Faculty of Pharmacy, University of Sydney, NSW 2006, Australia.
Save Sight Institute, the University of Sydney, Sydney, NSW 2000, Australia.
Adv Drug Deliv Rev. 2017 Jul 1;116:21-36. doi: 10.1016/j.addr.2016.06.004. Epub 2016 Jun 16.
Drug pharmacokinetics is influenced by the function of metabolising enzymes and influx/efflux transporters. Genetic variability of these genes is known to impact on clinical therapies. Solute Carrier Transporters (SLCs) are the primary influx transporters responsible for the cellular uptake of drug molecules, which consequently, impact on drug efficacy and toxicity. The Organic Anion Transporting Polypeptides (OATPs), Organic Anion Transporters (OATs) and Organic Cation Transporters (OCTs/OCTNs) are the most important SLCs involved in drug disposition. The information regarding the influence of SLC polymorphisms on drug pharmacokinetics is limited and remains a hot topic of pharmaceutical research. This review summarises the recent advance in the pharmacogenomics of SLCs with an emphasis on human OATPs, OATs and OCTs/OCTNs. Our current appreciation of the degree of variability in these transporters may contribute to better understanding the inter-patient variation of therapies and thus, guide the optimisation of clinical treatments.
药物药代动力学受代谢酶和内外流转运体的功能影响。这些基因的遗传变异已知会影响临床治疗。溶质载体转运体（SLCs）是负责药物分子细胞摄取的主要内流转运体，因此影响药物的疗效和毒性。有机阴离子转运多肽（OATPs）、有机阴离子转运体（OATs）和有机阳离子转运体（OCTs/OCTNs）是参与药物处置的最重要的 SLCs。关于 SLC 多态性对药物药代动力学影响的信息有限，仍然是药物研究的热点。本综述总结了 SLC 药物基因组学的最新进展，重点介绍了人 OATPs、OATs 和 OCTs/OCTNs。我们目前对这些转运体的变异性程度的认识可能有助于更好地理解治疗的个体间差异，从而指导临床治疗的优化。
