Identification

Name
Pentoxifylline
Accession Number
DB00806  (APRD00121)
Type
Small Molecule
Groups
Approved, Investigational
Description

A methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production. [PubChem]

Structure
Thumb
Synonyms
  • Oxpentifylline
  • Pentoxifilina
  • Pentoxifyllin
  • Pentoxifylline
  • Pentoxifyllinum
External IDs
BL 191 / BL-191 / C04AD03 / PTX
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pentoxifylline SRTablet, extended release400 mgOralAa Pharma Inc1997-01-14Not applicableCanada
TrentalTablet, film coated, extended release400 mg/1OralSanofi Aventis1984-08-302013-12-31Us
TrentalTablet, extended release400 mgOralSanofi Aventis1996-10-232013-03-01Canada
TrentalTablet, film coated400 mg/1OralPhysicians Total Care, Inc.1984-08-302011-09-30Us
Trental Srt 400mgTablet, extended release400 mgOralHoechst Roussel Canada Inc.1993-12-311998-08-12Canada
Trental Tab 400mgTablet, extended release400 mgOralHoechst Canada Inc.1984-12-311996-08-29Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nu-pentoxifylline-SR 400 mgTablet, extended release400 mgOralNu Pharm Inc1998-03-182012-09-04Canada
PentoxifyllineTablet, extended release400 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2014-12-262017-06-01Us
PentoxifyllineTablet, film coated, extended release400 mg/1OralCardinal Health1999-06-102012-10-31Us55154 666220180907 15195 f6oifd
PentoxifyllineTablet, film coated, extended release400 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
PentoxifyllineTablet, extended release400 mg/1OralLake Erie Medical Dba Quality Care Produts Llc1998-07-312016-06-01Us
PentoxifyllineTablet, extended release400 mg/1OralNucare Pharmaceuticals, Inc.1999-06-10Not applicableUs
PentoxifyllineTablet, extended release400 mg/1OralTeva1998-07-31Not applicableUs0093 511620180815 3285 1s16y5f
PentoxifyllineTablet, extended release400 mg/1OralAv Kare, Inc.2013-07-312017-11-01Us
PentoxifyllineTablet, film coated, extended release400 mg/1OralMylan Institutional1998-01-15Not applicableUs
PentoxifyllineTablet, extended release400 mg/1OralPhysicians Total Care, Inc.2003-03-25Not applicableUs00093 5116 01 nlmimage10 b92d5c8a
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Gapeam BudibacPentoxifylline (1 g/1g) + Amantadine hydrochloride (1 g/1g) + Baclofen (1 g/1g) + Bupivacaine hydrochloride (1 g/1g) + Cyclobenzaprine Hydrochloride (1 g/1g) + Diclofenac sodium (1 g/1g) + Gabapentin (1 g/1g)KitTopicalAlvix Laboratories2014-12-052018-03-08Us
International/Other Brands
Agapurin (Zentiva) / Agapurin SR (Zentiva) / An Ruo Ning (Nanjing Yaoda Bio-Pharmaceutical) / Angiopent (Helcor) / Ao Le Ni (C & O Pharmaceuticals) / Ao Nuo Hong (AosaiKang Pharmaceutical) / Aotong (Treeful Pharmaceutical) / Azupentat / Behrifil (Sanofi-Aventis) / Bo Shu Te (Jisheng Pharmaceutical) / Claudicat (Nycomed) / Durapental (Mylan dura) / Elorgan (Sanofi Aventis) / Endopentoksas (Endokriniai) / Pentilin (Krka) / Pentilin Retard (Krka) / Pentoflux (Bouchara-Recordati) / Pentofyllin (Sopharma) / Pentoksifilin (Panfarma) / Pentolab (Lamsa) / Pentomer (ratiopharm) / Pentoxil (Upsher-Smith) / Rentylin (Amdipharm) / Torental (Sanofi-Aventis) / Trental / Trentilin Retard (Santa-Farma)
Categories
UNII
SD6QCT3TSU
CAS number
6493-05-6
Weight
Average: 278.307
Monoisotopic: 278.137890462
Chemical Formula
C13H18N4O3
InChI Key
BYPFEZZEUUWMEJ-UHFFFAOYSA-N
InChI
InChI=1S/C13H18N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8H,4-7H2,1-3H3
IUPAC Name
3,7-dimethyl-1-(5-oxohexyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione
SMILES
CN1C=NC2=C1C(=O)N(CCCCC(C)=O)C(=O)N2C

Pharmacology

Indication

For the treatment of patients with intermittent lameness or immobility arising from chronic occlusive arterial disease of the limbs.

