Drug intelligence / Profile preview

ASP2205

Development stage
Discontinued
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

ASP2205 is a potent and selective small molecule agonist of the serotonin 5-HT2C receptor. It was developed to enhance pudendal nerve-mediated urethral closure reflexes via activation of the 5-HT2C receptor, with the aim of preventing involuntary urine loss. In preclinical studies, ASP2205 demonstrated high selectivity and potency for human and rat 5-HT2C receptors (EC50 values of 0.85 nM and 2.5 nM, respectively). However, in clinical trials involving healthy volunteers, ASP2205 did not increase urethral pressure or show efficacy for stress urinary incontinence; it was also associated with central nervous system-related side effects such as dizziness and nausea[1][10][7]. The drug is not approved for any indication.

Other names
ASP2205 fumarateASP-2205 fumarateASP 2205 fumarate
02

Targets

HTR2C (5-hydroxytryptamine 2C receptor)

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