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Pentoxifylline

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Also known as BL 191BL-191C04AD03Neotren mrNSC-637086NSC-758481OxpentifyllineOxypentifyllinePentoxifilinaPentoxilPentoxiphyllinTrentalTrental 100Trental 400SID11111613SID11111614SID26719692SID50105176SID85231180

Summary

Pentoxifylline (CHEMBL628) is an approved small molecule (ATC C04AD03) targeting ADORA2B; indicated across 62 conditions including cardiovascular disorder and chronic kidney disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C04AD03
  • Targets: 1 (ADORA2B)
  • Indications: 62 conditions
  • Clinical trials: 144
  • Chemistry: 278.31 Da · C13H18N4O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL628
NamePentoxifylline
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4740
ATCC04AD03
Molecular formulaC13H18N4O3
Molecular weight278.31
InChIKeyBYPFEZZEUUWMEJ-UHFFFAOYSA-N

SMILES: CC(=O)CCCCN1C(=O)C2=C(N=CN2C)N(C1=O)C

IUPAC name: 3,7-dimethyl-1-(5-oxohexyl)purine-2,6-dione

Also known as: BL 191, BL-191, C04AD03, Neotren mr, NSC-637086, NSC-758481, Oxpentifylline, Oxypentifylline, Pentoxifilina, Pentoxifylline, Pentoxil, Pentoxiphyllin

Patent coverage: 7,058 distinct patent families (26,061 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
ADORA2BA2B receptorAntagonist5.290.5%P29275

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Ubiquitin carboxyl-terminal hydrolase 2, Survival motor neuron protein, Prelamin-A/C, Inositol monophosphatase 1, Endonuclease 4, Peripheral myelin protein 22, Relaxin receptor 1, Tumor necrosis factor, Thyrotropin receptor, Phosphodiesterase 4.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P976977.6Potency25.1nMCHEMBL_ACT_4832770
P084827.15Potency70.8nMCHEMBL_ACT_4807400
ADORA2B5.29Ki5180nMCHEMBL_ACT_849816
LMNA5.25Potency5623nMCHEMBL_ACT_3641040
SMN15.25Potency5623nMCHEMBL_ACT_3888699
ACHE5.18IC506600nMCHEMBL_ACT_13377216

Target pathways

Aggregated over 1 target gene(s): ADORA2B.

Top Reactome pathways

17 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction1ADORA2B
Disease1ADORA2B
Signaling by GPCR1ADORA2B
Class A/1 (Rhodopsin-like receptors)1ADORA2B
GPCR downstream signalling1ADORA2B
Metabolism of proteins1ADORA2B
Adenosine P1 receptors1ADORA2B
Nucleotide-like (purinergic) receptors1ADORA2B
G alpha (s) signalling events1ADORA2B
GPCR ligand binding1ADORA2B
Infectious disease1ADORA2B
Surfactant metabolism1ADORA2B
Leishmania infection1ADORA2B
ADORA2B mediated anti-inflammatory cytokines production1ADORA2B
Anti-inflammatory response favouring Leishmania parasite infection1ADORA2B
Leishmania parasite growth and survival1ADORA2B
Parasitic Infection Pathways1ADORA2B

Dominant GO biological processes

GO termTargets
positive regulation of chronic inflammatory response to non-antigenic stimulus1
G protein-coupled receptor signaling pathway1
adenylate cyclase-activating G protein-coupled receptor signaling pathway1
activation of adenylate cyclase activity1
positive regulation of vascular endothelial growth factor production1
obsolete positive regulation of cGMP-mediated signaling1
obsolete cGMP-mediated signaling1
positive regulation of chemokine production1
positive regulation of interleukin-6 production1
vasodilation1
mast cell degranulation1
positive regulation of mast cell degranulation1
relaxation of vascular associated smooth muscle1
presynaptic modulation of chemical synaptic transmission1
G protein-coupled adenosine receptor signaling pathway1

