tretinoin

Modality

small molecule

Mechanism

12.1 Mechanism of Action Although tretinoin activates three members of the retinoic acid (RAR) nuclear receptors (RARα, RARβ, and RARγ) which may act to modify gene expression, subsequent protein synthesis, and epithelial cell growth and differentiation, it has not been established whether the clinical effects of tretinoin are mediated through activation of retinoic acid receptors and/or other mechanisms. The exact mechanism of action of topical tretinoin for treatment of acne vulgaris is unknown. Current evidence suggests that topical tretinoin decreases cohesiveness of follicular epithelial cells with decreased microcomedone formation. Additionally, tretinoin stimulates mitotic activity and increased turnover of follicular epithelial cells causing extrusion of the comedones.

Targets

RAR, RXR

Storage

—

Approved

acne vulgaris — FDA

In trial

acne vulgaris, rosacea, vitiligo

Sources

DailyMed (FDA label)DrugBank ClinicalTrials.gov

Last verified

2026-06-14

No curated MOA diagram yet. See lib/moa-data.ts for the shape; add an entry keyed by tretinoin.

Formulations

0.025% cream0.05% cream0.1% cream0.01% gel0.025% gel0.05% gel0.04% microsphere gel0.1% microsphere gel