Current Drug Metabolism - Volume 15, Issue 3, 2014

Allogenic hematopoietic stem cell transplantation (HSCT) is a well established but complex treatment option for malignant and non-malignant disorders in pediatric patients. Most commonly used myeloablative and non-myeloablative conditioning regimens in children comprise alkylating agents, such as busulfan (BU) and cyclophosphamide. Inter-individual variability in the pharmacokinetics of BU can result in altered cond Read More

Organic anion-transporting polypeptides (human OATPs; other species Oatps; gene family SLC21/SLCO) play important roles in drug absorption and distribution. In recent years, much information has been obtained on substrates that are transported by OATPs. Computer-based hydropathy analysis predicts that OATP family members share several structural features including twelve transmembrane domains (TMs), conserve Read More

Biologics, including but not limited to monoclonal antibodies (mAbs), cytokines, growth factors, enzymes, hormones, vaccines, antibody fragments (e.g. Fabs), and antibody drug conjugates (ADCs), have a powerful clinical impact on the management of a wide variety of diseases. When compared to small molecules (SMs), they have different physicochemical properties and demonstrate unique and complex pharmacokin Read More

Bioprecursor by definition is a type of prodrug that is designed to tackle pharmaceutical, pharmacokinetic or pharmacodynamic shortcomings of a drug that limit its clinical use. A retrometabolic approach is used to design bioprecursors which upon activation by either phase-I or phase-II metabolic enzymes result into an active metabolite. A bioprecursor differs from its active metabolite in many respects like physico-chem Read More

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequently used drugs, either on prescription or over-thecounter (OTC). Their daily dosage is based on randomised controlled trials and an empirical clinical assessment of their efficacy and toxicity that allows dose adjustment. The individual response can however be altered by environmental and genetic pharmacokinetic and pharmacodynamic factors. This review Read More