molecules of the month


oral, CNS-penetrant, picomolar PDE1 inhibitor

Ph. I/II in neurology and heart failure

from literature starting point, LBDD and SBDD


Intra-Cellular Therapies, New York, NY

lenrispodun chemical structure, oral, CNS-penetrant, picomolar PDE1 inhibitor - Intra-Cellular Therapies, New York, NY
6 mins read

Context. Lenrispodun (Intra-Cellular Therapies) is a phosphodiesterase (PDE) type 1 (PDE1) inhibitor being developed for CNS and non-CNS disorders, including heart failure, and cancer. Studies to identify PDE inhibitors date back at least 30 years, and at least 10 drugs have been approved targeting other PDE proteins (spearheaded by the PDE5 inhibitor sildenafil [Viagra]). However, no PDE1 inhibitors have been approved for at least two decades, despite the existence of the classic PDE1 inhibitor vinpocetine (structure), and reports of other PDE1-targeting agents during this time. This may be attributable to the general complexity of PDE proteins, as well as the high structural similarity among over 100 isoforms which may hinder selectivity, a challenge Intra-Cellular Therapies scientists are determined to overcome.…

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