The invention relates to compositions and methods useful for enhancing hair growth and promoting skin regeneration. Particularly, the invention provides topical compositions including trimebutine, salts, or active metabolites thereof, for enhancing or inducing hair growth and promoting skin regeneration. Compositions comprising trimebutine or a pharmaceutically acceptable salt or active metabolite thereof and their use in the method of promoting hair growth or skin regeneration. Preferably trimebutine is trimebutine maleate or N-desmethyl trimebutine. Compositions are preferably in a form for topical administration, such as a gel.