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Ibudilast

drug
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Also known as AV-411AV411KetasMN-166SID11114182SID50104937SID90341511SID46500478SID124880398SID124880396SID144207052SID170466049

Summary

Ibudilast (CHEMBL19449) is an approved small molecule (ATC R03DC04) targeting PDE3A, PDE4A, and PDE4B; indicated across 14 conditions including obstructive lung disease and spinal cord disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: R03DC04
  • Targets: 5 (PDE3A, PDE4A, PDE4B…)
  • Indications: 14 conditions
  • Clinical trials: 23
  • Chemistry: 230.31 Da · C14H18N2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL19449
NameIbudilast
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID3671
ATCR03DC04
Molecular formulaC14H18N2O
Molecular weight230.31
InChIKeyZJVFLBOZORBYFE-UHFFFAOYSA-N

SMILES: CC(C)C1=NN2C=CC=CC2=C1C(=O)C(C)C

IUPAC name: 2-methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one

Also known as: AV-411, AV411, Ibudilast, Ketas, MN-166, SID11114182, SID50104937, SID90341511, SID46500478, SID124880398, ibudilast, SID124880396

Patent coverage: 1,956 distinct patent families (7,461 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
PDE3Aphosphodiesterase 3AInhibition3.520.1%Q14432
PDE4Aphosphodiesterase 4AInhibition7.270.4%P27815
PDE4Bphosphodiesterase 4BInhibition7.190.2%Q07343
PDE4Cphosphodiesterase 4CInhibition6.620.2%Q08493
PDE5Aphosphodiesterase 5AInhibition3.990%O76074

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: Nuclear receptor ROR-gamma, RecQ-like DNA helicase BLM, cGMP-specific 3’,5’-cyclic phosphodiesterase, Thyrotropin receptor, Macrophage migration inhibitory factor, Menin/Histone-lysine N-methyltransferase MLL, Adenosine receptor A1, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Adenosine receptor A2a, 3’,5’-cyclic-AMP phosphodiesterase 4A.

Bioactivity

ChEMBL activities: 33 potent at pChembl ≥ 5 of 44 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
BLM7.6Potency25.1nMCHEMBL_ACT_4753935
BLM7.6Potency25.1nMCHEMBL_ACT_4945917
CYP2D67.4Potency39.8nMCHEMBL_ACT_4990278
CYP2D67.4AC5039.81nMCHEMBL_ACT_6062897
PDE4A7.27IC5054nMCHEMBL_ACT_2234509
PDE4A7.27IC5054nMCHEMBL_ACT_22875424
PDE4A7.27IC5054nMCHEMBL_ACT_26335779
PDE4B7.19IC5065nMCHEMBL_ACT_2234510
PDE4B7.19IC5065nMCHEMBL_ACT_22875425
PDE4B7.19IC5065nMCHEMBL_ACT_26335781
PDE4D6.78IC50166nMCHEMBL_ACT_2234514
PDE4D6.78IC50166nMCHEMBL_ACT_22875473
PDE4D6.78IC50166nMCHEMBL_ACT_26335780
PDE4C6.62IC50239nMCHEMBL_ACT_2234511
PDE4C6.62IC50239nMCHEMBL_ACT_22875472
PDE4C6.62IC50239nMCHEMBL_ACT_26335782
PDE4D6.4AC50400nMCHEMBL_ACT_25185442
CYP2C96.2Potency631nMCHEMBL_ACT_5017031
CYP1A26.2AC50631nMCHEMBL_ACT_6034017
PDE4A6.05EC50900nMCHEMBL_ACT_12071030
PDE4A5.89IC501300nMCHEMBL_ACT_12071013
MIF5.85Kd1400nMCHEMBL_ACT_22413944
PDE3A5.8IC501600nMCHEMBL_ACT_26325381
PDE3B5.57IC502700nMCHEMBL_ACT_26325382
CYP2C195.5Potency3162nMCHEMBL_ACT_4019320
CYP2C195.5AC503162nMCHEMBL_ACT_6030607
PDE5A5.46IC503510nMCHEMBL_ACT_26325379
PDE5A5.46IC503510nMCHEMBL_ACT_26325380
PDE4B5.3IC505000nMCHEMBL_ACT_6205278
P628135.24AC505700nMCHEMBL_ACT_25130708

Target pathways

Aggregated over 5 target gene(s): PDE3A, PDE4A, PDE4B, PDE4C, PDE5A.

