Drug intelligence / Profile preview

alitretinoin

Development stage
Approved
Lead developer
Ligand Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Topical, Oral
01

Overview

Alitretinoin is a first-generation retinoid and a vitamin A derivative used primarily as a topical treatment for cutaneous lesions in patients with AIDS-related Kaposi's sarcoma. It is also used off-label for chronic hand eczema and psoriasis. Alitretinoin binds to and activates all known intracellular retinoid receptor subtypes, including retinoic acid receptors (RARα, RARβ, RARγ) and retinoid X receptors (RXRα, RXRβ, RXRγ). Once activated, these nuclear receptors function as transcription factors that regulate the expression of genes involved in cellular differentiation, proliferation, inflammation modulation, and apoptosis. The drug exerts anti-inflammatory effects by suppressing chemokine receptor expression and reducing recruitment of inflammatory cells such as macrophages and dendritic cells. Its anti-proliferative effect is mediated through RARs while apoptotic activity is mediated via RXRs[1][2][5][6][8].

Brand names
Panretin
Other names
9-cis-retinoic acid
02

Targets

RXRB (Retinoid X receptor beta)RARB (Retinoic acid receptor beta)RARG (Retinoic acid receptor gamma)RXRA (Retinoid X receptor alpha)RXRG (RXRγ)RARA (Retinoic acid receptor alpha)

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