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Atlas / Drug / Alvimopan

Alvimopan

drug
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Also known as Alvimopan anhydrousAlvimopan dihydrateAnhydrous alvimopanEnteregLY-246736LY-246736 DIHYDRATELY246736ALVIMOPAN (MONOHYDRATE)Alvimopan

Summary

Alvimopan (CHEMBL270190) is an approved small molecule (ATC A06AH02) targeting OPRD1, OPRK1, and OPRM1; indicated across 6 conditions including constipation disorder and peritoneal neoplasm.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A06AH02
  • Targets: 3 (OPRD1, OPRK1, OPRM1)
  • Indications: 6 conditions
  • Clinical trials: 24
  • Chemistry: 424.5 Da · C25H32N2O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL270190
NameAlvimopan
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5488548
ATCA06AH02
Molecular formulaC25H32N2O4
Molecular weight424.5
InChIKeyUPNUIXSCZBYVBB-JVFUWBCBSA-N

SMILES: C[C@H]1CN(CC[C@@]1(C)C2=CC(=CC=C2)O)C[C@H](CC3=CC=CC=C3)C(=O)NCC(=O)O

IUPAC name: 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid

Also known as: Alvimopan, Alvimopan anhydrous, Alvimopan dihydrate, Anhydrous alvimopan, Entereg, LY-246736, LY-246736 DIHYDRATE, LY246736, ALVIMOPAN, ALVIMOPAN (MONOHYDRATE), alvimopan, Alvimopan (monohydrate)

Patent coverage: 483 distinct patent families (1,781 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
OPRD1δ receptorAntagonist7.920.2%P41143
OPRK1κ receptorAntagonist70%P41145
OPRM1μ receptorAntagonist9.330%P35372

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Voltage-dependent L-type calcium channel subunit alpha-1C, Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK), Mu-type opioid receptor, Delta-type opioid receptor, Kappa-type opioid receptor, Kappa-type opioid receptor.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
OPRM19.5Ki0.32nMCHEMBL_ACT_18101569
OPRM19.33Ki0.47nMCHEMBL_ACT_2119441
OPRM19.11Ki0.77nMCHEMBL_ACT_25041354
OPRM18.77IC501.7nMCHEMBL_ACT_2119469
OPRM18.52IC503nMCHEMBL_ACT_18185735
OPRM18.52AC503nMCHEMBL_ACT_25158209
OPRM18.5IC503.16nMCHEMBL_ACT_18185743
OPRD18.3Ki5.01nMCHEMBL_ACT_18101604
P411448.3Ki5.01nMCHEMBL_ACT_18101639
OPRD17.92Ki12nMCHEMBL_ACT_2119515
OPRK17Ki100nMCHEMBL_ACT_2119489
CACNA1C5.3IC505012nMCHEMBL_ACT_15258105

Target pathways

Aggregated over 3 target gene(s): OPRD1, OPRK1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

PathwayTargetsGenes
Peptide ligand-binding receptors3OPRD1, OPRK1, OPRM1
G alpha (i) signalling events3OPRD1, OPRK1, OPRM1
Interleukin-4 and Interleukin-13 signaling2OPRD1, OPRM1
MECP2 regulates neuronal receptors and channels2OPRK1, OPRM1
Opioid Signalling1OPRM1
G-protein activation1OPRM1

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway3
phospholipase C-activating G protein-coupled receptor signaling pathway3
neuropeptide signaling pathway3
G protein-coupled opioid receptor signaling pathway3
signal transduction3
immune response2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger2
response to nicotine2
eating behavior2
response to ethanol2
sensory perception2
sensory perception of pain2
adult locomotory behavior1
negative regulation of gene expression1

Indications & clinical

Indications

6 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
constipation disorder4MONDO:0002203HP:0002019
peritoneal neoplasm3MONDO:0006901MONDO:0002087
fallopian tube neoplasm3MONDO:0021092MONDO:0002158
ovarian cancer3MONDO:0008170MONDO:0008170
ileus3MONDO:0004567MONDO:0004567

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

Clinical trials

Total trials: 24.

