Drug intelligence / Profile preview

dendrogenin a

Development stage
Preclinical
Lead developer
Affichem
Modality
Small Molecules
Administration
Not Yet Established (preclinical/experimental), Likely Parenteral For Research
01

Overview

**Dendrogenin A** is a mammalian cholesterol metabolite, arising from the conjugation of 5,6α-epoxy-cholesterol and histamine, and has potent antitumor properties. It acts as a **selective modulator of Liver X Receptors (LXR)**, with a higher affinity for LXRβ, and as a **selective inhibitor of cholesterol epoxide hydrolase (ChEH), particularly the 3β-hydroxysterol-Δ⁸,⁷-isomerase (D8D7I)** subunit[1][4][5][7][9][10]. By activating LXR and inhibiting D8D7I, Dendrogenin A induces lethal autophagy and differentiation in cancer cells, especially in melanoma and acute myeloid leukemia (AML), while displaying low toxicity to normal cells[1][3][4][6]. It also enhances the cytotoxic activity and DNA damage caused by anthracyclines and synergizes with cytarabine and idarubicin in leukemia models[3][6]. Dendrogenin A is being investigated for its clinical potential, primarily for AML[7].

Other names
5alpha-hydroxy-6beta-[2-(1H-imidazol-4-yl)-ethylamino]-cholestan-3beta-ol5alpha-hydroxy-6beta-(2-(1H-imidazol-4-yl)-ethylamino)-cholestan-3beta-ol
02

Targets

ChEH (Cholesterol epoxide hydrolase)LXRB (Liver X receptor beta)NR1H3 (Liver X receptor beta)EBP (Sterol isomerase (emopamil-binding protein))

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