Indications & clinical

Indications

62 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319
chronic kidney disease3MONDO:0005300EFO:0003884
endometriosis3MONDO:0005133EFO:0001065
necrotizing enterocolitis3MONDO:0005313EFO:0003928
alcoholic hepatitis3MONDO:0001505EFO:1001345
nephrotic syndrome3MONDO:0005377EFO:0004255
brachial plexus neuropathy3MONDO:0006683EFO:1000844
glomerulonephritis3MONDO:0002462MONDO:0002462
osteonecrosis3MONDO:0005380MONDO:0018373
cirrhosis of liver3MONDO:0005155EFO:0001422
liver failure3MONDO:0100192MONDO:0100192
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
cutaneous leishmaniasis2MONDO:0005446EFO:0005046
acute kidney injury2MONDO:0002492HP:0001919
fatty liver disease2MONDO:0004790HP:0001397
pulmonary sarcoidosis2MONDO:0001708DOID:13406
acute lymphoblastic leukemia2MONDO:0004967EFO:0000220
diabetic kidney disease2MONDO:0005016EFO:0000401
injury2MONDO:0021178EFO:0000546
breast neoplasm2MONDO:0021100EFO:0003869
upper aerodigestive tract neoplasm2MONDO:0005398EFO:0004284
leishmaniasis2MONDO:0011989EFO:0005044
brain disorder2MONDO:0005560EFO:0005774
Plasmodium falciparum malaria2MONDO:0005920EFO:0007444
metabolic dysfunction-associated steatohepatitis2MONDO:0007027EFO:1001249
primary biliary cholangitis2MONDO:0005388EFO:1001486
patent ductus arteriosus2MONDO:0011827HP:0001643
Behcet disease2MONDO:0007191EFO:0003780
acute coronary syndrome2MONDO:0005542EFO:0005672
major depressive disorder2MONDO:0002009MONDO:0002009
coronary artery disorder2MONDO:0005010EFO:0001645
depressive disorder2MONDO:0002050MONDO:0002050
biliary atresia2MONDO:0008867MONDO:0008867
epilepsy2MONDO:0005027EFO:0000474
inflammatory bowel disease2MONDO:0005265EFO:0003767
neoplasm2MONDO:0005070MONDO:0004992
sexually transmitted disease2MONDO:0021681MONDO:0021681
liver disorder2MONDO:0005154EFO:0001421
heart disorder2MONDO:0005267EFO:0003777
Parkinson disease2MONDO:0005180MONDO:0005180
long COVID-192MONDO:0100233MONDO:0100233
HIV infectious disease1MONDO:0005109EFO:0000764
central nervous system neoplasm1MONDO:0006130EFO:1000158
severe acute respiratory syndrome1MONDO:0005091MONDO:0100096
Duchenne muscular dystrophy1MONDO:0010679MONDO:0010679
alopecia areata1MONDO:0005340EFO:0004192
oral submucous fibrosis1MONDO:0018166EFO:1001818
Hermansky-Pudlak syndrome1MONDO:0019312MONDO:0019312
pancreatitis0MONDO:0004982EFO:0000278
Crohn disease0MONDO:0005011EFO:0000384
infertility disorder0MONDO:0005047EFO:0000545
anemia0MONDO:0002280EFO:0004272
acute pancreatitis0MONDO:0006515EFO:1000652
bipolar disorder0MONDO:0004985MONDO:0004985

8 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 144.

Phase distribution

PhaseTrials
PHASE241
Not specified28
PHASE422
PHASE320
PHASE2/PHASE312
EARLY_PHASE18
PHASE1/PHASE27
PHASE16