Associated Conditions
Pharmacodynamics

Pentoxifylline, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.

Mechanism of action

Pentoxifylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, pentoxifylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. It is also a non selective adenosine receptor antagonist.

TargetActionsOrganism
AcAMP-specific 3',5'-cyclic phosphodiesterase 4B
inhibitor
Human
AAdenosine receptor A1
antagonist
Human
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Human
AAdenosine receptor A2a
antagonist
Human
U5'-nucleotidase
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

70%

Metabolism
Not Available
Route of elimination

Excretion is almost totally urinary; the main biotransformation product is Metabolite V. Essentially no parent drug is found in the urine.

Half life

0.4-0.8 hours

Clearance
Not Available
Toxicity

LD50=1385 mg/kg(orally in mice)

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe therapeutic efficacy of (R)-warfarin can be increased when used in combination with Pentoxifylline.
(S)-WarfarinThe therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Pentoxifylline.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Pentoxifylline.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Pentoxifylline.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Pentoxifylline.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with Pentoxifylline.
3,5-diiodothyropropionic acidThe serum concentration of Pentoxifylline can be increased when it is combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Pentoxifylline.
4-hydroxycoumarinThe therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Pentoxifylline.
6-Deoxyerythronolide BThe metabolism of Pentoxifylline can be decreased when combined with 6-Deoxyerythronolide B.
Food Interactions
  • Take with food to reduce irritation. Limit caffeine intake.

