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CPL500036 is a potent, selective and orally bioavailable small molecule inhibitor of phosphodiesterase 10A (PDE10A), developed primarily for the treatment of schizophrenia and drug-induced dyskinesia in Parkinson's disease. It demonstrates high selectivity for PDE10A with an IC50 of 1 nM and has shown good brain penetration and safety profile distinct from marketed antipsychotics. In addition to its primary mechanism as a PDE10A inhibitor, it acts as a negative allosteric modulator at the muscarinic M2 receptor at much higher concentrations. The drug is being developed by Celon Pharma in collaboration with The National Centre for Research and Development. As of early 2025, it has completed phase II clinical trials in both schizophrenia and levodopa-induced dyskinesia associated with Parkinson's disease[1][2][3][4][5][7].
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