Basic Profile / Key Facts
Drug Category
Dosage Forms
Indications
For topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma.
Pharmacology
Alitretinoin (9-cis-retinoic acid) is a naturally-occurring endogenous retinoid indicated for topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma. Alitretinoin inhibits the growth of Kaposi's sarcoma (KS) cells in vitro.
Mechanism of Action
Alitretinoin binds to and activates all known intracellular retinoid receptor subtypes (RARa, RARb, RARg, RXRa, RXRb and RXRg). Once activated these receptors function as transcription factors that regulate the expression of genes that control the process of cellular differentiation and proliferation in both normal and neoplastic cells.
Absorption
Not Available
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Not Available
Contraindications
Panretin® gel is contraindicated in patients with a known hypersensitivity to retinoids or to any of the
ingredients of the product.
Drug Interactions
Patients who are applying Panretin® gel should not concurrently use products that contain DEET (N,
N-diethyl-m-toluamide), a common component of insect repellent products. Animal toxicology studies showed increased
DEET toxicity when DEET was included as proof of the formulation. Although there was no clinical evidence in the
vehicle-controlled studies of drug interactions with systemic antiretroviral agents, including protease inhibitors,
macrolide antibiotics, and azole antifungals, the effect of Panretin® gel on the steady-state concentrations of
these drugs is not known. No drug interaction data are available on concomitant administration of Panretin® gel
and systemic anti-KS agents.
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