Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor‐Positive Allosteric Modulator (D1PAM), in Healthy Subjects

• Published in: Clinical pharmacology in drug development Vol. 10; no. 4; pp. 393 - 403
• Main Authors: Wilbraham, Darren, Biglan, Kevin M., Svensson, Kjell A., Tsai, Max, Kielbasa, William
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.04.2021; John Wiley and Sons Inc
• Subjects: Administration, Oral; Adolescent; Adult; Aged; Allosteric Regulation - drug effects; Blood pressure; Blood Pressure - drug effects; Cohort Studies; Dopamine; Dopamine Agents - administration & dosage; Dopamine Agents - pharmacokinetics; Dopamine Agents - pharmacology; Dose-Response Relationship, Drug; Double-Blind Method; Female; Heart Rate - drug effects; Humans; Isoquinolines - administration & dosage; Isoquinolines - pharmacokinetics; Isoquinolines - pharmacology; Male; mevidalen (LY3154207); Middle Aged; Original Manuscript; Pharmacokinetics; Receptors, Dopamine D1 - drug effects; Receptors, Dopamine D1 - metabolism; safety; tolerability; Young Adult; pharmacokinetics; dopamine; mevidalen (LY3154207); safety; tolerability

Activation of the brain dopamine D1 receptor has attracted attention because of its promising role in neuropsychiatric diseases. Although efforts to develop D1 agonists have been challenging, a positive allosteric modulator (PAM), represents an attractive approach with potential better drug‐like pro...