Phase distribution

PhaseTrials
PHASE311
PHASE45
PHASE25
Not specified3

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00708201PHASE4COMPLETEDA Study of Alvimopan for the Management of Postoperative Ileus in Participants Undergoing Radical Cystectomy
NCT02785003PHASE4WITHDRAWNKetamine in Colorectal Surgery
NCT02789111PHASE4COMPLETEDTrial of Alvimopan in Major Spine Surgery
NCT03068975PHASE4TERMINATEDAlvimopan Use in Polytraumatized Patients
NCT04405037PHASE4COMPLETEDAlvimopan as a Rescue Treatment of Postoperative Ileus
NCT03216525PHASE3RECRUITINGAlvimopan Versus Placebo in Patients Undergoing Radical Cystectomy on an Enhanced Recovery Protocol
NCT06703476PHASE3RECRUITINGA Study of Surgical Techniques During Cystectomy
NCT00205842PHASE3COMPLETEDStudy of Alvimopan for the Management of Opioid-induced Postoperative Bowel Dysfunction/Postoperative Ileus
NCT00241722PHASE3COMPLETEDLong-Term Safety Evaluation Of Treatment Of Constipation Due To Opioids Being Taken For Persistent Non-Cancer Pain
NCT00256932PHASE3COMPLETEDTreatment Of Constipation Due To Opioids Being Taken For Persistent Non-Cancer Pain
NCT00259922PHASE3COMPLETEDAlvimopan For The Treatment Of Constipation Due To Opioids Being Taken For Persistent Non-Cancer Pain
NCT00388258PHASE3COMPLETEDStudy of Alvimopan for the Management of Opioid-induced Postoperative Bowel Dysfunction/Postoperative Ileus
NCT00388401PHASE3COMPLETEDStudy of Alvimopan for the Management of Opioid-induced Postoperative Bowel Dysfunction/Postoperative Ileus
NCT00388479PHASE3COMPLETEDStudy of Alvimopan for the Management of Opioid-induced Postoperative Bowel Dysfunction/ Postoperative Ileus
NCT01704651PHASE3COMPLETEDAccelerating Gastrointestinal Recovery
NCT02742181PHASE3TERMINATEDAlvimopan as Rescue in Post op Ileus
NCT00101998PHASE2COMPLETEDStudy Of Alvimopan Drug For Treatment Of Constipation Due To Prescription Pain Medication
NCT00135577PHASE2COMPLETEDStudy 767905/008 Extension Study: Alvimopan for Treatment of Opioid-Induced Bowel Dysfunction in Cancer Pain Subjects
NCT00331045PHASE2TERMINATEDClinical Evaluation Of Alvimopan (SB767905) On Constipation And Related Symptoms Associated With Opioid
NCT01258569PHASE2COMPLETEDEntereg Laparoscopic Colon Resection Study
NCT03352414PHASE2TERMINATEDPhase 2 RCT of Alvimopan vs. Placebo After CRS/HIPEC
NCT01150760Not specifiedCOMPLETEDClinical Outcomes After Bowel Resection in Patients Receiving Alvimopan Versus Patients Not Receiving Alvimopan in the Premier Perspective Database
NCT02218190Not specifiedCOMPLETEDAlvimopan and Ileus in PSF
NCT02379858Not specifiedTERMINATEDGastrointestinal Tract Recovery in Patients Undergoing Open Ventral Hernia Repair

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.

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

MoleculeSourceStatusShared targets
DihydroergotamineChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
PROPOXYPHENEChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
TAFAMIDISChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMIODARONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMLODIPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMOXAPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ASTEMIZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BENZTROPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BUPRENORPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BUTORPHANOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CANNABIDIOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CHLORPROMAZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CINNARIZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CLOTRIMAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CODEINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ECONAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FENTANYLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FLUPHENAZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FLUSPIRILENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
HYDROCODONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
HYDROMORPHONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LANSOPRAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LEVORPHANOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LOPERAMIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LOXAPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MEPERIDINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
METHADONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
METHYLNALTREXONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MICONAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MORPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NAFTOPIDILChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALBUPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALFURAFINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALMEFENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALOXONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALTREXONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NELFINAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OLICERIDINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OXYCODONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OXYMORPHONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PAROXETINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PASIREOTIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PENTAZOCINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PIMOZIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
RALOXIFENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
RITONAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SAMIDORPHANChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SAQUINAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SUNITINIBChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
TAMOXIFENChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
TRAMADOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ASIMADOLINEChEMBLPhase 3OPRD1, OPRK1, OPRM1
ATICAPRANTChEMBLPhase 3OPRD1, OPRK1, OPRM1
CEBRANOPADOLChEMBLPhase 3OPRD1, OPRK1, OPRM1
NAVACAPRANTChEMBLPhase 3OPRD1, OPRK1, OPRM1
TRIMEBUTINEChEMBLPhase 3OPRD1, OPRK1, OPRM1
BREMAZOCINEChEMBLPhase 2OPRD1, OPRK1, OPRM1
CARFENTANILChEMBLPhase 2OPRD1, OPRK1, OPRM1

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