References

General References
  1. Authors unspecified: European Pentoxifylline Multi-Infarct Dementia Study. Eur Neurol. 1996;36(5):315-21. [PubMed:8864715]
External Links
Human Metabolome Database
HMDB0014944
KEGG Drug
D00501
KEGG Compound
C07424
PubChem Compound
4740
PubChem Substance
46505940
ChemSpider
4578
BindingDB
10850
ChEBI
7986
ChEMBL
CHEMBL628
Therapeutic Targets Database
DAP000048
PharmGKB
PA450864
HET
PNX
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pentoxifylline
ATC Codes
R03DA20 — Combinations of xanthinesC04AD03 — Pentoxifylline
AHFS Codes
  • 20:24.00 — Hemorrheologic Agents
PDB Entries
2a3c / 3arr / 3aru / 3tvx
FDA label
Download (51.7 KB)
MSDS
Download (73.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentAcute Pancreatitis (AP)1
0RecruitingPreventionPancreatitis1
0RecruitingTreatmentCrohn's Disease (CD)1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1TerminatedTreatmentAlcoholic Hepatitis (AH)1
1TerminatedTreatmentHepatopulmonary Syndrome1
1, 2CompletedTreatmentMuscular Dystrophy, Duchenne2
2Active Not RecruitingTreatmentLong-term Adverse Effects of Radiotherapy for Pelvic Cancer1
2CompletedPreventionColorectal Cancers / Hepatic Metastases / Irradiation Damage / Radiation Induced Liver Disease1
2CompletedPreventionFibrosis1
2CompletedSupportive CareCancer, Breast / Lymphedema of the extremities1
2CompletedTreatmentAnemia of Chronic Kidney Disease1
2CompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV)1
2CompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections / Vascular Diseases1
2CompletedTreatmentCardiovascular Disease (CVD) / Coronary Artery Disease / Depression / Depressive Symptoms / Heart Diseases / Major Depressive Disorder (MDD)1
2CompletedTreatmentFatty Liver1
2CompletedTreatmentFibrosis / Radiation Injuries1
2CompletedTreatmentNonalcoholic Steatohepatitis1
2CompletedTreatmentPrimary Biliary Cholangitis1
2CompletedTreatmentSarcoidosis, Pulmonary1
2RecruitingPreventionBrain Metastasis1
2RecruitingPreventionNeoplasms, Head and Neck1
2RecruitingTreatmentBiliary Atresia1
2RecruitingTreatmentLeishmaniasis1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2TerminatedTreatmentEnd Stage Renal Disease (ESRD)1
2TerminatedTreatmentNeoplasms, Breast1
2TerminatedTreatmentPlasmodium Falciparum Malaria1
2TerminatedTreatmentWounds and Injuries1
2Unknown StatusTreatmentFibrosis1
2Unknown StatusTreatmentNecrotizing Enterocolitis1
2Unknown StatusTreatmentPatent Ductus Arteriosus (PDA)1
2, 3CompletedTreatmentAcute Alcoholic Hepatitis1
2, 3CompletedTreatmentDiabetic Nephropathies1
2, 3CompletedTreatmentLeishmaniasis, Cutaneous2
2, 3CompletedTreatmentLiver Diseases / Nonalcoholic Steatohepatitis1
2, 3Not Yet RecruitingTreatmentAcute Kidney Injury (AKI) / Pentoxifylline1
2, 3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
3Active Not RecruitingTreatmentCancer, Breast1
3Active Not RecruitingTreatmentInfection, Human Immunodeficiency Virus I1
3CompletedTreatmentAcute on Chronic Pancreatitis / Acute Pancreatitis (AP) / Autoimmune Pancreatitis / Cancer Acute Pancreatitis / Drug Induced AP / Gallstone Pancreatitis / Hypertriglyceridemia Acute Pancreatitis / Hypertriglyceridemia AP / Idiopathic (Unknown) Acute Pancreatitis / Medication Induced Acute Pancreatitis / Miscellaneous (i.e. Acute on Chronic Pancreatitis) / Pancreatitis, Alcoholic / Post-ERCP AP / Post-ERCP/Post-procedural Pancreatitis / Trauma Acute Pancreatitis / Trauma AP1
3CompletedTreatmentAlcoholic Hepatitis (AH) / Severe alcoholic liver disease1
3CompletedTreatmentChronic Renal Failure (CRF)1
3CompletedTreatmentEndometriosis-Associated Infertility1
3CompletedTreatmentGlomerulonephritis minimal lesion1
3CompletedTreatmentHTLV-1 / Immune System Diseases / Pentoxifylline / Physical Disability / Tropical Spastic Paraparesis1
3CompletedTreatmentHepatic Failure / Liver Cirrhosis1
3CompletedTreatmentIntermittent Claudication Fontaine Stage II PAOD / Stage II Peripheral Arterial Occlusive Disease1
3CompletedTreatmentNeonatal Late Onset Sepsis1
3CompletedTreatmentRadiation Induced Brachial Plexopathy1
3Not Yet RecruitingSupportive CareCarcinoma, Breast / Fibrosis1
3RecruitingTreatmentAcute Kidney Injury (AKI)1
3RecruitingTreatmentAvascular Necrosis / Bisphosphonate-related Osteonecrosis of the Jaw / Medication-related Osteonecrosis of the Jaw1
3RecruitingTreatmentErectile Dysfunction (ED) / Prostate Cancer1
3TerminatedTreatmentGlomerulonephritis1
3Unknown StatusTreatmentAlcoholic Hepatitis (AH)1
4CompletedPreventionDiabetic Nephropathies1
4CompletedTreatmentBMI >30 kg/m21
4CompletedTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentEnd-Stage Renal Disease (ESRD) / Hemodialysis Treatment / Inflammatory Reaction1
4CompletedTreatmentOsteoradionecrosis1
4Not Yet RecruitingTreatmentDiabetic Kidney Disease1
4RecruitingTreatmentChronic Kidney Disease stage3 and 4 / Type 2 Diabetes Mellitus1
4RecruitingTreatmentChronic Renal Failure (CRF)1
4RecruitingTreatmentLumbar Disc Disease / Lumbar Radiculopathy / Prolapsed Lumbar Disc1
4Unknown StatusTreatmentHepacivirus / Human Immunodeficiency Virus (HIV) Infections1
4Unknown StatusTreatmentIrritable Bowel Syndrome (IBS)1
4Unknown StatusTreatmentSepsis of the Newborn1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableAlcoholic Hepatitis (AH) / Severe alcoholic liver disease1
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentPrimary Glomerulonephritis1
Not AvailableCompletedTreatmentRecurrent Aphthous Stomatitis1
Not AvailableEnrolling by InvitationTreatmentDizziness / Vertigo1
Not AvailableNo Longer AvailableNot AvailableDiabetes, Diabetes Mellitus Type 11
Not AvailableNot Yet RecruitingTreatmentAdvanced Gastric Cancer Adenocarcinoma of Esophagogastric Junction1
Not AvailableTerminatedTreatmentGraves Ophthalmopathy1
Not AvailableUnknown StatusPreventionCapsular Contractures1
Not AvailableUnknown StatusPreventionRenal Dysfunction1
Not AvailableUnknown StatusTreatmentCongestive Heart Failure (CHF)1
Not AvailableUnknown StatusTreatmentHepatopulmonary Syndrome1
Not AvailableUnknown StatusTreatmentMetabolic Parameters and Liver Histology1
Not AvailableUnknown StatusTreatmentNon-Alcoholic Steatohepatitis1
Not AvailableWithdrawnPreventionContrast Induced Nephropathy (CIN) / Diabetes Mellitus (DM)1

