Landiolol
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Also known as AOP-200704AOP200704LDLL-600LDLL600ONO-1101Landiolol HCl
Summary
Landiolol (CHEMBL1742466) is an approved small molecule (ATC C07AB14) targeting ADRB1; indicated across 7 conditions including cardiovascular disorder and atrial fibrillation.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C07AB14
- Targets: 1 (ADRB1)
- Indications: 7 conditions
- Clinical trials: 16
- Chemistry: 509.6 Da · C25H39N3O8
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1742466 |
| Name | Landiolol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 114905 |
| ATC | C07AB14 |
| Molecular formula | C25H39N3O8 |
| Molecular weight | 509.6 |
| InChIKey | WMDSZGFJQKSLLH-RBBKRZOGSA-N |
SMILES: CC1(OC[C@H](O1)COC(=O)CCC2=CC=C(C=C2)OC[C@H](CNCCNC(=O)N3CCOCC3)O)C
IUPAC name: [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4-[(2S)-2-hydroxy-3-[2-(morpholine-4-carbonylamino)ethylamino]propoxy]phenyl]propanoate
Also known as: AOP-200704, AOP200704, Landiolol, LDLL-600, LDLL600, ONO-1101, LANDIOLOL, landiolol, Landiolol HCl
Parent form; salt/anhydrous children: CHEMBL2362410
Patent coverage: 531 distinct patent families (2,131 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).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| ADRB1 | β1-adrenoceptor | Antagonist | 7 | 0% | P08588 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): ADRB1.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | ADRB1 |
| Signaling by GPCR | 1 | ADRB1 |
| Class A/1 (Rhodopsin-like receptors) | 1 | ADRB1 |
| Amine ligand-binding receptors | 1 | ADRB1 |
| GPCR downstream signalling | 1 | ADRB1 |
| Adrenoceptors | 1 | ADRB1 |
| G alpha (s) signalling events | 1 | ADRB1 |
| GPCR ligand binding | 1 | ADRB1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of heart rate by epinephrine-norepinephrine | 1 |
| positive regulation of the force of heart contraction by epinephrine-norepinephrine | 1 |
| diet induced thermogenesis | 1 |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | 1 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| response to cold | 1 |
| positive regulation of cardiac muscle cell apoptotic process | 1 |
| heat generation | 1 |
| negative regulation of multicellular organism growth | 1 |
| fear response | 1 |
| positive regulation of MAPK cascade | 1 |
| regulation of circadian sleep/wake cycle, sleep | 1 |
| brown fat cell differentiation | 1 |
| adenylate cyclase-activating adrenergic receptor signaling pathway | 1 |
| positive regulation of cold-induced thermogenesis | 1 |
Indications & clinical
Indications
7 indications (0 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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| cardiovascular disorder | 3 | MONDO:0004995 | EFO:0000319 |
| atrial fibrillation | 3 | MONDO:0004981 | EFO:0000275 |
| toxic shock syndrome | 3 | MONDO:0001881 | EFO:0006834 |
| atrial flutter | 1 | MONDO:0005310 | EFO:0003911 |
| cardiac arrest | 1 | MONDO:0000745 | EFO:0009492 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 16.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 6 |
| PHASE2 | 4 |
| PHASE4 | 3 |
| PHASE2/PHASE3 | 1 |
| PHASE1/PHASE2 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06793670 | PHASE4 | RECRUITING | Landiolol in Mitral Valve Surgery |
| NCT07168421 | PHASE4 | RECRUITING | LANdiolol to Avoid TAchycardia in Patients at Risk for Cardiovascular Events Undergoing Major Non-cardiac Surgery |
| NCT04223739 | PHASE4 | UNKNOWN | Comparison of Two Strategies for the Management of Atrial Fibrillation After Cardiac Surgery |
| NCT04748796 | PHASE3 | RECRUITING | Comparison of Landiolol Versus Standard of Care for Prevention of Mortality in Patients Hospitalized for a Septic Shock With Hypercontractility |
| NCT04931225 | PHASE3 | RECRUITING | LANdiolol MIcrocirculatory Effects During Septic chOc (MILANOS) |
| NCT00212654 | PHASE2/PHASE3 | COMPLETED | Controlled Study of ONO-1101 in Patients With Postoperative Tachyarrhythmias in Japan |
