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Identification
NameRoflumilast
Accession NumberDB01656  (EXPT02802)
TypeSmall Molecule
GroupsApproved
Description

Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor. Due to its selective inhibition of the PDE4 isoenzyme in lung cells, roflumilast is indicated for the management of chronic obstrtuctive pulmonary disease (COPD) exacerbations. Treatment with Roflumilast is associated with an increase in psychiatric adverse reactions, including suicide and suicidal attempts.

Structure
Thumb
Synonyms
Daliresp
ROF
Roflumilastum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Daliresptablet500 ug/1oralAstra Zeneca Pharmaceuticals Lp2015-07-01Not applicableUs
Daliresptablet500 ug/1oralCardinal Health2011-02-28Not applicableUs
Daliresptablet500 ug/1oralForest Laboratories, Inc.2011-02-28Not applicableUs
Daxastablet500 mcgoralTakeda Canada Inc2010-12-30Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII0P6C6ZOP5U
CAS number162401-32-3
WeightAverage: 403.207
Monoisotopic: 402.034954148
Chemical FormulaC17H14Cl2F2N2O3
InChI KeyInChIKey=MNDBXUUTURYVHR-UHFFFAOYSA-N
InChI
InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24)
IUPAC Name
3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
SMILES
FC(F)OC1=C(OCC2CC2)C=C(C=C1)C(=O)NC1=C(Cl)C=NC=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylamides. These are organic compounds that contain a carboxamide group that is N-linked to a aryl group. They have the generic structure RC(=O)N(R')H, R = organyl group and R'= aryl group.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassN-arylamides
Sub ClassNot Available
Direct ParentN-arylamides
Alternative Parents
Substituents
  • N-arylamide
  • Benzoic acid or derivatives
  • Benzamide
  • Polyhalopyridine
  • Phenol ether
  • Benzoyl
  • Aminopyridine
  • Alkyl aryl ether
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Carboxylic acid derivative
  • Halomethane
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationRoflumilast is indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. Roflumilast is not a bronchodilator and is not indicated for the relief of acute bronchospasm.
PharmacodynamicsRoflumilast (and its active metabolite, roflumilast N-oxide) increases cyclic adenosine-3′, 5′-monophosphate (cAMP) in lung cells by inhibiting PDE4. Increased cAMP activates PKA, which inactivates transcription factors involved in inflammation. Romflumilast also decreases the amount of sputum neutrophils and eosinophils in COPD patients.
Mechanism of actionRoflumilast is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Roflumilast.
Related Articles
AbsorptionAfter a 500mcg dose, the bioavailability of roflumilast is about 80%. In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours. While in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged.
Volume of distribution

Roflumilast has a Vd of 2.9L/kg with a dose of 500mcg. Permeability of roflumilast across the blood-brain barrier appears to be poor in rat studies.

Protein bindingRoflumilast is 99% plasma protein bound.
Metabolism

Roflumilast is metabolized to roflumilast N-oxide, the active metabolite of roflumilast in humans, by CYP3A4 and CYP1A2.

SubstrateEnzymesProduct
Roflumilast
Not Available
Roflumilast N-oxideDetails
Route of eliminationRoflumilast is excreted 70% in the urine as roflumilast N-oxide.
Half lifePlasma half-life of roflumilast is 17 hours and its metabolite is 30 hours (oral dose).
Clearance

~9.6 L/hour.

ToxicityHeadache, weight loss, GI upset, insomnia, and loose stools.
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+1.0
Blood Brain Barrier+0.9874
Caco-2 permeable+0.5235
P-glycoprotein substrateNon-substrate0.7295
P-glycoprotein inhibitor INon-inhibitor0.5775
P-glycoprotein inhibitor IINon-inhibitor0.622
Renal organic cation transporterNon-inhibitor0.8057
CYP450 2C9 substrateNon-substrate0.8082
CYP450 2D6 substrateNon-substrate0.7705
CYP450 3A4 substrateSubstrate0.5821
CYP450 1A2 substrateInhibitor0.7732
CYP450 2C9 inhibitorInhibitor0.5686
CYP450 2D6 inhibitorNon-inhibitor0.7204
CYP450 2C19 inhibitorInhibitor0.7813
CYP450 3A4 inhibitorInhibitor0.6242
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8602
Ames testNon AMES toxic0.5216
CarcinogenicityNon-carcinogens0.8843
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3522 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9704
hERG inhibition (predictor II)Non-inhibitor0.6336
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral500 ug/1
Tabletoral500 mcg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5712298 No2000-01-272020-01-27Us
US8431154 No2003-02-192023-02-19Us
US8536206 No2004-03-082024-03-08Us
US8604064 No2004-03-082024-03-08Us
US8618142 No2004-03-082024-03-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point159.7Not Available
water solubilityinsoluble (0.52-0.56 mg/L at 22°C)Not Available
pKa8.74Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0062 mg/mLALOGPS
logP4.47ALOGPS
logP4.45ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)8.18ChemAxon
pKa (Strongest Basic)2.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area60.45 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity93.92 m3·mol-1ChemAxon
Polarizability35.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (81 KB)
SpectraNot Available
References
Synthesis Reference

