Levodopa
drugOn this page
Also known as BendopaBrocadopaCvt-301DoparInbrijaLarodopaLevodopa component of carbilevLevodopa component of corbiltaLevodopa component of crexontLevodopa component of dhivyLevodopa component of dopasnapLevodopa component of duopaLevodopa component of ipx-203Levodopa component of ipx203Levodopa component of parcopaLevodopa component of rytaryLevodopa component of sinemetLevodopa component of stalevoLevodopum
Summary
Levodopa (CHEMBL1009) is an approved small-molecule prodrug (ATC N04BA01) targeting GPR143; indicated across 27 conditions including parkinson disease and restless legs syndrome.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: N04BA01
- Targets: 1 (GPR143)
- Indications: 27 conditions
- Clinical trials: 151
- Chemistry: 197.19 Da · C9H11NO4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1009 |
| Name | Levodopa |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 6047 |
| ChEBI | CHEBI:15765 |
| ATC | N04BA01 |
| Molecular formula | C9H11NO4 |
| Molecular weight | 197.19 |
| InChIKey | WTDRDQBEARUVNC-LURJTMIESA-N |
SMILES: C1=CC(=C(C=C1C[C@@H](C(=O)O)N)O)O
IUPAC name: (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid
ChEBI definition: An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson’s disease
Pharmacological roles (ChEBI): prodrug, hapten, neurotoxin, antiparkinson drug, dopaminergic agent, antidyskinesia agent, allelochemical.
Other ChEBI roles (chemical / environmental): plant growth retardant, human metabolite, mouse metabolite, plant metabolite.
Also known as: Bendopa, Brocadopa, Cvt-301, Dopar, Inbrija, Larodopa, Levodopa, Levodopa component of carbilev, Levodopa component of corbilta, Levodopa component of crexont, Levodopa component of dhivy, Levodopa component of dopasnap
Patent coverage: 34,622 distinct patent families (103,854 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 103,453 (100%) 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 |
|---|---|---|---|---|---|
| GPR143 | GPR143 | Agonist | 0% | P51810 |
Broader ChEMBL bioactivity targets: 20 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Lysine-specific demethylase 4E, Ubiquitin carboxyl-terminal hydrolase 2, ATP-dependent DNA helicase Q1, 4’-phosphopantetheinyl transferase ffp, Tyrosine-protein kinase Fyn, Epidermal growth factor receptor, Prostaglandin G/H synthase 1, 5-hydroxytryptamine receptor 2A, Prostaglandin G/H synthase 2.
Bioactivity
ChEMBL activities: 13 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| Q9F4F7 | 8.2 | Potency | 6.3 | nM | CHEMBL_ACT_4801455 |
| P08482 | 7.15 | Potency | 70.8 | nM | CHEMBL_ACT_4807440 |
| HSD17B10 | 6.5 | Potency | 316.2 | nM | CHEMBL_ACT_4865385 |
| TDP1 | 6.3 | Potency | 501.2 | nM | CHEMBL_ACT_3939857 |
| PTGS1 | 6.17 | AC50 | 670 | nM | CHEMBL_ACT_25206310 |
| FYN | 5.67 | IC50 | 2146 | nM | CHEMBL_ACT_7765936 |
| P12530 | 5.65 | IC50 | 2258 | nM | CHEMBL_ACT_7765858 |
| EGFR | 5.54 | IC50 | 2880 | nM | CHEMBL_ACT_7765934 |
| LCK | 5.43 | IC50 | 3729 | nM | CHEMBL_ACT_7765940 |
| HSD17B10 | 5.4 | Potency | 3981 | nM | CHEMBL_ACT_4849600 |
| PTGS1 | 5.39 | AC50 | 4110 | nM | CHEMBL_ACT_25205379 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4131746 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4519269 |
Target pathways
Aggregated over 1 target gene(s): GPR143.
