Levosalbutamol
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Also known as Albuterol (r)-formASF-1096LevalbuterolR-salbutamolSID11111805SID11111806SID11112645SID11113612R-(-)salbutamolLevalbuterol hydrochloride
Summary
Levosalbutamol (CHEMBL1002) is an approved small molecule targeting ADRB1; indicated across 2 conditions including chronic obstructive pulmonary disease and asthma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- Targets: 1 (ADRB1)
- Indications: 2 conditions
- Clinical trials: 19
- Chemistry: 239.31 Da · C13H21NO3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1002 |
| Name | Levosalbutamol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 123600 |
| ChEBI | CHEBI:8746 |
| Molecular formula | C13H21NO3 |
| Molecular weight | 239.31 |
| InChIKey | NDAUXUAQIAJITI-LBPRGKRZSA-N |
SMILES: CC(C)(C)NC[C@@H](C1=CC(=C(C=C1)O)CO)O
IUPAC name: 4-[(1R)-2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
Also known as: Albuterol (r)-form, ASF-1096, Levalbuterol, Levosalbutamol, R-salbutamol, SID11111805, SID11111806, SID11112645, SID11113612, R-(-)salbutamol, LEVOSALBUTAMOL, Levalbuterol hydrochloride
Parent form; salt/anhydrous children: CHEMBL1201061, CHEMBL3989589, CHEMBL3989693
Patent coverage: 7,464 distinct patent families (27,028 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 26,790 (99%) of the total. 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 | Partial agonist | 4.7 | 0% | P08588 |
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Thyrotropin receptor, Beta-2 adrenergic receptor, Cytochrome P450 2D6, Nuclear factor NF-kappa-B p105 subunit, Cytochrome P450 1A2, Hypoxia-inducible factor 1-alpha.
Bioactivity
ChEMBL activities: 28 potent at pChembl ≥ 5 of 29 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HIF1A | 8.49 | Potency | 3.2 | nM | CHEMBL_ACT_4129681 |
| HIF1A | 8.49 | Potency | 3.2 | nM | CHEMBL_ACT_4518717 |
| HIF1A | 8.1 | Potency | 7.9 | nM | CHEMBL_ACT_4131708 |
| HIF1A | 8.1 | Potency | 7.9 | nM | CHEMBL_ACT_4519231 |
| TSHR | 6.9 | Potency | 125.9 | nM | CHEMBL_ACT_3911195 |
| ADRB2 | 6.84 | EC50 | 145 | nM | CHEMBL_ACT_7995363 |
| ADRB2 | 6.84 | EC50 | 144.5 | nM | CHEMBL_ACT_7995388 |
| ADRB2 | 6.56 | EC50 | 275 | nM | CHEMBL_ACT_7995371 |
| ADRB2 | 6.56 | EC50 | 275.4 | nM | CHEMBL_ACT_7995394 |
| ADRB2 | 6.34 | EC50 | 457 | nM | CHEMBL_ACT_7995373 |
| ADRB2 | 6.34 | EC50 | 457.1 | nM | CHEMBL_ACT_7995396 |
| TSHR | 6.3 | Potency | 501.2 | nM | CHEMBL_ACT_3912697 |
| TSHR | 6.3 | Potency | 501.2 | nM | CHEMBL_ACT_4723059 |
| TSHR | 6 | Potency | 1000 | nM | CHEMBL_ACT_3924090 |
| HIF1A | 6 | Potency | 1000 | nM | CHEMBL_ACT_4132762 |
| HIF1A | 6 | Potency | 1000 | nM | CHEMBL_ACT_4519531 |
| TSHR | 6 | Potency | 1000 | nM | CHEMBL_ACT_4698749 |
| TSHR | 5.9 | Potency | 1259 | nM | CHEMBL_ACT_3918877 |
| TSHR | 5.9 | Potency | 1259 | nM | CHEMBL_ACT_4616807 |
| CYP2D6 | 5.9 | Potency | 1259 | nM | CHEMBL_ACT_4965694 |
| ADRB2 | 5.42 | Ki | 3802 | nM | CHEMBL_ACT_7995370 |
| ADRB2 | 5.42 | Ki | 3802 | nM | CHEMBL_ACT_7995393 |
| ADRB2 | 5.33 | Ki | 4677 | nM | CHEMBL_ACT_7995372 |
| ADRB2 | 5.33 | Ki | 4677 | nM | CHEMBL_ACT_7995395 |
| ADRB2 | 5.25 | Ki | 5623 | nM | CHEMBL_ACT_7995359 |
