Disclosed are unsaturated alkyl esters of 5-aminovulinic acid of the following chemical formula 1, or pharmaceutically acceptable salts thereof, a method for preparing the same, and uses thereof. [Chemical Formula I] NH2—CH2—CO—CH2—CH2—CO—O—R wherein, R is a group selected from a group consisting of 2-propenyl, 3-butenyl, 4-pentenyl, 5-hexenyl, cis-2-pentenyl, cis-3-hexenyl, cis-4-hexenyl, and trans-2-hexenyl. Also, a pharmaceutical composition comprising the unsaturated alkyl ester of 5-aminovulinic acid or a salt thereof as an active ingredient is provided. This pharmaceutical composition is easily absorbed transdermally and is of low cytotoxicity. Featuring no amino-protecting processes, the method guarantees high production yields.
