title: The influence of lipophilicity in drug discovery and design.
abstract: BACKGROUND
  The role of lipophilicity in drug discovery and design is a critical one. Lipophilicity is a key physicochemical property that plays a crucial role in determining ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties and the overall suitability of drug candidates. There is increasing evidence to suggest that control of physicochemical properties such as lipophilicity, within a defined optimal range, can improve compound quality and the likelihood of therapeutic success.
  
  
  METHODS
  This review focuses on understanding lipophilicity, techniques used to measure lipophilicity, and summarizes the importance of lipophilicity in drug discovery and development, including a discussion of its impact on individual ADMET parameters as well as its overall influence on the drug discovery and design process, specifically within the past 15 years.
  
  
  CONCLUSIONS
  A current review of the literature reveals a continued reliance on the synthesis of novel structures with increased potency, rather than a focus on maintaining optimal physicochemical properties associated with ADMET throughout drug optimization. Particular attention to the optimum region of lipophilicity, as well as monitoring of lipophilic efficiency indices, may contribute significantly to the overall quality of candidate drugs at different stages of discovery.
authors.affiliation: Commonwealth Medical College, Department of Basic Sciences, Scranton, PA 18509, USA.
authors.forename: John A
authors.initials: JA
authors.lastname: Arnott
authors.forename: Sonia Lobo
authors.initials: SL
authors.lastname: Planey
mesh_terms: D020003:1-Octanol / Q000737:chemistry; D000042:Absorption; D000818:Animals; D055808:Drug Discovery; D006801:Humans; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D014867:Water / Q000737:chemistry
chemical_list: D004364:Pharmaceutical Preparations; D014867:Water; D020003:1-Octanol