Drug intelligence / Profile preview

caesaldekarin e

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

**caesaldekarin e** is a cassane diterpenoid primarily isolated from plants of the *Caesalpinia* genus, such as *Caesalpinia bonduc*[1][6]. It has demonstrated significant anti-inflammatory properties in preclinical studies, notably ameliorating dextran sulfate sodium (DSS)-induced experimental colitis in mice by reducing disease severity, suppressing inflammatory infiltration, maintaining intestinal barrier integrity, restoring gut microbiota composition (especially increasing *Lactobacillus* abundance), and modulating tryptophan metabolism by inhibiting indoleamine 2,3-dioxygenase 1 (IDO-1)[1]. Importantly, caesaldekarin e acts as a selective glucocorticoid receptor (GR) modulator, inhibiting GR dimerization and (+) GRE-mediated transactivation while enhancing GR-mediated transcriptional repression and the interaction between GR and NF-κB subunit p65, thereby attenuating inflammation with reduced glucocorticoid-like side effects[2][5]. This dual mechanism—targeting both inflammation and GR signaling—positions caesaldekarin e as a potential novel therapeutic agent for inflammatory diseases, especially where conventional glucocorticoids have limitations due to side effects[2].

02

Targets

IDO1 (Indoleamine 2,3-dioxygenase 1)GR (Glucocorticoid receptor)

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