http://en.wikipedia.org/wiki/File:Roflumilast_syn.png

General References
  1. Meyers JA, Taverna J, Chaves J, Makkinje A, Lerner A: Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells. Clin Cancer Res. 2007 Aug 15;13(16):4920-7. [PubMed:17699872 ]
  2. Sanz MJ, Cortijo J, Taha MA, Cerda-Nicolas M, Schatton E, Burgbacher B, Klar J, Tenor H, Schudt C, Issekutz AC, Hatzelmann A, Morcillo EJ: Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability. Br J Pharmacol. 2007 Oct;152(4):481-92. Epub 2007 Aug 20. [PubMed:17704822 ]
  3. Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28. [PubMed:17726343 ]
  4. Chong J, Poole P, Leung B, Black PN: Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2011 May 11;(5):CD002309. doi: 10.1002/14651858.CD002309.pub3. [PubMed:21563134 ]
  5. Grootendorst DC, Gauw SA, Verhoosel RM, Sterk PJ, Hospers JJ, Bredenbroker D, Bethke TD, Hiemstra PS, Rabe KF: Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD. Thorax. 2007 Dec;62(12):1081-7. Epub 2007 Jun 15. [PubMed:17573446 ]
  6. Thappali SR, Varanasi KV, Veeraraghavan S, Vakkalanka SK, Mukkanti K: Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study. J Mass Spectrom. 2012 Dec;47(12):1612-9. doi: 10.1002/jms.3103. [PubMed:23280750 ]
External Links
ATC CodesR03DX07
AHFS Codes
  • 48:32
PDB Entries
FDA labelDownload (255 KB)
MSDSDownload (569 KB)
Interactions
Drug Interactions
Drug
2-MethoxyethanolRoflumilast may increase the immunosuppressive activities of 2-Methoxyethanol.
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurineRoflumilast may increase the immunosuppressive activities of 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine.
AbataceptRoflumilast may increase the immunosuppressive activities of Abatacept.
abetimusRoflumilast may increase the immunosuppressive activities of abetimus.
ABR-215757Roflumilast may increase the immunosuppressive activities of ABR-215757.
AdalimumabRoflumilast may increase the immunosuppressive activities of Adalimumab.
AfelimomabRoflumilast may increase the immunosuppressive activities of Afelimomab.
AlefaceptRoflumilast may increase the immunosuppressive activities of Alefacept.
AlemtuzumabRoflumilast may increase the immunosuppressive activities of Alemtuzumab.
alicaforsenRoflumilast may increase the immunosuppressive activities of alicaforsen.
AltretamineRoflumilast may increase the immunosuppressive activities of Altretamine.
AmsacrineRoflumilast may increase the immunosuppressive activities of Amsacrine.
AnakinraRoflumilast may increase the immunosuppressive activities of Anakinra.
Anti-thymocyte Globulin (Rabbit)Roflumilast may increase the immunosuppressive activities of Anti-thymocyte Globulin (Rabbit).
ApremilastRoflumilast may increase the immunosuppressive activities of Apremilast.
AzacitidineRoflumilast may increase the immunosuppressive activities of Azacitidine.
AzathioprineRoflumilast may increase the immunosuppressive activities of Azathioprine.
BasiliximabRoflumilast may increase the immunosuppressive activities of Basiliximab.
BelataceptRoflumilast may increase the immunosuppressive activities of Belatacept.
BelimumabRoflumilast may increase the immunosuppressive activities of Belimumab.
BetamethasoneRoflumilast may increase the immunosuppressive activities of Betamethasone.
BleomycinRoflumilast may increase the immunosuppressive activities of Bleomycin.
BlinatumomabRoflumilast may increase the immunosuppressive activities of Blinatumomab.
Brentuximab vedotinRoflumilast may increase the immunosuppressive activities of Brentuximab vedotin.
BriakinumabRoflumilast may increase the immunosuppressive activities of Briakinumab.
BudesonideRoflumilast may increase the immunosuppressive activities of Budesonide.
BusulfanRoflumilast may increase the immunosuppressive activities of Busulfan.
CabazitaxelRoflumilast may increase the immunosuppressive activities of Cabazitaxel.
CanakinumabRoflumilast may increase the immunosuppressive activities of Canakinumab.
CapecitabineRoflumilast may increase the immunosuppressive activities of Capecitabine.
CarbamazepineThe serum concentration of Roflumilast can be decreased when it is combined with Carbamazepine.
CarboplatinRoflumilast may increase the immunosuppressive activities of Carboplatin.
CarmustineRoflumilast may increase the immunosuppressive activities of Carmustine.
CastanospermineRoflumilast may increase the immunosuppressive activities of Castanospermine.
Certolizumab pegolRoflumilast may increase the immunosuppressive activities of Certolizumab pegol.
ChlorambucilRoflumilast may increase the immunosuppressive activities of Chlorambucil.
CimetidineThe serum concentration of the active metabolites of Roflumilast can be increased when Roflumilast is used in combination with Cimetidine.
CiprofloxacinThe serum concentration of Roflumilast can be increased when it is combined with Ciprofloxacin.
CisplatinRoflumilast may increase the immunosuppressive activities of Cisplatin.
CladribineRoflumilast may increase the immunosuppressive activities of Cladribine.
ClofarabineRoflumilast may increase the immunosuppressive activities of Clofarabine.
CorticotropinRoflumilast may increase the immunosuppressive activities of Corticotropin.
Cortisone acetateRoflumilast may increase the immunosuppressive activities of Cortisone acetate.
CyclophosphamideRoflumilast may increase the immunosuppressive activities of Cyclophosphamide.
CyclosporineRoflumilast may increase the immunosuppressive activities of Cyclosporine.
CytarabineRoflumilast may increase the immunosuppressive activities of Cytarabine.
DacarbazineRoflumilast may increase the immunosuppressive activities of Dacarbazine.
DaclizumabRoflumilast may increase the immunosuppressive activities of Daclizumab.
DactinomycinRoflumilast may increase the immunosuppressive activities of Dactinomycin.
DasatinibRoflumilast may increase the immunosuppressive activities of Dasatinib.
DaunorubicinRoflumilast may increase the immunosuppressive activities of Daunorubicin.
DexamethasoneRoflumilast may increase the immunosuppressive activities of Dexamethasone.
Dimethyl fumarateRoflumilast may increase the immunosuppressive activities of Dimethyl fumarate.
DinutuximabRoflumilast may increase the immunosuppressive activities of Dinutuximab.
DocetaxelRoflumilast may increase the immunosuppressive activities of Docetaxel.
DoxorubicinRoflumilast may increase the immunosuppressive activities of Doxorubicin.
EculizumabRoflumilast may increase the immunosuppressive activities of Eculizumab.
EfalizumabRoflumilast may increase the immunosuppressive activities of Efalizumab.
EnzalutamideThe serum concentration of Roflumilast can be decreased when it is combined with Enzalutamide.
EpirubicinRoflumilast may increase the immunosuppressive activities of Epirubicin.
EstramustineRoflumilast may increase the immunosuppressive activities of Estramustine.
EtanerceptRoflumilast may increase the immunosuppressive activities of Etanercept.
EtoposideRoflumilast may increase the immunosuppressive activities of Etoposide.
EverolimusRoflumilast may increase the immunosuppressive activities of Everolimus.
FingolimodRoflumilast may increase the immunosuppressive activities of Fingolimod.
FloxuridineRoflumilast may increase the immunosuppressive activities of Floxuridine.
FludarabineRoflumilast may increase the immunosuppressive activities of Fludarabine.
FludrocortisoneRoflumilast may increase the immunosuppressive activities of Fludrocortisone.
FluorouracilRoflumilast may increase the immunosuppressive activities of Fluorouracil.
FluvoxamineThe serum concentration of the active metabolites of Roflumilast can be increased when Roflumilast is used in combination with Fluvoxamine.
FosphenytoinThe serum concentration of Roflumilast can be decreased when it is combined with Fosphenytoin.
Gallium nitrateRoflumilast may increase the immunosuppressive activities of Gallium nitrate.
GemcitabineRoflumilast may increase the immunosuppressive activities of Gemcitabine.
Gemtuzumab ozogamicinRoflumilast may increase the immunosuppressive activities of Gemtuzumab ozogamicin.
Glatiramer AcetateRoflumilast may increase the immunosuppressive activities of Glatiramer Acetate.
GlimepirideRoflumilast may increase the immunosuppressive activities of Glimepiride.
GolimumabRoflumilast may increase the immunosuppressive activities of Golimumab.
HydrocortisoneRoflumilast may increase the immunosuppressive activities of Hydrocortisone.
HydroxyureaRoflumilast may increase the immunosuppressive activities of Hydroxyurea.
Ibritumomab tiuxetanRoflumilast may increase the immunosuppressive activities of Ibritumomab tiuxetan.
IbrutinibRoflumilast may increase the immunosuppressive activities of Ibrutinib.
IcatibantRoflumilast may increase the immunosuppressive activities of Icatibant.
IdarubicinRoflumilast may increase the immunosuppressive activities of Idarubicin.
IdelalisibRoflumilast may increase the immunosuppressive activities of Idelalisib.
IfosfamideRoflumilast may increase the immunosuppressive activities of Ifosfamide.
ImatinibRoflumilast may increase the immunosuppressive activities of Imatinib.
ImiquimodRoflumilast may increase the immunosuppressive activities of Imiquimod.
InfliximabRoflumilast may increase the immunosuppressive activities of Infliximab.
IrinotecanRoflumilast may increase the immunosuppressive activities of Irinotecan.
L-PhenylalanineRoflumilast may increase the immunosuppressive activities of L-Phenylalanine.
LeflunomideRoflumilast may increase the immunosuppressive activities of Leflunomide.
LenalidomideRoflumilast may increase the immunosuppressive activities of Lenalidomide.
LomustineRoflumilast may increase the immunosuppressive activities of Lomustine.
MechlorethamineRoflumilast may increase the immunosuppressive activities of Mechlorethamine.
MelphalanRoflumilast may increase the immunosuppressive activities of Melphalan.
MepolizumabRoflumilast may increase the immunosuppressive activities of Mepolizumab.
MercaptopurineRoflumilast may increase the immunosuppressive activities of Mercaptopurine.
MethotrexateRoflumilast may increase the immunosuppressive activities of Methotrexate.
MethylprednisoloneRoflumilast may increase the immunosuppressive activities of Methylprednisolone.
MitomycinRoflumilast may increase the immunosuppressive activities of Mitomycin.
MitotaneThe serum concentration of Roflumilast can be decreased when it is combined with Mitotane.
MitoxantroneRoflumilast may increase the immunosuppressive activities of Mitoxantrone.
MuromonabRoflumilast may increase the immunosuppressive activities of Muromonab.
Mycophenolate mofetilRoflumilast may increase the immunosuppressive activities of Mycophenolate mofetil.
Mycophenolic acidRoflumilast may increase the immunosuppressive activities of Mycophenolic acid.
NatalizumabRoflumilast may increase the immunosuppressive activities of Natalizumab.
NelarabineRoflumilast may increase the immunosuppressive activities of Nelarabine.
NevirapineThe serum concentration of Roflumilast can be decreased when it is combined with Nevirapine.
NilotinibRoflumilast may increase the immunosuppressive activities of Nilotinib.
ObinutuzumabRoflumilast may increase the immunosuppressive activities of Obinutuzumab.
OxaliplatinRoflumilast may increase the immunosuppressive activities of Oxaliplatin.
PaclitaxelRoflumilast may increase the immunosuppressive activities of Paclitaxel.
PalbociclibRoflumilast may increase the immunosuppressive activities of Palbociclib.
PanobinostatRoflumilast may increase the immunosuppressive activities of Panobinostat.
PazopanibRoflumilast may increase the immunosuppressive activities of Pazopanib.
PegaspargaseRoflumilast may increase the immunosuppressive activities of Pegaspargase.
PemetrexedRoflumilast may increase the immunosuppressive activities of Pemetrexed.
PentobarbitalThe serum concentration of Roflumilast can be decreased when it is combined with Pentobarbital.
PentostatinRoflumilast may increase the immunosuppressive activities of Pentostatin.
PhenobarbitalThe serum concentration of Roflumilast can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Roflumilast can be decreased when it is combined with Phenytoin.
PimecrolimusRoflumilast may increase the immunosuppressive activities of Pimecrolimus.
PirfenidoneRoflumilast may increase the immunosuppressive activities of Pirfenidone.
PomalidomideRoflumilast may increase the immunosuppressive activities of Pomalidomide.
PralatrexateRoflumilast may increase the immunosuppressive activities of Pralatrexate.
PrednisoloneRoflumilast may increase the immunosuppressive activities of Prednisolone.
PrednisoneRoflumilast may increase the immunosuppressive activities of Prednisone.
PrimidoneThe serum concentration of Roflumilast can be decreased when it is combined with Primidone.
