Tavapadon
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Also known as Cvl-751Pf-06649751
Summary
Tavapadon (CHEMBL3697617) is a phase-3 clinical-stage small molecule targeting DRD1; indicated across 3 conditions including parkinson disease and liver disorder.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (DRD1)
- Indications: 3 conditions
- Clinical trials: 18
- Chemistry: 391.3 Da · C19H16F3N3O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3697617 |
| Name | Tavapadon |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 86764100 |
| Molecular formula | C19H16F3N3O3 |
| Molecular weight | 391.3 |
| InChIKey | AKQXQLUNFKDZBN-UHFFFAOYSA-N |
SMILES: CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C
IUPAC name: 1,5-dimethyl-6-[2-methyl-4-[[3-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]pyrimidine-2,4-dione
Also known as: Cvl-751, CVL-751, Pf-06649751, PF-06649751, Tavapadon, TAVAPADON
Patent coverage: 23 distinct patent families (76 SureChEMBL compound mentions), from 3 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 |
|---|---|---|---|---|---|
| DRD1 | D1 receptor | Partial agonist | 8.07 | 0% | P21728 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: D(1A) dopamine receptor.
Bioactivity
ChEMBL activities: 6 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DRD1 | 8.07 | Ki | 8.54 | nM | CHEMBL_ACT_17685037 |
| DRD1 | 8.07 | Ki | 8.54 | nM | CHEMBL_ACT_19118711 |
| DRD1 | 8.07 | Ki | 8.54 | nM | CHEMBL_ACT_25917636 |
| DRD1 | 8.07 | Ki | 8.54 | nM | CHEMBL_ACT_28348700 |
| DRD1 | 7.68 | Ki | 21 | nM | CHEMBL_ACT_17685038 |
| DRD1 | 7.68 | Ki | 21 | nM | CHEMBL_ACT_28348703 |
Target pathways
Aggregated over 1 target gene(s): DRD1.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Dopamine receptors | 1 | DRD1 |
| G alpha (s) signalling events | 1 | DRD1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| temperature homeostasis | 1 |
| conditioned taste aversion | 1 |
| behavioral fear response | 1 |
| response to amphetamine | 1 |
| protein import into nucleus | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase-activating dopamine receptor signaling pathway | 1 |
| G protein-coupled dopamine receptor signaling pathway | 1 |
| synapse assembly | 1 |
| memory | 1 |
| mating behavior | 1 |
| grooming behavior | 1 |
| adult walking behavior | 1 |
| visual learning | 1 |
Indications & clinical
Indications
3 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 |
|---|---|---|---|
| Parkinson disease | 3 | MONDO:0005180 | MONDO:0005180 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| kidney disorder | 1 | MONDO:0005240 | EFO:0003086 |
Clinical trials
Total trials: 18.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 12 |
| PHASE3 | 4 |
| PHASE2 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04201093 | PHASE3 | COMPLETED | Fixed-Dose Trial in Early Parkinson’s Disease (PD) |
| NCT04223193 | PHASE3 | COMPLETED | Flexible-Dose Trial in Early Parkinson’s Disease (PD) |
| NCT04542499 | PHASE3 | COMPLETED | Flexible-Dose, Adjunctive Therapy Trial in Adults With Parkinson’s Disease With Motor Fluctuations (TEMPO-3) |
| NCT04760769 | PHASE3 | COMPLETED | Open-label Trial in Parkinson’s Disease (PD) |
| NCT02847650 | PHASE2 | TERMINATED | Efficacy, Safety and Tolerability of PF-06649751 in Parkinson’s Disease Patients at Early Stage of the Disease |
| NCT01981694 | PHASE1 | COMPLETED | A Phase I Trial to Investigate the Safety and Tolerability of PF-06649751 |
| NCT02066909 | PHASE1 | COMPLETED | A Study To Observe Safety And Blood Concentrations Of PF-06649751 During And Following The Oral Administration Of Multiple Doses Of PF-06649751 In Healthy Adult Western and Japanese Volunteers |
| NCT02224664 | PHASE1 | COMPLETED | Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of PF-06649751 in Parkinson’s Disease |
| NCT02262767 | PHASE1 | COMPLETED | A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of PF-06649751 Co-administered With Trimethobenzamide Hydrochloride in Healthy Subjects |
| NCT02373072 | PHASE1 | COMPLETED | A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of PF-06649751 in Subjects With Idiopathic Parkinson’s Disease |
| NCT04241393 | PHASE1 | COMPLETED | An Open-label Trial to Evaluate Mass Balance of Tavapadon at Steady State in Healthy Subjects |
| NCT04295642 | PHASE1 | COMPLETED | A 2-Part Trial of CVL-751 in Subjects With Parkinson’s Disease |
| NCT05404529 | PHASE1 | COMPLETED | To Evaluate the Pharmacokinetics (PK) and Safety of Tavapadon in Participants With Mild and Moderate Hepatic Impairment Compared to Participants With Normal Hepatic Function |
| NCT05404542 | PHASE1 | COMPLETED | To Evaluate Pharmacokinetics (PK) and Safety of Tavapadon in Participants With Severe Renal Impairment Compared to Participants With Normal Renal Function |
| NCT05581823 | PHASE1 | COMPLETED | Study to Evaluate the Effects of Cytochrome P450 (CYP) 3A4 Inducer Carbamazepine on Tavapadon Pharmacokinetics in Healthy Adult Participants |
| NCT05610189 | PHASE1 | COMPLETED | Multiple-dose Trial to Determine the Clinical Bioequivalence Between Tavapadon Tablets in Participants With Parkinson’s Disease |
| NCT06895356 | PHASE1 | COMPLETED | A Study to Assess the Relative Bioavailability of Oral Tavapadon in Healthy Adult Participants |
| NCT07158827 | Not specified | AVAILABLE | Expanded Access to Tavapadon |
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.