| ADRB2 | 5.25 | Ki | 5623 | nM | CHEMBL_ACT_7995384 |
| NFKB1 | 5.2 | Potency | 6310 | nM | CHEMBL_ACT_3671877 |
| NFKB1 | 5.2 | Potency | 6310 | nM | CHEMBL_ACT_4589025 |
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
2 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 |
|---|---|---|---|
| chronic obstructive pulmonary disease | 3 | MONDO:0005002 | EFO:0000341 |
| asthma | 3 | MONDO:0004979 | MONDO:0004979 |
Clinical trials
Total trials: 19.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 7 |
| PHASE4 | 6 |
| PHASE2 | 4 |
| Not specified | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00819637 | PHASE4 | TERMINATED | A Pilot Study to Determine the Most Effective Dose of Arformoterol for Treating Acute Asthmatic Patients |
| NCT00830882 | PHASE4 | WITHDRAWN | Peak Bronchoprotection Conferred by Levosalbutamol and Racemic Salbutamol |
| NCT00831376 | PHASE4 | COMPLETED | Trough Bronchoprotection Conferred by Levosalbutamol and Racemic Salbutamol |
| NCT01151579 | PHASE4 | COMPLETED | Effect of Nebulized Bronchodilators on Heart Rate |
| NCT02170532 | PHASE4 | COMPLETED | Aerosolized Beta-Agonist Isomers in Asthma |
| NCT05173584 | PHASE4 | UNKNOWN | Levalbuterol Compared to Albuterol Regarding Cardiac Side Effects and Potassium Lowering Effects. |
| NCT00073840 | PHASE3 | COMPLETED | Study of Levalbuterol, Racemic Albuterol and Placebo in Subjects Twelve Years of Age and Older With Asthma |
| NCT00667407 | PHASE3 | COMPLETED | Efficacy and Safety of Levalbuterol Versus Racemic Albuterol in Asthma |
| NCT00685126 | PHASE3 | COMPLETED | Study of Levalbuterol and Racemic Albuterol in Pediatric Subjects With Reactive Airways Disease (RAD) |
| NCT00809757 | PHASE3 | COMPLETED | A Safety, Efficacy and Tolerability Study in Pediatric Subjects With Asthma |
| NCT02414854 | PHASE3 | COMPLETED | Evaluation of Dupilumab in Patients With Persistent Asthma (Liberty Asthma Quest) |
| NCT02528214 | PHASE3 | COMPLETED | Evaluation of Dupilumab in Patients With Severe Steroid Dependent Asthma |
| NCT04446637 | PHASE3 | WITHDRAWN | Acute Bronchodilator Effects of Ipratropium/Levosalbutamol 20/50 mcg Fixed Dose Combination vs Salbutamol 100 mcg Inhaler Plus Ipratropium 20 mcg Inhalation Aerosol Free Combination in Patients With Stable COPD |
| NCT00583947 | PHASE2 | COMPLETED | A Safety and Tolerability Study of Arformoterol Tartrate Inhalation Solution in Pediatric Subjects |
| NCT01312961 | PHASE2 | COMPLETED | Efficacy, Safety, and Tolerability of Dupilumab in Patients With Persistent Moderate to Severe Eosinophilic Asthma |
| NCT01656811 | PHASE2 | COMPLETED | A Study of Daily Dosing With Levalbuterol, Racemic Albuterol, and Placebo in Pediatric Subjects With Asthma |
| NCT01854047 | PHASE2 | COMPLETED | An Evaluation of Dupilumab in Patients With Moderate to Severe Uncontrolled Asthma |
| NCT01833026 | Not specified | COMPLETED | COPD Assessment and Management Bundle Versus Usual Care |
| NCT02802111 | Not specified | COMPLETED | Change in Oxygen Consumption Following Inhalation Beta Agonists in Healthy Adults |
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: chronic obstructive pulmonary disease, asthma
- 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