NP-18-3 Oral Capsule - Phase 2a clinical program

5-HT2B Antagonist and Sigma-1/Sigma-2 agonist/antagonist

Oral Swallowed Capsule - Phase 1 & 2 clinical studies

The figure on the right shows the docked pose of NP-18-3

in the binding pocket of the Sigma-1 receptor (PDB ID: 6DK1)

NP-18-3 is an orally-bioavailable selective full antagonist to the 5-Hydroxytryptamine receptor 2B (5-HT2B) and a ligand for the Sigma-1 receptor. NP-18-2 is a highly selective for 5-HT2B (Ki=3.4 nM) with more than 500-fold differences in affinity for 5-HT2BR compared with all other 5-HT receptor subtypes tested except for the 5-HT1A receptor (5-HT1A, Ki = 100nM). NP-18-2 also demonstrates selective binding to the Sigma-2 receptor (Ki = 42 nM) and Sigma-1 receptor (Ki = 100 nM) in radioligand binding assays.

An oral capsule formulation of NP-18-3 has completed multiple Phase 1 and 2 clinical studies and is currently in Phase 2 clinical development.

Intellectual Property

A new composition-of-matter patent will be filed in the next year.