatment of atopic dermatitis. Am J Clin Dermatol. 2002;3(6):381-8. [PubMed:12113647 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
potentiator
General Function:
Type i transforming growth factor beta receptor binding
Specific Function:
Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand. Recruites SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. May modulate the RYR1 calcium channel activity. PPIases accelerate the folding of proteins....
Gene Name:
FKBP1A
Uniprot ID:
P62942
Molecular Weight:
11950.665 Da
References
  1. Reitamo S, Remitz A, Kyllonen H, Saarikko J: Topical noncorticosteroid immunomodulation in the treatment of atopic dermatitis. Am J Clin Dermatol. 2002;3(6):381-8. [PubMed:12113647 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zollinger M, Waldmeier F, Hartmann S, Zenke G, Zimmerlin AG, Glaenzel U, Baldeck JP, Schweitzer A, Berthier S, Moenius T, Grassberger MA: Pimecrolimus: absorption, distribution, metabolism, and excretion in healthy volunteers after a single oral dose and supplementary investigations in vitro. Drug Metab Dispos. 2006 May;34(5):765-74. Epub 2006 Feb 7. [PubMed:16467136 ]
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Drug created on June 13, 2005 07:24 / Updated on June 26, 2016 03:07