Drug intelligence / Profile preview

N-desethyl otenabant

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Not Administered Directly (appears Only As A Metabolite Of Otenabant)
01

Overview

N-desethyl otenabant is the major human metabolite of otenabant (CP-945,598), a selective cannabinoid receptor type 1 (CB1) antagonist originally developed for metabolic and weight loss indications. N-desethyl otenabant retains structural similarity to the parent compound and is formed via hepatic N-dealkylation. The core mechanism involves antagonism (possibly with inverse agonism) at the cannabinoid receptor 1, a G-protein coupled receptor that regulates appetite and metabolism. Parent compound development was discontinued in clinical trials due to CNS side effects. N-desethyl otenabant itself was studied primarily as a metabolite in pharmacokinetic analyses of otenabant.[2][3]

Other names
N-desethyl otenabantCE-156,706SRU4YD01MFSRU-4YD01MFSRU 4YD01MFCP-945,598 metabolite M1
02

Targets

CNR1 (Cannabinoid receptor 1)

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