Drug intelligence / Profile preview

liposomal tretinoin

Development stage
Phase 2
Lead developer
Agenus
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Topical
01

Overview

Liposomal tretinoin is a specialized formulation of all-trans-retinoic acid (ATRA) encapsulated within liposomal vesicles to improve therapeutic outcomes and reduce side effects compared to conventional formulations. In systemic administration (intravenous), the liposomal delivery system provides sustained plasma concentrations and alters the drug's pharmacokinetic profile, which has been investigated for treating various malignancies such as Kaposi's sarcoma, acute promyelocytic leukemia, and renal cell carcinoma. In topical applications, liposomal encapsulation enhances the penetration of tretinoin into the skin while significantly reducing the local irritation, erythema, and "flare-up" reactions typically associated with standard tretinoin gels and creams used for acne vulgaris. Tretinoin works by binding to and activating nuclear retinoic acid receptors (RARs), which subsequently modulate gene expression to promote cell differentiation and inhibit proliferation.

Brand names
Atragen
Other names
tretinoin liposomeall-trans-retinoic acid liposomeliposomal all-trans-retinoic acid
02

Targets

RARA (Retinoic acid receptor alpha)RARG (Retinoic acid receptor gamma)RARB (Retinoic acid receptor beta)

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