| NCT00924586 | PHASE3 | COMPLETED | Study of ONO-1101 in Patients Scheduled for Multi-Slice Computed Tomography (CT) |
| NCT03779178 | PHASE3 | COMPLETED | Landiolol in Postoperative Atrial Fibrillation |
| NCT04607122 | PHASE3 | COMPLETED | Prevention of Atrial Fibrillation by Low-dose Landiolol Administration After Cardiac Surgery |
| NCT05084118 | PHASE3 | UNKNOWN | Landiolol for Prevention of Postoperative Atrial Fibrillation in Patients Undergoing Cardiac Surgery |
| NCT00212680 | PHASE2 | COMPLETED | Controlled Study of ONO-1101 in Patients With Postoperative Tachyarrhythmias in Japan |
| NCT00311038 | PHASE2 | COMPLETED | Pilot Study of ONO-1101 in Patients Scheduled for Multi-slice CT |
| NCT00560209 | PHASE2 | COMPLETED | Study of ONO-1101 in Patients Scheduled for Coronary Angiography |
| NCT01313143 | PHASE2 | COMPLETED | A Short Term Pharmacokinetic, Pharmacodynamic and Tolerability Study to Compare AOP200704 vs. Esmolol |
| NCT05554978 | PHASE1/PHASE2 | UNKNOWN | Beta-blockade With Landiolol in Out-of-hospital Cardiac Arrest |
| NCT01741519 | PHASE1 | COMPLETED | Long-term PK and Safety/Tolerability Testing LDLL600 Against Esmolol in Healthy Volunteers |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
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.
180 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| OLODATEROL | ChEMBL + PubChem | Phase 4 (approved) | ADRB1 |
| TAMSULOSIN | ChEMBL + PubChem | Phase 4 (approved) | ADRB1 |
| ACEBUTOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| ALBUTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ARFORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ATENOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BETAXOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BISOPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARTEOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CELIPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| CODEINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DARIFENACIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| DECITABINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | ADRB1 |
| DULOXETINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| EBASTINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | ADRB1 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | ADRB1 |
| EPINEPHRINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ERGOTAMINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ESMOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| FENOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| FORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| INDACATEROL | ChEMBL | Phase 4 (approved) | ADRB1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | ADRB1 |
| ISOCONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LABETALOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | ADRB1 |
| LEVOBUNOLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | ADRB1 |
| METARAMINOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| METHYLERGONOVINE | ChEMBL | Phase 4 (approved) | ADRB1 |
| METOPROLOL | ChEMBL | Phase 4 (approved) | ADRB1 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | ADRB1 |
Related Atlas pages
- Genes: ADRB1
- Diseases: cardiovascular disorder, atrial fibrillation, toxic shock syndrome
- Drugs: Olodaterol, Tamsulosin, Acebutolol, Albuterol, Amiodarone, Amitriptyline, Arformoterol, Aripiprazole, Astemizole, Atenolol, Azelastine, Benfluorex, Benperidol, Benzbromarone, Bepridil, Betaxolol, Bisoprolol, Brexpiprazole, Bromocriptine, Candesartan Cilexetil, Cariprazine, Carteolol, Carvedilol, Celiprolol, Chlorhexidine, Chlorprothixene, Cinacalcet, Clemastine, Clomipramine, Clotrimazole, Codeine, Darifenacin, Daunorubicin, Decitabine, Diethylstilbestrol, Dobutamine, Domperidone, Duloxetine, Ebastine, Econazole, Efavirenz, Epalrestat, Epinephrine, Ergotamine, Esmolol, Fenoterol, Fluspirilene, Formoterol, Indacaterol, Indocyanine Green Acid Form, Isoconazole, Isoproterenol, Labetalol, Lasofoxifene, Levobunolol, Lorcaserin, Metaraminol, Methylergonovine, Metoprolol