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Identification
NameSirolimus
Accession NumberDB00877  (APRD00178, DB02439)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionA macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. [PubChem]
Structure
Thumb
Synonyms
(-)-Rapamycin
Rapamycin
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gd-sirolimustablet5 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-sirolimussolution1.0 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-sirolimustablet1.0 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-sirolimustablet2 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
RapamuneCoated tablet0.5 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunesolution1 mg/mLoralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.1999-09-01Not applicableUs
Rapamunetablet5 mgoralPfizer Canada IncNot applicableNot applicableCanada
RapamuneCoated tablet2 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet, sugar coated1 mg/1oralCardinal Health2001-07-01Not applicableUs
RapamuneOral solution1 mg/mlOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet, sugar coated.5 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2010-03-01Not applicableUs
RapamuneCoated tablet2 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet1.0 mgoralPfizer Canada Inc2003-03-25Not applicableCanada
RapamuneCoated tablet1 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet, sugar coated1 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2001-07-01Not applicableUs
RapamuneCoated tablet0.5 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet2 mgoralPfizer Canada IncNot applicableNot applicableCanada
RapamuneCoated tablet1 mgOral usePfizer Limited2001-03-13Not applicableEu
Rapamunetablet, sugar coated2 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2001-07-01Not applicableUs
Rapamune Oral Solutionsolution1.0 mgoralPfizer Canada Inc2001-05-15Not applicableCanada
Sirolimustablet, sugar coated2 mg/1oralGreenstone LLC2014-10-27Not applicableUs
Sirolimustablet, sugar coated.5 mg/1oralGreenstone LLC2014-01-07Not applicableUs
Sirolimustablet, sugar coated1 mg/1oralGreenstone LLC2014-10-27Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sirolimustablet1 mg/1oralDr. Reddy's Laboratories Limited2014-10-27Not applicableUs
Sirolimustablet, film coated.5 mg/1oralAmerican Health Packaging2015-03-31Not applicableUs
Sirolimustablet2 mg/1oralDr. Reddy's Laboratories Limited2014-10-27Not applicableUs
Sirolimustablet, film coated.5 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-01-15Not applicableUs
Sirolimustablet, film coated.5 mg/1oralCadila Healthcare Limited2014-01-15Not applicableUs
Sirolimustablet1 mg/1oralAmerican Health Packaging2015-10-15Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIW36ZG6FT64
CAS number53123-88-9
WeightAverage: 914.1719
Monoisotopic: 913.555141619
Chemical FormulaC51H79NO13
InChI KeyInChIKey=QFJCIRLUMZQUOT-KLHQEZAJSA-N
InChI
InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33+,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1
IUPAC Name
(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2S)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0⁴,⁹]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
SMILES
[H][C@@]1(C[[email protected]](C)[C@]2([H])CC(=O)[[email protected]](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[[email protected]](C)C[[email protected]](C)\C=C\C=C\C=C(C)\[[email protected]](C[C@]3([H])CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O2)OC)CC[C@@H](O)[C@@H](C1)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
  • Macrolide
  • Alpha-amino acid ester
  • Cyclohexanol
  • Piperidine
  • Oxane
  • Tertiary carboxylic acid amide
  • Cyclic alcohol
  • Cyclic ketone
  • Tertiary amine
  • Secondary alcohol
  • Lactone
  • Lactam
  • Ketone
  • Hemiacetal
  • Carboxylic acid ester
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the prophylaxis of organ rejection in patients receiving renal transplants.
PharmacodynamicsSirolimus, a macrocyclic lactone produced by Streptomyces hygroscopicus, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.
Mechanism of actionSirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding92%
Metabolism
SubstrateEnzymesProduct
Sirolimus
41-O-demethylrapamycinDetails
Route of eliminationNot Available
Half life57-63 hours
ClearanceNot Available
ToxicityNot Available
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-0.7841
Blood Brain Barrier-0.9599
Caco-2 permeable-0.6341
P-glycoprotein substrateSubstrate0.8052
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IIInhibitor0.8021
Renal organic cation transporterNon-inhibitor0.8116
CYP450 2C9 substrateNon-substrate0.878
CYP450 2D6 substrateNon-substrate0.9138
CYP450 3A4 substrateSubstrate0.7776
CYP450 1A2 substrateNon-inhibitor0.9007
CYP450 2C9 inhibitorNon-inhibitor0.9125
CYP450 2D6 inhibitorNon-inhibitor0.9414
CYP450 2C19 inhibitorNon-inhibitor0.9158
CYP450 3A4 inhibitorNon-inhibitor0.9333
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9742
Ames testNon AMES toxic0.6617
CarcinogenicityNon-carcinogens0.9546
BiodegradationNot ready biodegradable0.9593
Rat acute toxicity2.8689 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9831
hERG inhibition (predictor II)Non-inhibitor0.8443
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Wyeth pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Coated tabletOral use0.5 mg
Coated tabletOral use1 mg
Coated tabletOral use2 mg
Oral solutionOral use1 mg/ml
Solutionoral1 mg/mL
Tabletoral1.0 mg
Tabletoral2 mg
Tabletoral5 mg
Tablet, sugar coatedoral.5 mg/1
Tablet, sugar coatedoral1 mg/1
Tablet, sugar coatedoral2 mg/1
Solutionoral1.0 mg
Tabletoral1 mg/1
Tabletoral2 mg/1
Tablet, film coatedoral.5 mg/1
Prices
Unit descriptionCostUnit
Rapamune 2 mg tablet20.59USD tablet
Rapamune 1 mg/ml Solution12.19USD ml
Rapamune 1 mg tablet11.95USD tablet
Rapamune 0.5 mg tablet5.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2103571 No2003-04-292012-02-21Canada
CA2293793 No2006-07-112018-06-11Canada
US5212155 No1993-05-182010-05-18Us
US5989591 Yes1998-09-112018-09-11Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00173 mg/mLALOGPS
logP4.85ALOGPS
logP7.45ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area195.43 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity250.66 m3·mol-1ChemAxon
Polarizability100.46 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Y. Chen, “One pot synthesis of tetrazole derivatives of sirolimus.” U.S. Patent US20080167335, issued July 10, 2008.

US20080167335
General References
  1. Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. [PubMed:15896681 ]
  2. Shuchman M: Trading restenosis for thrombosis? New questions about drug-eluting stents. N Engl J Med. 2006 Nov 9;355(19):1949-52. [PubMed:17093244 ]
  3. Sun SY, Rosenberg LM, Wang X, Zhou Z, Yue P, Fu H, Khuri FR: Activation of Akt and eIF4E survival pathways by rapamycin-mediated mammalian target of rapamycin inhibition. Cancer Res. 2005 Aug 15;65(16):7052-8. [PubMed:16103051 ]
  4. Chan S: Targeting the mammalian target of rapamycin (mTOR): a new approach to treating cancer. Br J Cancer. 2004 Oct 18;91(8):1420-4. [PubMed:15365568 ]
  5. Graziani EI: Recent advances in the chemistry, biosynthesis and pharmacology of rapamycin analogs. Nat Prod Rep. 2009 May;26(5):602-9. doi: 10.1039/b804602f. Epub 2009 Mar 5. [PubMed:19387497 ]
External Links
ATC CodesS01XA23L04AA10
AHFS Codes
  • 92:00.00
PDB Entries
FDA labelDownload (480 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Sirolimus.
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Sirolimus.
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Sirolimus.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Sirolimus.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Sirolimus.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be decreased when it is combined with Sirolimus.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Sirolimus.
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Sirolimus.
AldosteroneThe serum concentration of Aldosterone can be decreased when it is combined with Sirolimus.
AlitretinoinThe serum concentration of Alitretinoin can be decreased when it is combined with Sirolimus.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Sirolimus.
AmbrisentanThe serum concentration of Ambrisentan can be decreased when it is combined with Sirolimus.
AmiodaroneThe metabolism of Sirolimus can be decreased when combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be decreased when it is combined with Sirolimus.
AmlodipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Amlodipine.
Amphotericin BThe therapeutic efficacy of Amphotericin B can be decreased when used in combination with Sirolimus.
AmrinoneThe risk or severity of adverse effects can be increased when Sirolimus is combined with Amrinone.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Sirolimus.
AprepitantThe serum concentration of Sirolimus can be increased when it is combined with Aprepitant.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be decreased when it is combined with Sirolimus.
AtazanavirThe metabolism of Sirolimus can be decreased when combined with Atazanavir.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Sirolimus.
AtenololThe serum concentration of Atenolol can be decreased when it is combined with Sirolimus.
AtomoxetineThe metabolism of Sirolimus can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Sirolimus.
AzelnidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Azelnidipine.
AzimilideThe risk or severity of adverse effects can be increased when Sirolimus is combined with Azimilide.
BarnidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Barnidipine.
BenazeprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Benazepril.
BenidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Benidipine.
BepridilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be decreased when it is combined with Sirolimus.
BevacizumabBevacizumab may increase the cardiotoxic activities of Sirolimus.
BexaroteneThe serum concentration of Sirolimus can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Sirolimus can be increased when it is combined with Boceprevir.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Sirolimus.
BortezomibThe metabolism of Sirolimus can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Sirolimus can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Sirolimus.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Sirolimus.
BromocriptineThe serum concentration of Bromocriptine can be decreased when it is combined with Sirolimus.
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Sirolimus.
BuspironeThe metabolism of Buspirone can be decreased when combined with Sirolimus.
BusulfanThe serum concentration of Busulfan can be increased when it is combined with Sirolimus.
CabazitaxelThe serum concentration of Cabazitaxel can be decreased when it is combined with Sirolimus.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Sirolimus.
CaffeineThe serum concentration of Caffeine can be decreased when it is combined with Sirolimus.
CamptothecinThe serum concentration of Camptothecin can be decreased when it is combined with Sirolimus.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Sirolimus.
CandoxatrilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Candoxatril.
CaptoprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Captopril.
CarbamazepineThe metabolism of Sirolimus can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be decreased when it is combined with Sirolimus.
CarfilzomibThe serum concentration of Carfilzomib can be decreased when it is combined with Sirolimus.
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Sirolimus.
CeritinibThe serum concentration of Sirolimus can be increased when it is combined with Ceritinib.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Sirolimus.
CerivastatinThe serum concentration of Cerivastatin can be decreased when it is combined with Sirolimus.
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Sirolimus.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Sirolimus.
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Sirolimus.
CilazaprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Cilazapril.
CilnidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Cilnidipine.
CimetidineThe serum concentration of Cimetidine can be decreased when it is combined with Sirolimus.
CinnarizineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Cinnarizine.
CiprofloxacinThe serum concentration of Ciprofloxacin can be decreased when it is combined with Sirolimus.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Sirolimus.
CisplatinThe serum concentration of Cisplatin can be decreased when it is combined with Sirolimus.
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Sirolimus.
ClarithromycinThe metabolism of Sirolimus can be decreased when combined with Clarithromycin.
ClarithromycinThe serum concentration of Clarithromycin can be decreased when it is combined with Sirolimus.
ClemastineThe metabolism of Sirolimus can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be decreased when it is combined with Sirolimus.
ClomifeneThe serum concentration of Clomifene can be decreased when it is combined with Sirolimus.
ClonidineThe serum concentration of Clonidine can be decreased when it is combined with Sirolimus.
ClopidogrelThe serum concentration of Clopidogrel can be decreased when it is combined with Sirolimus.
ClotrimazoleThe serum concentration of Sirolimus can be increased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Clozapine.
CobicistatThe metabolism of Sirolimus can be decreased when combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be decreased when it is combined with Sirolimus.
ColchicineThe serum concentration of Colchicine can be decreased when it is combined with Sirolimus.
ConivaptanThe serum concentration of Sirolimus can be increased when it is combined with Conivaptan.
ConivaptanThe metabolism of Conivaptan can be decreased when combined with Sirolimus.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Sirolimus.
CrizotinibThe serum concentration of Sirolimus can be increased when it is combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Sirolimus.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Sirolimus.
CyclosporineThe metabolism of Sirolimus can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Sirolimus.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Sirolimus.
DabrafenibThe serum concentration of Sirolimus can be decreased when it is combined with Dabrafenib.
DactinomycinThe serum concentration of Dactinomycin can be decreased when it is combined with Sirolimus.
DapagliflozinThe serum concentration of Dapagliflozin can be decreased when it is combined with Sirolimus.
DarodipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Darodipine.
DarunavirThe metabolism of Sirolimus can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Sirolimus can be increased when it is combined with Dasatinib.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Sirolimus.
DaunorubicinThe serum concentration of Daunorubicin can be decreased when it is combined with Sirolimus.
DebrisoquinThe serum concentration of Debrisoquin can be decreased when it is combined with Sirolimus.
DeferasiroxThe serum concentration of Sirolimus can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Sirolimus can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Sirolimus.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Sirolimus.
DexamethasoneThe serum concentration of Sirolimus can be decreased when it is combined with Dexamethasone.
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Sirolimus.
DidanosineDidanosine can cause a decrease in the absorption of Sirolimus resulting in a reduced serum concentration and potentially a decrease in efficacy.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Sirolimus.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Sirolimus.
DigitoxinThe serum concentration of Digitoxin can be decreased when it is combined with Sirolimus.
DigoxinDigoxin may decrease the cardiotoxic activities of Sirolimus.
DigoxinThe serum concentration of Digoxin can be decreased when it is combined with Sirolimus.
DihydroergotamineThe metabolism of Sirolimus can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be decreased when it is combined with Sirolimus.
DiltiazemThe metabolism of Sirolimus can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be decreased when it is combined with Sirolimus.
DipyridamoleThe serum concentration of Dipyridamole can be decreased when it is combined with Sirolimus.
DocetaxelThe serum concentration of Docetaxel can be decreased when it is combined with Sirolimus.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Sirolimus.
DofetilideThe metabolism of Dofetilide can be decreased when combined with Sirolimus.
DomperidoneThe serum concentration of Domperidone can be decreased when it is combined with Sirolimus.
DotarizineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Dotarizine.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Sirolimus.
DoxycyclineThe metabolism of Sirolimus can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Sirolimus can be decreased when combined with Dronedarone.
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Sirolimus.
EdoxabanThe serum concentration of Edoxaban can be decreased when it is combined with Sirolimus.
EfavirenzThe serum concentration of Sirolimus can be decreased when it is combined with Efavirenz.
EfonidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Efonidipine.
EletriptanThe serum concentration of Eletriptan can be decreased when it is combined with Sirolimus.
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Sirolimus.
EnalaprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Sirolimus is combined with Enalaprilat.
EnzalutamideThe serum concentration of Sirolimus can be decreased when it is combined with Enzalutamide.
EperisoneThe risk or severity of adverse effects can be increased when Sirolimus is combined with Eperisone.
EpinastineThe serum concentration of Epinastine can be decreased when it is combined with Sirolimus.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Sirolimus.
ErythromycinThe metabolism of Sirolimus can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be decreased when it is combined with Sirolimus.
Eslicarbazepine acetateThe serum concentration of Sirolimus can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Sirolimus.
EstriolThe serum concentration of Estriol can be decreased when it is combined with Sirolimus.
EstroneThe serum concentration of Estrone can be decreased when it is combined with Sirolimus.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Sirolimus.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Sirolimus.
EtravirineThe serum concentration of Etravirine can be increased when it is combined with Sirolimus.
EtravirineThe serum concentration of Sirolimus can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Sirolimus.
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Sirolimus.
EzetimibeThe serum concentration of Ezetimibe can be decreased when it is combined with Sirolimus.
FelodipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Felodipine.
FendilineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Fendiline.
FesoterodineThe serum concentration of Fesoterodine can be decreased when it is combined with Sirolimus.
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Sirolimus.
FidaxomicinThe serum concentration of Fidaxomicin can be decreased when it is combined with Sirolimus.
