Tavapadon (CVL-751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist.

Administered subcutaneously to captive-bred macaques, Tavapadon at a dose of 0.1 mg/kg results in a mean maximal unbound plasma concentration of 8 nM, with peak levels reached 3 hours post-administration. At lower doses (0.02 and 0.04 mg/kg; s.c.), only the 0.04 mg/kg dosage significantly increases locomotor activity, while the 0.02 mg/kg dosage exhibits minimal to no impact. Furthermore, a 0.04 mg/kg dose of Tavapadon not only enhances locomotor activity but also notably improves parkinsonian disability scores, with maximum benefits observed at 110 minutes after administration. Higher doses of Tavapadon (0.1 and 0.15 mg/kg; s.c.) demonstrate a statistically significant improvement in locomotor activity compared to a vehicle control [1].