Mevidalen (LY-3154207) is an investigational dopaminergic drug under development for the treatment of Lewy body disease, including Parkinson’s disease. It functions as a selective positive allosteric modulator (PAM) of the dopamine D1 receptor, offering a novel approach to managing symptoms associated with these conditions. The molecule has demonstrated wakefulness-promoting effects in sleep-deprived individuals, which could be beneficial for patients experiencing excessive daytime sleepiness, a common symptom in Lewy body disease.
In preclinical studies, mevidalen has shown efficacy in enhancing dopamine signaling, which is crucial for motor control, cognition, and mood regulation. However, the drug’s metabolism primarily involves the CYP3A4 enzyme, posing a potential risk for drug-drug interactions (DDIs) with CYP3A4 inhibitors and inducers.
As of November 2023, mevidalen is in phase II clinical trials for Lewy body disease. Despite its promise, mevidalen has been associated with side effects including increased heart rate and blood pressure, insomnia, dizziness, nausea, vomiting, anxiety, fatigue, headaches, palpitations, and contact dermatitis. Additionally, there is a risk of falls in patients with dementia.
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| Other Names | CHEMBL4468760, SCHEMBL21489570 |
|---|---|
| IUPAC Name | 2-(2, 6-dichlorophenyl)-1-[(1S, 3R)-3-(hydroxymethyl)-1-methyl-5-(1-methylpyrazol-4-yl)-3, 4-dihydro-1H-isoquinolin-2-yl]ethanone |
| CAS | 2379422-72-5 |
| Molecular Weight | 444.3 |
| Molecular Formula | C23H23Cl2N3O2 |
| SMILES | C[C@H]1C2=CC=CC(=C2C[C@@H](N1C(=O)CC3=C(C=CC=C3Cl)Cl)CO)C4=CN(N=C4)C |