Topical retinoyl β-glucuronide (RBG) is beneficial in the treatment of mild to moderate acne (acne vulgaris) in patients largely of North-European origin in the US. Because the skin types of people in India are different from those in the US, we investigated the effectiveness and toxicity of topical RBG in acne patients in India. Each day, 27 acne patients were treated topically with the vehicle, and 39 acne patients were treated topically with 0.16% RBG cream for 18 weeks in a double-blind study. A significant reduction (p < 0.001) in total lesions, inflammatory lesions and noninflammatory lesions in patients treated with RBG as compared with the vehicle only (86.8, 80.2 and 94.6% vs. 40.1, 34.3 and 50%, respectively) was observed. No side effects were associated with topical RBG treatment. Thus, topical 0.16% RBG is a rapid, effective and nontoxic treatment for mild to moderate acne in Asian-Indian patients.