Top Reactome pathways
3 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Amine ligand-binding receptors | 1 | GPR143 |
| G alpha (q) signalling events | 1 | GPR143 |
| Regulation of MITF-M-dependent genes involved in pigmentation | 1 | GPR143 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| eye pigment biosynthetic process | 1 |
| signal transduction | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| visual perception | 1 |
| melanosome localization | 1 |
| melanosome transport | 1 |
| melanosome organization | 1 |
| regulation of melanosome transport | 1 |
| regulation of melanosome organization | 1 |
| neuropeptide signaling pathway | 1 |
Indications & clinical
Indications
27 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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| Parkinson disease | 4 | MONDO:0005180 | MONDO:0005180 |
| restless legs syndrome | 3 | MONDO:0005391 | EFO:0004270 |
| stroke disorder | 3 | MONDO:0005098 | EFO:0000712 |
| amblyopia | 3 | MONDO:0001020 | MONDO:0001020 |
| cocaine dependence | 2 | MONDO:0005186 | EFO:0002610 |
| age-related macular degeneration | 2 | MONDO:0005150 | EFO:0001365 |
| autism spectrum disorder | 2 | MONDO:0005258 | EFO:0003756 |
| spinal cord injury | 2 | MONDO:0043797 | EFO:1001919 |
| aphasia | 2 | MONDO:0000598 | HP:0002381 |
| post-traumatic stress disorder | 2 | MONDO:0005146 | EFO:0001358 |
| albinism | 2 | MONDO:0043209 | MONDO:0043209 |
| Angelman syndrome | 2 | MONDO:0007113 | MONDO:0007113 |
| oculocutaneous albinism | 2 | MONDO:0018910 | MONDO:0018910 |
| retinitis pigmentosa | 2 | MONDO:0019200 | MONDO:0019200 |
| Tourette syndrome | 1 | MONDO:0007661 | EFO:0004895 |
| orthostatic hypotension | 1 | MONDO:0005469 | EFO:0005252 |
| nicotine dependence | 1 | MONDO:0008575 | EFO:0003768 |
| amyotrophic lateral sclerosis | 1 | MONDO:0004976 | MONDO:0004976 |
| asthma | 1 | MONDO:0004979 | MONDO:0004979 |
| brain injury | 0 | MONDO:0043510 | MONDO:0043510 |
| diabetic retinopathy | 0 | MONDO:0005266 | EFO:0003770 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 151.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 38 |
| PHASE2 | 35 |
| PHASE1 | 30 |
| Not specified | 17 |
| PHASE3 | 16 |
| PHASE2/PHASE3 | 8 |
| PHASE1/PHASE2 | 5 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06075771 | PHASE4 | RECRUITING | Dopaminergic Therapy for Anhedonia - 2 |
| NCT06234995 | PHASE4 | RECRUITING | Cortical Electrophysiology of Response Inhibition in Parkinson’s Disease |
| NCT00102284 | PHASE4 | TERMINATED | Neuromodulation and Language Acquisition (Project Stage Ia) |
| NCT00102869 | PHASE4 | COMPLETED | Dopaminergic Enhancement of Learning and Memory in Aphasia |
| NCT00103805 | PHASE4 | COMPLETED | Improved Language Acquisition With Levodopa |
| NCT00111371 | PHASE4 | UNKNOWN | Dopaminergic Enhancement of Learning and Memory in Healthy Adults and Patients With Dyslexia |
| NCT00125567 | PHASE4 | COMPLETED | Stalevo in Early Wearing-Off Patients |
| NCT00143026 | PHASE4 | COMPLETED | Study to Compare the Effect of Treatment With Carbidopa/Levodopa/Entacapone on the Quality of Life of Patients With Parkinson’s Disease. This Study is Not Recruiting in the United States |
| NCT00153972 | PHASE4 | COMPLETED | Dopamine Turnover Rate as Surrogate Parameter for Diagnosis of Early Parkinson’s Disease |
| NCT00219284 | PHASE4 | COMPLETED | Effects of Carbidopa/Levodopa/Entacapone on Motor Function and Quality of Life in Patients With Parkinson’s Disease |
| NCT00306124 | PHASE4 | UNKNOWN | Dopaminergic Enhancement of Learning and Memory in Healthy Adults and Patients With Dementia/Mild Cognitive Impairment |
| NCT00391898 | PHASE4 | COMPLETED | Efficacy of Levodopa/Carbidopa/Entacapone vs Levodopa/Carbidopa in Parkinson’s Disease Patients With Early Wearing-off |