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03060434PHASE4ACTIVE_NOT_RECRUITINGPentoxifylline and Lumbar Radiculopathy
NCT03625648PHASE4ACTIVE_NOT_RECRUITINGPentoxifylline in Diabetic Kidney Disease
NCT06823362PHASE4NOT_YET_RECRUITINGBioequivalence Study of Pentoxifylline 400 Mg in Healthy Subjects Under Fasting and Fed Conditions
NCT00155246PHASE4COMPLETEDEfficacy of Pentoxifylline on Chronic Kidney Disease
NCT00770328PHASE4COMPLETEDThe Effects of Pentoxifylline on PAI-1 in an Obese Population
NCT01006499PHASE4UNKNOWNRole of ‘Pentoxifylline and or IgM Enriched Intravenous Immunoglobulin in the Treatment of Neonatal Sepsis’
NCT01269827PHASE4COMPLETEDPentoxifylline and Systemic Inflammation in Hemodialysis Patients
NCT01377285PHASE4UNKNOWNRenoprotection by Pentoxifylline and Angiotensin Receptor Blocker in Chronic Kidney Disease (CKD)
NCT01382303PHASE4COMPLETEDEffect of Pentoxifylline on Proteinuria in Korean Type 2 Diabetic Patients
NCT01542268PHASE4UNKNOWNEffect of Pentoxifylline on Tight Junctions (TJs) of Intestinal Mucosa in Patients With Irritable Bowel Syndrome(IBS)
NCT02008214PHASE4UNKNOWNEfficacy of PTX+IFN Alpha+ RBV on Hepatitis C Virus Coinfected HIV Patients
NCT02368457PHASE4COMPLETEDManagement of Mandibular ORN: PENTO as Medical Treatment
NCT03006952PHASE4COMPLETEDAdd-on Pentoxifylline to Losartan Versus Increasing Dose of Losartan on NT-PRO BNP in Type 2 Diabetics With Nephropathy
NCT03664414PHASE4UNKNOWNPentoxifylline Effect in Patients With Diabetic Nephropathy.(PENFOSIDINE STUDY)
NCT03859570PHASE4WITHDRAWNPentoxifylline in Lupus Nephritis
NCT04391231PHASE4WITHDRAWNHEMolysis in a Percutaneous Axial Flow LVAD, Effects of Pentoxifylline in a Randomized Controlled Trial
NCT04910178PHASE4COMPLETEDFollow-up of NAFLD Patients With MRI-PDFF
NCT04977661PHASE4COMPLETEDComparing the Effects of Vitamin E, Ursodeoxycholic Acid and Pentoxyfylline on Egyptian Non-alcoholic Steatohepatitis (NASH) Patients
NCT05490953PHASE4UNKNOWNEnhancing Effect on Tumour Apoptosis With the Use of Pentoxifylline in Patients With Hodgkin Lymphoma
NCT05583266PHASE4UNKNOWNEfficacy of Pentoxifylline on Cerebrovascular Function in Patients With Cerebral Small Vessel Disease(PERFORM)
NCT06115174PHASE4UNKNOWNClinical Study Evaluating the Anticancer Effect of Pentoxiphylline in Patients With Metastatic Colorectal Cancer
NCT06265389PHASE4COMPLETEDPentoxifylline as an Adjuvant Therapy in the Treatment of Pediatric Pneumonia; A New Perspective of an Old Drug
NCT03040778PHASE3ACTIVE_NOT_RECRUITINGPentoxifylline and Tocopherol (PENTO) in the Treatment of Medication-related Osteonecrosis of the Jaw (MRONJ)
NCT05284656PHASE3ACTIVE_NOT_RECRUITINGEffect of Folic Acid and/or Pentoxifylline on Patients With Chronic Kidney Disease
NCT05897034PHASE2/PHASE3NOT_YET_RECRUITINGCombination Therapy Between Doxycycline, Pentoxifylline, and Nitazoxanide in Sexually Active Men
NCT06040489PHASE2/PHASE3RECRUITINGPilot Study: Oral Treatment of American Tegumentary Leishmaniasis (Cutaneous and Mucosal Forms) in the Elderly
NCT06421870PHASE3RECRUITINGRenoprotective Effects of Dapagliflozin Versus Pentoxiphylline in Chronic Kidney Disease Patients
NCT07499817PHASE3RECRUITINGEffect of Pentoxyfilline on Endometrial Thickness and Frozen Embryo Transfer Outcomes
NCT00162552PHASE3COMPLETEDClinical Trial of Pentoxifylline in Patient With Cirrhosis
NCT00267670PHASE2/PHASE3COMPLETEDPentoxifylline/Nonalcoholic Steatohepatitis (NASH) Study: The Effect of Pentoxifylline on NASH
NCT00285298PHASE3COMPLETEDPentoxifylline and Progression of Chronic Kidney Disease in Moderate-to-high Risk Patients
NCT00354198PHASE3TERMINATEDEfficacy of Pentoxifylline on Rapidly Progressive Glomerulonephritis
NCT00354731PHASE3COMPLETEDEfficacy of Pentoxifylline on Primary Nephrotic Syndrome
NCT00632697PHASE3COMPLETEDPentoxifylline and Endometriosis
NCT00663949PHASE2/PHASE3COMPLETEDAssessment of the Effect of Captopril Versus Combination of Captopril and Pentoxifylline on Reducing Proteinuria in Type 2 Diabetic Nephropathy
NCT01214226PHASE3COMPLETEDDouble-blind Randomized Controlled Trial in Severe Alcoholic Hepatitis
NCT01263925PHASE3COMPLETEDProstaglandin E1 in Outpatients With Intermittent Claudication
NCT01291433PHASE3COMPLETEDTrial of Combined Pentoxifylline-tocopherol-clodronate vs Placebo in Radiation-induced Brachial Plexopathy
NCT01381055PHASE2/PHASE3COMPLETEDAntimony Plus Pentoxifylline in Cutaneous Leishmaniasis
NCT01455337PHASE3UNKNOWNShort-term Survival in Patients With Severe Alcoholic Hepatitis Treated With Steroid Versus Pentoxifylline

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

23 molecules share ≥1 primary target. Top 23 by shared-target count:

MoleculeSourceStatusShared targets
ACEFYLLINEChEMBLPhase 4 (approved)ADORA2B
ADENOSINEChEMBLPhase 4 (approved)ADORA2B
CAFFEINEChEMBLPhase 4 (approved)ADORA2B
ISTRADEFYLLINEChEMBLPhase 4 (approved)ADORA2B
REGADENOSONChEMBLPhase 4 (approved)ADORA2B
THEOPHYLLINEChEMBLPhase 4 (approved)ADORA2B
BINODENOSONChEMBLPhase 3ADORA2B
ROLOFYLLINEChEMBLPhase 3ADORA2B
TONAPOFYLLINEChEMBLPhase 3ADORA2B
TOZADENANTChEMBLPhase 3ADORA2B
TRABODENOSONChEMBLPhase 3ADORA2B
CIFORADENANTChEMBLPhase 2ADORA2B
DENBUFYLLINEChEMBLPhase 2ADORA2B
DERENOFYLLINEChEMBLPhase 2ADORA2B
ENPROFYLLINEChEMBLPhase 2ADORA2B
ETOFYLLINEChEMBLPhase 2ADORA2B
ETRUMADENANTChEMBLPhase 2ADORA2B
IMARADENANTChEMBLPhase 2ADORA2B
MIVEBRESIBChEMBLPhase 2ADORA2B
PSILOCINChEMBLPhase 2ADORA2B
SONEDENOSONChEMBLPhase 2ADORA2B
TECADENOSONChEMBLPhase 2ADORA2B
VIPADENANTChEMBLPhase 2ADORA2B

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot