Drug intelligence / Profile preview

13-cis retinoic acid + tocopherol

Development stage
Unknown
Modality
Implantable Devices → Device-based Delivery → Drug Delivery Systems, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Oral
01

Overview

This drug is a combination of 13-cis retinoic acid (also known as isotretinoin) and tocopherol (vitamin E, specifically the alpha form). 13-cis retinoic acid is a synthetic retinoid that modulates gene expression by activating nuclear retinoic acid receptors, leading to effects on cell differentiation and proliferation. It has been studied for its antineoplastic properties in cancer chemoprevention and treatment. Tocopherol acts as an antioxidant, protecting cells from oxidative damage. The combination has been investigated primarily to reduce the toxicity associated with high-dose 13-cis retinoic acid therapy while potentially enhancing its clinical activity. Studies suggest that adding tocopherol may lower the rate of severe side effects typical of high-dose isotretinoin and could enhance response rates in premalignant lesions[1][5]. The combination has been explored mainly in myelodysplastic syndromes (MDS), oral premalignancy, and other cancer prevention settings.

Other names
13cRA + alpha-tocopherolisotretinoin + vitamin E13-cis-retinoic acid + alpha-tocopherol
02

Targets

PUFAs (Polyunsaturated fatty acyl chains)RARB (Retinoic acid receptor beta)RARG (Retinoic acid receptor gamma)RARA (Retinoic acid receptor alpha)Cyp (Cyclophilin family)

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