Top Reactome pathways

5 total, by targets touching each:

PathwayTargetsGenes
DARPP-32 events3PDE4A, PDE4B, PDE4C
G alpha (s) signalling events3PDE3A, PDE4A, PDE4C
cGMP effects1PDE5A
Smooth Muscle Contraction1PDE5A
RHOBTB1 GTPase cycle1PDE5A

Dominant GO biological processes

GO termTargets
negative regulation of cAMP/PKA signal transduction5
signal transduction5
cAMP catabolic process3
G protein-coupled receptor signaling pathway2
cellular response to xenobiotic stimulus2
oocyte maturation1
lipid metabolic process1
response to xenobiotic stimulus1
regulation of meiotic nuclear division1
negative regulation of apoptotic process1
negative regulation of vascular permeability1
positive regulation of vascular permeability1
positive regulation of oocyte development1
regulation of ribonuclease activity1
cellular response to cGMP1

Indications & clinical

Indications

14 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
obstructive lung disease4MONDO:0002267HP:0006536
spinal cord disorder3MONDO:0002545HP:0002196
opiate dependence2MONDO:0005530EFO:0005611
chronic progressive multiple sclerosis2MONDO:0005284EFO:0003840
methamphetamine dependence2MONDO:0005419EFO:0004701
viral pneumonia2MONDO:0006012EFO:0007541
amyotrophic lateral sclerosis2MONDO:0004976MONDO:0004976
alcohol abuse2MONDO:0002046MONDO:0007079
long COVID-192MONDO:0100233MONDO:0100233
glioblastoma1MONDO:0018177EFO:0000519
diabetic neuropathy1MONDO:0006626EFO:1000783
substance-related disorder1MONDO:0002494MONDO:0002491
migraine disorder1MONDO:0005277MONDO:0005277

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

Clinical trials

Total trials: 23.

Phase distribution

PhaseTrials
PHASE210
PHASE15
PHASE1/PHASE24
PHASE2/PHASE32
PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04057898PHASE2/PHASE3ACTIVE_NOT_RECRUITINGEvaluation of MN-166 (Ibudilast) for 12 Months Followed by an Open-label Extension for 6 Months in Patients With ALS
NCT04631471PHASE3RECRUITINGRegeneration in Cervical Degenerative Myelopathy
NCT05513560PHASE2/PHASE3COMPLETEDRECLAIM: Recovering From COVID-19 Lingering Symptoms Adaptive Integrative Medicine
NCT05414240PHASE2ACTIVE_NOT_RECRUITINGIbudilast for Treating Alcohol Use Disorder
NCT00576277PHASE1/PHASE2COMPLETEDSafety, Tolerability, Pharmacokinetics and Preliminary Efficacy of AV411 in Neuropathic Pain
NCT00723177PHASE2COMPLETEDPhase IIa Study of AV411, a Glial Activation Inhibitor, for Opioid Withdrawal
NCT01317992PHASE1/PHASE2UNKNOWNIbudilast in the Treatment of Medication Overuse Headache
NCT01740414PHASE2COMPLETEDEffects of Ibudilast on Oxycodone Self-administration in Opioid Abusers
NCT01860807PHASE2COMPLETEDTrial of Ibudilast for Methamphetamine Dependence
NCT01982942PHASE2COMPLETEDSafety, Tolerability and Activity Study of Ibudilast in Subjects With Progressive Multiple Sclerosis
NCT02238626PHASE2COMPLETEDIbudilast (MN-166) in Subjects With Amyotrophic Lateral Sclerosis (ALS)
NCT02714036PHASE1/PHASE2COMPLETEDA Biomarker Study to Evaluate MN-166 in Subjects With Amyotrophic Literal Sclerosis (ALS)
NCT03341078PHASE2COMPLETEDPilot Study of the Effect of Ibudilast on Neuroinflammation in Methamphetamine Users
NCT03489850PHASE2COMPLETEDIbudilast and Withdrawal-Related Dysphoria
NCT03594435PHASE2COMPLETEDIbudilast for the Treatment of Alcohol Use Disorder
NCT03782415PHASE1/PHASE2COMPLETEDStudy to Evaluate Ibudilast and TMZ Combo Treatment in Newly Diagnosed and Recurrent Glioblastoma
NCT04429555PHASE2COMPLETEDEfficacy, Safety, Tolerability, and Biomarkers of Ibudilast (MN-166) in Patients Hospitalized With COVID-19 at Risk for ARDS
NCT01217970PHASE1COMPLETEDSafety Interaction Trial Ibudilast and Methamphetamine
NCT01389193PHASE1COMPLETEDIbudilast in the Treatment of Patients With Chronic Migraine.
NCT02025998PHASE1COMPLETEDDevelopment of Ibudilast for Alcohol Use Disorder
NCT03533387PHASE1COMPLETEDStudy of MN-166 (Ibudilast) Extended Release Tablet Formulations Compared With Capsules in Healthy Volunteers
NCT04054206PHASE1COMPLETEDRelative Bioavailability of MN-166 (Ibudilast) in Extended Release Tablet vs. Intermediate-release Capsule in Healthy Volunteers
NCT06743776Not specifiedAVAILABLEScalable Expanded Access With Analysis of Neurofilament and Other Biomarkers for Ibudilast in ALS

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.

