The most successful system currently used in the clinic consists of administering a γ-cyclodextrin bearing a hydrophobic core and a hydrophilic crown tailored to scavenge the muscle relaxants rocuronium and vecuronium during general anaesthesia 1, 2, 3, 4. To circumvent this growing drug safety issue, researchers have started to develop dual drug-antidote strategies. Among classical examples of iatrogenic accidents, triggered by molecular therapy, are complex drug interactions, anaphylaxis and drug-induced coagulopathy. However, such optimized drugs, usually long acting and metabolically stable molecules, might also be the source of some adverse effects. Consequently, the ability of the chemist to tweak molecule structure to optimize its absorption, distribution, metabolism and excretion profile without losing pharmacological activity or in vivo specificity accounts for a large part of a drug’s therapeutic efficacy. Indeed, once the drug has been administered and after its entry into the systemic circulation, it undergoes complex distribution, metabolism and excretion processes. Optimization of absorption, distribution, metabolism and excretion profile to allow the most efficient targeting of the effector site is an essential step in the course of drug development.
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