Pharmacoeconomics

Manufacturers
  • Actavis elizabeth llc
  • Apotex inc
  • Biovail laboratories inc
  • Heritage pharmaceuticals inc
  • Impax laboratories inc
  • Mylan pharmaceuticals inc
  • Pliva inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Upsher smith laboratories inc
  • Sanofi aventis us llc
Packagers
  • Amerisource Health Services Corp.
  • Amneal Pharmaceuticals
  • Apotex Inc.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Biovail Pharmaceuticals
  • Cardinal Health
  • Dept Health Central Pharmacy
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Gallipot
  • Golden State Medical Supply Inc.
  • Heartland Repack Services LLC
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Merrell Pharmaceuticals Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Pliva Inc.
  • Prepak Systems Inc.
  • Remedy Repack
  • Sandhills Packaging Inc.
  • Sanofi-Aventis Inc.
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Torpharm Inc.
  • Tya Pharmaceuticals
  • UDL Laboratories
  • Upsher Smith Laboratories
  • Va Cmop Dallas
  • Vangard Labs Inc.
  • Zoetica Pharmaceutical Corp.
Dosage forms
FormRouteStrength
KitTopical
Tablet, extended releaseOral400 mg/1
Tablet, film coated, extended releaseOral400 mg/1
Tablet, extended releaseOral400 mg
Tablet, film coatedOral400 mg/1
Prices
Unit descriptionCostUnit
TRENtal 400 mg Controlled Release Tabs1.4USD tab
Trental er 400 mg tablet1.27USD tablet
Pentoxifylline powder0.91USD g
Trental 400 mg Sustained-Release Tablet0.88USD tablet
Pentoxifylline 400 mg tablet sa0.71USD tablet
Pentoxifylline CR 400 mg Controlled Release Tabs0.62USD tab
Pentoxil 400 mg Controlled Release Tabs0.62USD tab
Pentoxil er 400 mg tablet0.62USD tablet
Pentoxifylline er 400 mg tablet0.6USD tablet
Apo-Pentoxifylline Sr 400 mg Sustained-Release Tablet0.4USD tablet
Nu-Pentoxifylline-Sr 400 mg Sustained-Release Tablet0.4USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)105 °CNot Available
water solubility7.7E+004 mg/L (at 25 °C)MERCK INDEX (1996)
logP0.29BIOBYTE (1995)
Predicted Properties
PropertyValueSource
Water Solubility5.17 mg/mLALOGPS
logP0.08ALOGPS
logP0.23ChemAxon
logS-1.7ALOGPS
pKa (Strongest Acidic)19.64ChemAxon
pKa (Strongest Basic)-0.93ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area75.51 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity73.52 m3·mol-1ChemAxon
Polarizability29.27 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9851
Caco-2 permeable-0.5056
P-glycoprotein substrateSubstrate0.595
P-glycoprotein inhibitor INon-inhibitor0.6905
P-glycoprotein inhibitor IIInhibitor0.7157
Renal organic cation transporterNon-inhibitor0.7023
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.6511
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9518
CYP450 2D6 inhibitorNon-inhibitor0.943
CYP450 2C19 inhibitorNon-inhibitor0.9313
CYP450 3A4 inhibitorNon-inhibitor0.9827
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.901
Ames testNon AMES toxic0.7131
CarcinogenicityNon-carcinogens0.8965
BiodegradationNot ready biodegradable0.7457
Rat acute toxicity2.4070 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6463
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0059-1890000000-c9be2fe26b2862cba4f5
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001r-2900000000-d54457aaede5317cef72
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0059-2970000000-95d1edcd63b61b13b22e