ProcarbazineRoflumilast may increase the immunosuppressive activities of Procarbazine.
RifabutinThe serum concentration of Roflumilast can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Roflumilast can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Roflumilast can be decreased when it is combined with Rifapentine.
RilonaceptRoflumilast may increase the immunosuppressive activities of Rilonacept.
RiociguatRoflumilast may increase the hypotensive activities of Riociguat.
RituximabRoflumilast may increase the immunosuppressive activities of Rituximab.
RuxolitinibRoflumilast may increase the immunosuppressive activities of Ruxolitinib.
SecukinumabRoflumilast may increase the immunosuppressive activities of Secukinumab.
SeocalcitolRoflumilast may increase the immunosuppressive activities of Seocalcitol.
SiltuximabRoflumilast may increase the immunosuppressive activities of Siltuximab.
SirolimusRoflumilast may increase the immunosuppressive activities of Sirolimus.
SorafenibRoflumilast may increase the immunosuppressive activities of Sorafenib.
SteproninRoflumilast may increase the immunosuppressive activities of Stepronin.
StreptozocinRoflumilast may increase the immunosuppressive activities of Streptozocin.
SunitinibRoflumilast may increase the immunosuppressive activities of Sunitinib.
TacrolimusRoflumilast may increase the immunosuppressive activities of Tacrolimus.
TemozolomideRoflumilast may increase the immunosuppressive activities of Temozolomide.
TemsirolimusRoflumilast may increase the immunosuppressive activities of Temsirolimus.
TeniposideRoflumilast may increase the immunosuppressive activities of Teniposide.
TepoxalinRoflumilast may increase the immunosuppressive activities of Tepoxalin.
TeriflunomideRoflumilast may increase the immunosuppressive activities of Teriflunomide.
ThalidomideRoflumilast may increase the immunosuppressive activities of Thalidomide.
ThiotepaRoflumilast may increase the immunosuppressive activities of Thiotepa.
TioguanineRoflumilast may increase the immunosuppressive activities of Tioguanine.
TocilizumabRoflumilast may increase the immunosuppressive activities of Tocilizumab.
TofacitinibRoflumilast may increase the immunosuppressive activities of Tofacitinib.
TopotecanRoflumilast may increase the immunosuppressive activities of Topotecan.
TositumomabRoflumilast may increase the immunosuppressive activities of Tositumomab.
TrabectedinRoflumilast may increase the immunosuppressive activities of Trabectedin.
Trastuzumab emtansineRoflumilast may increase the immunosuppressive activities of Trastuzumab emtansine.
TretinoinRoflumilast may increase the immunosuppressive activities of Tretinoin.
TriamcinoloneRoflumilast may increase the immunosuppressive activities of Triamcinolone.
UstekinumabRoflumilast may increase the immunosuppressive activities of Ustekinumab.
VedolizumabRoflumilast may increase the immunosuppressive activities of Vedolizumab.
VilanterolRoflumilast may increase the immunosuppressive activities of Vilanterol.
VinblastineRoflumilast may increase the immunosuppressive activities of Vinblastine.
VincristineRoflumilast may increase the immunosuppressive activities of Vincristine.
VindesineRoflumilast may increase the immunosuppressive activities of Vindesine.
VinorelbineRoflumilast may increase the immunosuppressive activities of Vinorelbine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Ubiquitin protein ligase binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4D
Uniprot ID:
Q08499
Molecular Weight:
91114.1 Da
References
  1. Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28. [PubMed:17726343 ]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4A
Uniprot ID:
P27815
Molecular Weight:
98142.155 Da
References
  1. Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28. [PubMed:17726343 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents.
Gene Name:
PDE4B
Uniprot ID:
Q07343
Molecular Weight:
83342.695 Da
References
  1. Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28. [PubMed:17726343 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4C
Uniprot ID:
Q08493
Molecular Weight:
79900.795 Da
References
  1. Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28. [PubMed:17726343 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 31, 2016 02:14