335 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| PIMAVANSERIN | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| TAFAMIDIS | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| TAFENOQUINE | ChEMBL + PubChem | Phase 4 (approved) | DRD1 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | DRD1 |
| ALECTINIB | ChEMBL | Phase 4 (approved) | DRD1 |
| ALPROSTADIL | ChEMBL | Phase 4 (approved) | DRD1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | DRD1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | DRD1 |
| AMLODIPINE | ChEMBL | Phase 4 (approved) | DRD1 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | DRD1 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | DRD1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | DRD1 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | DRD1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | DRD1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | DRD1 |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | DRD1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | DRD1 |
| BENZIODARONE | ChEMBL | Phase 4 (approved) | DRD1 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | DRD1 |
| BENZYDAMINE | ChEMBL | Phase 4 (approved) | DRD1 |
| BEXAROTENE | ChEMBL | Phase 4 (approved) | DRD1 |
| BITHIONOL | ChEMBL | Phase 4 (approved) | DRD1 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | DRD1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | DRD1 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | DRD1 |
| BROMODIPHENHYDRAMINE | ChEMBL | Phase 4 (approved) | DRD1 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | DRD1 |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | DRD1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | DRD1 |
| CASPOFUNGIN | ChEMBL | Phase 4 (approved) | DRD1 |
| CELECOXIB | ChEMBL | Phase 4 (approved) | DRD1 |
| CETRORELIX | ChEMBL | Phase 4 (approved) | DRD1 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | DRD1 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | DRD1 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | DRD1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CLOMIPHENE | ChEMBL | Phase 4 (approved) | DRD1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CLOPIDOGREL | ChEMBL | Phase 4 (approved) | DRD1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | DRD1 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | DRD1 |
| COBIMETINIB | ChEMBL | Phase 4 (approved) | DRD1 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | DRD1 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | DRD1 |
| DANAZOL | ChEMBL | Phase 4 (approved) | DRD1 |
| DEQUALINIUM | ChEMBL | Phase 4 (approved) | DRD1 |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | DRD1 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | DRD1 |
| DIBENZEPIN | ChEMBL | Phase 4 (approved) | DRD1 |
| DICYCLOMINE | ChEMBL | Phase 4 (approved) | DRD1 |
Related Atlas pages
- Genes: DRD1
- Diseases: Parkinson disease
- Drugs: Desloratadine, Dihydroergotamine, Paliperidone, Pimavanserin, Regorafenib, Tafamidis, Tafenoquine, Acetophenazine, Alectinib, Alprostadil, Amiodarone, Amitriptyline, Amlodipine, Amoxapine, Apomorphine, Aripiprazole, Asenapine, Astemizole, Azelastine, Bazedoxifene, Benperidol, Benziodarone, Benztropine, Benzydamine, Bexarotene, Bithionol, Bosutinib, Brexpiprazole, Bromocriptine, Bromodiphenhydramine, Brompheniramine, Cabergoline, Cabozantinib, Cannabidiol, Cariprazine, Carvedilol, Caspofungin, Celecoxib, Cetrorelix, Chlorpromazine, Chlorprothixene, Cinnarizine, Cisapride, Citalopram, Clemastine, Clomiphene, Clomipramine, Clopidogrel, Clotrimazole, Clozapine, Cobimetinib, Cyclizine, Cyproheptadine, Danazol, Dequalinium, Desogestrel, Dexbrompheniramine, Dibenzepin, Dicyclomine