316 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
SILDENAFILChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
TadalafilChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
VARDENAFILChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
DIPYRIDAMOLEChEMBLPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
MILRINONEChEMBLPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
PAPAVERINEChEMBLPhase 3PDE3A, PDE4A, PDE4B, PDE4C, PDE5A
ApremilastChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C
LOSARTANChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C
CRISABOROLEChEMBLPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C
ENOXIMONEChEMBLPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C
INAMRINONEChEMBLPhase 4 (approved)PDE3A, PDE4A, PDE4B, PDE4C
ADIBENDANChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
CIPAMFYLLINEChEMBLPhase 2PDE4A, PDE4B, PDE4C, PDE5A
ENPROFYLLINEChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
IMAZODANChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
INDOLIDANChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
LIXAZINONEChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
ROLIPRAMChEMBLPhase 2PDE4A, PDE4B, PDE4C, PDE5A
ZAPRINASTChEMBLPhase 2PDE4A, PDE4B, PDE4C, PDE5A
ZARDAVERINEChEMBLPhase 2PDE3A, PDE4A, PDE4B, PDE4C
ENSIFENTRINEChEMBLPhase 4 (approved)PDE4A, PDE4B, PDE4C
PENTOXIFYLLINEChEMBLPhase 4 (approved)PDE4A, PDE4B, PDE4C
ROFLUMILASTChEMBLPhase 4 (approved)PDE4A, PDE4B, PDE4C
THEOPHYLLINEChEMBLPhase 4 (approved)PDE4A, PDE4B, PDE4C
CILOMILASTChEMBLPhase 3PDE4A, PDE4B, PDE4C
MUFEMILASTChEMBLPhase 3PDE4A, PDE4B, PDE4C
TETOMILASTChEMBLPhase 3PDE4A, PDE4B, PDE4C
AZD-6482ChEMBLPhase 2PDE4A, PDE4B, PDE4C
BMS-911543ChEMBLPhase 2PDE4A, PDE4B, PDE4C
CDC-801ChEMBLPhase 2PDE4A, PDE4B, PDE4C
DENBUFYLLINEChEMBLPhase 2PDE4A, PDE4B, PDE4C
LOTAMILASTChEMBLPhase 2PDE4A, PDE4B, PDE4C
MK-0873ChEMBLPhase 2PDE4A, PDE4B, PDE4C
NITRAQUAZONEChEMBLPhase 2PDE4A, PDE4B, PDE4C
ORISMILASTChEMBLPhase 2PDE3A, PDE4A, PDE4B
PELRINONEChEMBLPhase 2PDE4A, PDE4B, PDE4C
PICLAMILASTChEMBLPhase 2PDE4A, PDE4B, PDE4C
PUMAFENTRINEChEMBLPhase 2PDE4A, PDE4B, PDE4C
REVAMILASTChEMBLPhase 2PDE4A, PDE4B, PDE4C
STREPTONIGRINChEMBLPhase 2PDE4A, PDE4B, PDE4C
TOCLADESINEChEMBLPhase 2PDE4A, PDE4B, PDE4C
TRANIMILASTChEMBLPhase 2PDE4A, PDE4B, PDE4C
TREQUINSINChEMBLPhase 2PDE4A, PDE4B, PDE4C
gentian violetChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A
UmeclidiniumChEMBL + PubChemPhase 4 (approved)PDE3A, PDE4A
ACARBOSEChEMBLPhase 4 (approved)PDE3A, PDE4A
ALECTINIBChEMBLPhase 4 (approved)PDE3A, PDE4A
DEQUALINIUMChEMBLPhase 4 (approved)PDE3A, PDE4A
ESTRADIOL CYPIONATEChEMBLPhase 4 (approved)PDE3A, PDE4A
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)PDE3A, PDE4A
FEXOFENADINEChEMBLPhase 4 (approved)PDE3A, PDE4A
HEXACHLOROPHENEChEMBLPhase 4 (approved)PDE3A, PDE4A
PALBOCICLIBChEMBLPhase 4 (approved)PDE4A, PDE5A
PHENAZOPYRIDINEChEMBLPhase 4 (approved)PDE3A, PDE4A
PHYTONADIONEChEMBLPhase 4 (approved)PDE3A, PDE4A
PRIMAQUINEChEMBLPhase 4 (approved)PDE3A, PDE4A
TELMISARTANChEMBLPhase 4 (approved)PDE3A, PDE4A
TICAGRELORChEMBLPhase 4 (approved)PDE3A, PDE4A
TRIMETREXATEChEMBLPhase 4 (approved)PDE3A, PDE4A
TROGLITAZONEChEMBLPhase 4 (approved)PDE3A, PDE4A

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