FingolimodSirolimus may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe metabolism of Sirolimus can be decreased when combined with Fluconazole.
FlunarizineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Flunarizine.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be decreased when it is combined with Sirolimus.
FluvoxamineThe metabolism of Sirolimus can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Sirolimus can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Sirolimus can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Fosinopril.
FosphenytoinThe serum concentration of Sirolimus can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Sirolimus can be increased when it is combined with Fusidic Acid.
GabapentinThe risk or severity of adverse effects can be increased when Sirolimus is combined with Gabapentin.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Sirolimus.
GemcitabineThe serum concentration of Gemcitabine can be decreased when it is combined with Sirolimus.
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Sirolimus.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Sirolimus.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Sirolimus.
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Sirolimus.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Sirolimus.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Sirolimus.
GrazoprevirThe serum concentration of Grazoprevir can be decreased when it is combined with Sirolimus.
GrepafloxacinThe serum concentration of Grepafloxacin can be decreased when it is combined with Sirolimus.
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Sirolimus.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Sirolimus.
IbuprofenThe serum concentration of Ibuprofen can be decreased when it is combined with Sirolimus.
IdelalisibThe serum concentration of Sirolimus can be increased when it is combined with Idelalisib.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Sirolimus.
ImatinibThe metabolism of Sirolimus can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Sirolimus.
ImipramineThe serum concentration of Imipramine can be decreased when it is combined with Sirolimus.
IndacaterolThe serum concentration of Indacaterol can be decreased when it is combined with Sirolimus.
IndinavirThe metabolism of Sirolimus can be decreased when combined with Indinavir.
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Sirolimus.
IndomethacinThe serum concentration of Indomethacin can be decreased when it is combined with Sirolimus.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Sirolimus.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Sirolimus.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Sirolimus.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Sirolimus.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Sirolimus.
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Sirolimus.
IrinotecanThe serum concentration of Irinotecan can be decreased when it is combined with Sirolimus.
IsavuconazoniumThe metabolism of Sirolimus can be decreased when combined with Isavuconazonium.
IsradipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Isradipine.
IsradipineThe metabolism of Sirolimus can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Sirolimus can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Sirolimus can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be decreased when it is combined with Sirolimus.
KetazolamThe serum concentration of Ketazolam can be decreased when it is combined with Sirolimus.
KetoconazoleThe serum concentration of Sirolimus can be increased when it is combined with Ketoconazole.
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Sirolimus.
LacidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Lacidipine.
LamivudineThe serum concentration of Lamivudine can be decreased when it is combined with Sirolimus.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Sirolimus.
LansoprazoleThe serum concentration of Lansoprazole can be decreased when it is combined with Sirolimus.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Sirolimus.
LeflunomideThe risk or severity of adverse effects can be increased when Sirolimus is combined with Leflunomide.
LenalidomideThe serum concentration of Lenalidomide can be decreased when it is combined with Sirolimus.
LenvatinibThe serum concentration of Lenvatinib can be decreased when it is combined with Sirolimus.
LercanidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Lercanidipine.
LevetiracetamThe serum concentration of Levetiracetam can be decreased when it is combined with Sirolimus.
LevofloxacinThe serum concentration of Levofloxacin can be decreased when it is combined with Sirolimus.
LevomilnacipranThe serum concentration of Levomilnacipran can be decreased when it is combined with Sirolimus.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Sirolimus.
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Sirolimus.
LisinoprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Lisinopril.
LoperamideThe serum concentration of Loperamide can be decreased when it is combined with Sirolimus.
LopinavirThe metabolism of Sirolimus can be decreased when combined with Lopinavir.
LosartanThe metabolism of Losartan can be decreased when combined with Sirolimus.
LovastatinThe metabolism of Sirolimus can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Sirolimus can be increased when it is combined with Luliconazole.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Sirolimus is combined with Magnesium Sulfate.
ManidipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Manidipine.
MannitolThe serum concentration of Mannitol can be decreased when it is combined with Sirolimus.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Sirolimus.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Sirolimus.
MethotrexateThe serum concentration of Methotrexate can be decreased when it is combined with Sirolimus.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Sirolimus.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Sirolimus.
MibefradilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Mibefradil.
MidazolamThe serum concentration of Midazolam can be decreased when it is combined with Sirolimus.
MifepristoneThe serum concentration of Sirolimus can be increased when it is combined with Mifepristone.
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Sirolimus.
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Sirolimus.
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Sirolimus.
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Sirolimus.
MitotaneThe serum concentration of Sirolimus can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be decreased when it is combined with Sirolimus.
ModafinilThe serum concentration of Sirolimus can be decreased when it is combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Moexipril.
MorphineThe serum concentration of Morphine can be decreased when it is combined with Sirolimus.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Sirolimus.
NadololThe serum concentration of Nadolol can be decreased when it is combined with Sirolimus.
NafcillinThe serum concentration of Sirolimus can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Sirolimus.
NaloxoneThe serum concentration of Naloxone can be decreased when it is combined with Sirolimus.
NatalizumabThe risk or severity of adverse effects can be increased when Sirolimus is combined with Natalizumab.
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Sirolimus.
NefazodoneThe metabolism of Sirolimus can be decreased when combined with Nefazodone.
NelfinavirThe serum concentration of Sirolimus can be increased when it is combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Sirolimus.
NetupitantThe serum concentration of Sirolimus can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Sirolimus can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Sirolimus.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Sirolimus.
NiguldipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Niguldipine.
NilotinibThe metabolism of Sirolimus can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Sirolimus.
NiludipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Niludipine.
NilvadipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Nilvadipine.
NimesulideThe risk or severity of adverse effects can be increased when Sirolimus is combined with Nimesulide.
NimodipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Nimodipine.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Sirolimus.
NisoldipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Nisoldipine.
NitrendipineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Nitrendipine.
NizatidineThe serum concentration of Nizatidine can be decreased when it is combined with Sirolimus.
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Sirolimus.
OlaparibThe metabolism of Sirolimus can be decreased when combined with Olaparib.
OmapatrilatThe risk or severity of adverse effects can be increased when Sirolimus is combined with Omapatrilat.
OmbitasvirThe serum concentration of Ombitasvir can be decreased when it is combined with Sirolimus.
OsimertinibThe serum concentration of Sirolimus can be increased when it is combined with Osimertinib.
OsimertinibThe serum concentration of Osimertinib can be decreased when it is combined with Sirolimus.
OuabainOuabain may decrease the cardiotoxic activities of Sirolimus.
PaclitaxelThe serum concentration of Paclitaxel can be decreased when it is combined with Sirolimus.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Sirolimus.
PalbociclibThe serum concentration of Sirolimus can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Sirolimus.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Sirolimus.
PentobarbitalThe metabolism of Sirolimus can be increased when combined with Pentobarbital.
PerhexilineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Perhexiline.
PerindoprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Perindopril.
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Sirolimus.
PhenobarbitalThe metabolism of Sirolimus can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be decreased when it is combined with Sirolimus.
PhenytoinThe serum concentration of Sirolimus can be decreased when it is combined with Phenytoin.
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Sirolimus.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sirolimus.
PimozideSirolimus may increase the arrhythmogenic activities of Pimozide.
PinaveriumThe risk or severity of adverse effects can be increased when Sirolimus is combined with Pinaverium.
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Sirolimus.
PitavastatinThe serum concentration of Pitavastatin can be decreased when it is combined with Sirolimus.
PomalidomideThe serum concentration of Pomalidomide can be decreased when it is combined with Sirolimus.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Sirolimus.
PosaconazoleThe serum concentration of Sirolimus can be increased when it is combined with Posaconazole.
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Sirolimus.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Sirolimus.
PrazosinThe serum concentration of Prazosin can be decreased when it is combined with Sirolimus.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Sirolimus.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Sirolimus.
PregabalinThe risk or severity of adverse effects can be increased when Sirolimus is combined with Pregabalin.
PrenylamineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Prenylamine.
PrimidoneThe metabolism of Sirolimus can be increased when combined with Primidone.
ProgesteroneThe therapeutic efficacy of Progesterone can be decreased when used in combination with Sirolimus.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Sirolimus.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Sirolimus.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Sirolimus.
QuinaprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Quinapril.
QuinidineThe metabolism of Quinidine can be decreased when combined with Sirolimus.
QuinineThe serum concentration of Quinine can be decreased when it is combined with Sirolimus.
Rabies vaccineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Rabies vaccine.
RamiprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Ramipril.
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Sirolimus.
RanolazineThe metabolism of Ranolazine can be decreased when combined with Sirolimus.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Sirolimus.
RescinnamineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Rescinnamine.
ReserpineThe serum concentration of Reserpine can be decreased when it is combined with Sirolimus.
RifabutinThe metabolism of Sirolimus can be increased when combined with Rifabutin.
RifampicinThe metabolism of Sirolimus can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be decreased when it is combined with Sirolimus.
RifapentineThe metabolism of Sirolimus can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Sirolimus.
RisedronateThe risk or severity of adverse effects can be increased when Sirolimus is combined with Risedronate.
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Sirolimus.
RitonavirThe metabolism of Sirolimus can be decreased when combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Sirolimus.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Sirolimus.
RoflumilastRoflumilast may increase the immunosuppressive activities of Sirolimus.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Sirolimus.
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Sirolimus.
Salicylic acidThe serum concentration of Salicylic acid can be decreased when it is combined with Sirolimus.
SaquinavirThe metabolism of Sirolimus can be decreased when combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Sirolimus.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Sirolimus.
SelexipagThe serum concentration of Selexipag can be decreased when it is combined with Sirolimus.
SildenafilThe metabolism of Sirolimus can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Sirolimus.
SiltuximabThe serum concentration of Sirolimus can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Sirolimus can be increased when it is combined with Simeprevir.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Sirolimus.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Sirolimus.
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Sirolimus.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Sirolimus.
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Sirolimus.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Sirolimus.
SparfloxacinThe serum concentration of Sparfloxacin can be decreased when it is combined with Sirolimus.
SphingosineThe serum concentration of Sphingosine can be decreased when it is combined with Sirolimus.
SpiraprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Spirapril.
St. John's WortThe serum concentration of Sirolimus can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Sirolimus can be increased when it is combined with Stiripentol.
SucralfateSucralfate can cause a decrease in the absorption of Sirolimus resulting in a reduced serum concentration and potentially a decrease in efficacy.
SulfisoxazoleThe metabolism of Sirolimus can be decreased when combined with Sulfisoxazole.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Sirolimus.
SunitinibThe metabolism of Sunitinib can be decreased when combined with Sirolimus.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sirolimus.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Sirolimus.
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Sirolimus.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be decreased when it is combined with Sirolimus.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Sirolimus.
TelaprevirThe serum concentration of Sirolimus can be increased when it is combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Sirolimus.
TelithromycinThe metabolism of Sirolimus can be decreased when combined with Telithromycin.
TemocaprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Temocapril.
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Sirolimus.
TicagrelorThe serum concentration of Ticagrelor can be decreased when it is combined with Sirolimus.
TiclopidineThe metabolism of Sirolimus can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be decreased when it is combined with Sirolimus.
TocilizumabThe serum concentration of Sirolimus can be decreased when it is combined with Tocilizumab.
TofacitinibSirolimus may increase the immunosuppressive activities of Tofacitinib.
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Sirolimus.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Sirolimus.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Sirolimus is combined with Tolfenamic Acid.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Sirolimus.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Sirolimus.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Sirolimus.
TrandolaprilThe risk or severity of adverse effects can be increased when Sirolimus is combined with Trandolapril.
TranilastThe risk or severity of adverse effects can be increased when Sirolimus is combined with Tranilast.
TrastuzumabTrastuzumab may increase the neutropenic activities of Sirolimus.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Sirolimus.
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Sirolimus.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Sirolimus.
UmeclidiniumThe serum concentration of Umeclidinium can be decreased when it is combined with Sirolimus.
VecuroniumThe serum concentration of Vecuronium can be decreased when it is combined with Sirolimus.
VenlafaxineThe metabolism of Sirolimus can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be decreased when it is combined with Sirolimus.
VerapamilThe metabolism of Sirolimus can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be decreased when it is combined with Sirolimus.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Sirolimus.
VinblastineThe serum concentration of Vinblastine can be decreased when it is combined with Sirolimus.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Sirolimus.
VismodegibThe serum concentration of Vismodegib can be decreased when it is combined with Sirolimus.
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Sirolimus.
VoriconazoleThe serum concentration of Sirolimus can be increased when it is combined with Voriconazole.
XylometazolineThe risk or severity of adverse effects can be increased when Sirolimus is combined with Xylometazoline.
ZiconotideThe risk or severity of adverse effects can be increased when Sirolimus is combined with Ziconotide.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Sirolimus.
ZiprasidoneThe metabolism of Sirolimus can be decreased when combined with Ziprasidone.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Sirolimus.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. Dowling RJ, Topisirovic I, Fonseca BD, Sonenberg N: Dissecting the role of mTOR: lessons from mTOR inhibitors. Biochim Biophys Acta. 2010 Mar;1804(3):433-9. doi: 10.1016/j.bbapap.2009.12.001. Epub 2009 Dec 11. [PubMed:20005306 ]
  2. Shuuin T, Karashima H: [Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma]. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9. [PubMed:19620795 ]
  3. Sehgal SN: Sirolimus: its discovery, biological properties, and mechanism of action. Transplant Proc. 2003 May;35(3 Suppl):7S-14S. [PubMed:12742462 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
other
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Sehgal SN: Sirolimus: its discovery, biological properties, and mechanism of action. Transplant Proc. 2003 May;35(3 Suppl):7S-14S. [PubMed:12742462 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
other/unknown
General Function:
Ligand-dependent nuclear receptor transcription coactivator activity
Specific Function:
Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name:
FGF2
Uniprot ID:
P09038
Molecular Weight:
30769.715 Da
References
  1. Sehgal SN: Sirolimus: its discovery, biological properties, and mechanism of action. Transplant Proc. 2003 May;35(3 Suppl):7S-14S. [PubMed:12742462 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [PubMed:10490933 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764 ]
  2. Wacher VJ, Silverman JA, Wong S, Tran-Tau P, Chan AO, Chai A, Yu XQ, O'Mahony D, Ramtoola Z: Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate. J Pharmacol Exp Ther. 2002 Oct;303(1):308-13. [PubMed:12235265 ]
  3. Arceci RJ, Stieglitz K, Bierer BE: Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype. Blood. 1992 Sep 15;80(6):1528-36. [PubMed:1381629 ]
  4. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Fehrenbach T, Cui Y, Faulstich H, Keppler D: Characterization of the transport of the bicyclic peptide phalloidin by human hepatic transport proteins. Naunyn Schmiedebergs Arch Pharmacol. 2003 Nov;368(5):415-20. Epub 2003 Oct 3. [PubMed:14530907 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Monovalent cation:proton antiporter activity
Specific Function:
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acyclovir, ganciclovir and also the zwitterionic cephalosporin, cephalexin and cephradin. Seems to also play a role in the uptake of oxaliplatin (a new platinum anticancer agent). Able to transport...
Gene Name:
SLC47A1
Uniprot ID:
Q96FL8
Molecular Weight:
61921.585 Da
References
  1. Meyer zu Schwabedissen HE, Verstuyft C, Kroemer HK, Becquemont L, Kim RB: Human multidrug and toxin extrusion 1 (MATE1/SLC47A1) transporter: functional characterization, interaction with OCT2 (SLC22A2), and single nucleotide polymorphisms. Am J Physiol Renal Physiol. 2010 Apr;298(4):F997-F1005. doi: 10.1152/ajprenal.00431.2009. Epub 2010 Jan 6. [PubMed:20053795 ]
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Drug created on June 13, 2005 07:24 / Updated on September 27, 2016 03:40