Taxonomy

Description
This compound belongs to the class of organic compounds known as xanthines. These are purine derivatives with a ketone group conjugated at carbons 2 and 6 of the purine moiety.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Imidazopyrimidines
Sub Class
Purines and purine derivatives
Direct Parent
Xanthines
Alternative Parents
6-oxopurines / Alkaloids and derivatives / Pyrimidones / N-substituted imidazoles / Vinylogous amides / Heteroaromatic compounds / Ureas / Lactams / Ketones / Azacyclic compounds
show 4 more
Substituents
Xanthine / 6-oxopurine / Purinone / Alkaloid or derivatives / Pyrimidone / N-substituted imidazole / Pyrimidine / Azole / Imidazole / Heteroaromatic compound
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
oxopurine (CHEBI:7986)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
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 f...
Gene Name
PDE4B
Uniprot ID
Q07343
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Molecular Weight
83342.695 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Details
2. Adenosine receptor A1
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Purine nucleoside binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
ADORA1
Uniprot ID
P30542
Uniprot Name
Adenosine receptor A1
Molecular Weight
36511.325 Da
References
  1. Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [PubMed:3588607]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, ...
Gene Name
PDE5A
Uniprot ID
O76074
Uniprot Name
cGMP-specific 3',5'-cyclic phosphodiesterase
Molecular Weight
99984.14 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]
Kind
Protein
Organism
Human
Pharmacological action
Yes
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
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Molecular Weight
98142.155 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]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Identical protein binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
ADORA2A
Uniprot ID
P29274
Uniprot Name
Adenosine receptor A2a
Molecular Weight
44706.925 Da
References
  1. Kreth S, Ledderose C, Luchting B, Weis F, Thiel M: Immunomodulatory properties of pentoxifylline are mediated via adenosine-dependent pathways. Shock. 2010 Jul;34(1):10-6. doi: 10.1097/SHK.0b013e3181cdc3e2. [PubMed:19997047]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Nucleotide binding
Specific Function
Hydrolyzes extracellular nucleotides into membrane permeable nucleosides. Exhibits AMP-, NAD-, and NMN-nucleosidase activities.
Gene Name
NT5E
Uniprot ID
P21589
Uniprot Name
5'-nucleotidase
Molecular Weight
63367.255 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. Ustunsoy H, Sivrikoz MC, Tarakcioglu M, Bakir K, Guldur E, Celkan MA: The effects of pentoxifylline on the myocardial inflammation and ischemia-reperfusion injury during cardiopulmonary bypass. J Card Surg. 2006 Jan-Feb;21(1):57-61. [PubMed:16426349]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 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. Lee SH, Slattery JT: Cytochrome P450 isozymes involved in lisofylline metabolism to pentoxifylline in human liver microsomes. Drug Metab Dispos. 1997 Dec;25(12):1354-8. [PubMed:9394024]
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Drug created on June 13, 2005 07:24 / Updated on November 20, 2018 00:47