Pharmacological outcomes depend on many factors, with many of them being sexually dimorphic. Thus, physiological gender/sex (GENS) differences can influence pharmacokinetics, pharmacodynamics and, thus, bioavailability and resulting in efficacy of treatment, meaning GENS differences should be an important consideration in therapeutics. In particular, drug response can change according to different hormonal environments. Therefore, GENS-specific differences have a particular clinical relevance in terms of drug delivery, especially for those substances with a narrow therapeutic margin. Since adverse effects are more frequent among women, safety is a key issue. Overall, the status of women, from a pharmacological point of view, is often different and less studied than that of men and deserves particular attention. Further studies focused on women's responses to drugs are necessary in order to make optimal pharmacotherapeutic decisions.