| NCT00485069 | PHASE4 | COMPLETED | REQUIP (Ropinirole Hydrochloride) IR Long-Term Phase 4 Study |
| NCT00601978 | PHASE4 | WITHDRAWN | Carbidopa/Levodopa Versus Carbidopa/Levodopa/Entacapone on Markers of Event Related Potentials (ERPs) in Patients With Idiopathic Parkinson’s Disease (PD) and End-of-dose Wearing Off |
| NCT00642356 | PHASE4 | TERMINATED | Carbidopa/Levodopa/Entacapone Versus Immediate Release (IR) Carbidopa/Levodopa on Non-motor Symptoms in Patients With Idiopathic Parkinson’s Disease and Demonstrating Non-motor Symptoms of Wearing Off |
| NCT00812760 | PHASE4 | COMPLETED | Effect of Levodopa on Human Multifocal Electroretinogram |
| NCT00888186 | PHASE4 | COMPLETED | Different Dyskinesias in Parkinson’s Disease and Their Relation to Levodopa Pharmacokinetics |
| NCT00906828 | PHASE4 | COMPLETED | Pharmacokinetics of Levodopa/Carbidopa Infusion With and Without Oral Catechol-O-methyl Transferase (COMT) Inhibitors |
| NCT00914134 | PHASE4 | COMPLETED | Duodenal Levodopa Infusion, Quality of Life and Autonomic Nervous System in Parkinson’s Disease |
| NCT01327261 | PHASE4 | COMPLETED | Fasting Comparative Bioavailability of Two Tablet Formulations of Levodopa /Benserazide in Healthy Volunteers |
| NCT01494532 | PHASE4 | COMPLETED | A Fixed Dose Study of Ropinirole Prolonged Release as Adjunctive Treatment in Patients With Advanced Parkinson’s Disease |
| NCT01683253 | PHASE4 | COMPLETED | Remission of ICD by Switching Dopamine Agonist to Levodopa/Carbidopa |
| NCT01770145 | PHASE4 | COMPLETED | Apokyn for Motor IMProvement of Morning AKinesia Trial (AM IMPAKT) |
| NCT01951105 | PHASE4 | COMPLETED | Effect of L-dopa In Subacute Back Pain Population |
| NCT02346630 | PHASE4 | WITHDRAWN | Combining Robotic-Assisted Therapy and Pharmacotherapy in Post-Stroke Rehabilitation |
| NCT02513485 | PHASE4 | COMPLETED | Inflammation-related Alterations in Neurocircuitry: Reversal With Levodopa |
| NCT02560389 | PHASE4 | COMPLETED | Dopamine Enhancement of Fear Extinction Learning in PTSD (1R21MH108753) |
| NCT02744391 | PHASE4 | COMPLETED | A Study of L-DOPA for Depression and Slowing in Older Adults |
| NCT02769793 | PHASE4 | COMPLETED | Efficacy of Levodopa/Benserazide Dispersible Tablet on Response Fluctuations in PD Patients With Delayed ON |
| NCT02847442 | PHASE4 | COMPLETED | Efficacy and Safety of Opicapone in Clinical Practice |
| NCT03761030 | PHASE4 | TERMINATED | L-DOPA vs. Placebo for Depression and Psychomotor Slowing in Older Adults |
| NCT04493320 | PHASE4 | TERMINATED | 1/2-Dopaminergic Dysfunction in Late-Life Depression (The D3 Study) |
| NCT04650217 | PHASE4 | TERMINATED | Levodopa and Exercise for Older Adults With Depression and Psychomotor Slowing |
| NCT04723147 | PHASE4 | COMPLETED | DTA (Dopaminergic Therapy for Anhedonia) Study |
| NCT04742348 | PHASE4 | WITHDRAWN | Research on Translational Outcomes of Alcohol (Project RETRO) |
| NCT04990284 | PHASE4 | COMPLETED | eArly levoDopa With Opicapone in Parkinson’s paTients wIth motOr fluctuatioNs. |
| NCT06115538 | PHASE4 | UNKNOWN | Comparison of Dopamin Level in Idiopathic Parkinson’s Patients |
| NCT06236230 | PHASE4 | UNKNOWN | Basic and Clinical Studies of Levodopa/Carbidopa/Entacapone in the Treatment of Early Parkinson’s Disease |
| NCT06785298 | PHASE2/PHASE3 | RECRUITING | Fexofenadine as Adjuvant Therapy in Parkinson Disease |
| NCT07229651 | PHASE2/PHASE3 | RECRUITING | Metformin in Parkinson Disease |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 6 clinical and 25 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Genes: GPR143
- Diseases: Parkinson disease, restless legs syndrome, stroke disorder, amblyopia