Abstract
During the last decade, a greater focus has been given to impact of genetic variation in membrane transporters on the pharmacokinetics and toxicity of numerous therapeutic drugs. While the majority of transporter-related pharmacogenetic research has been in regards to classic genes encoding the outward-directed ATP-binding cassette (ABC) transporters, such as ABCB1 (Pglycoprotein), ABCC2 (MRP2), and ABCG2 (BCRP), more studies have been conducted in recent years evaluating genes encoding solute carriers (SLC) that mediate the cellular uptake of drugs, such as SLCO1B1 (OATP1B1) and SLC22A1 (OCT1). The distribution of ABC and SLC transporters in tissues key to pharmacokinetics, such as intestine (absorption), blood-brain-barrier (distribution), liver (metabolism), and kidneys (excretion), strongly suggests that genetic variation associated with changes in protein expression or function of these transporters may have a substantial impact on systemic drug exposure and toxicity. In this current article, we will review recent advances in understanding the contribution of critical ABC and SLC transporters to interindividual pharmacokinetic and dynamic variability of substrate drugs.
Current Pharmaceutical Design
Title: Pharmacogenetics of Drug Transporters
Volume: 16 Issue: 2
Author(s): R. M. Franke, E. R. Gardner and A. Sparreboom
Affiliation:
Abstract: During the last decade, a greater focus has been given to impact of genetic variation in membrane transporters on the pharmacokinetics and toxicity of numerous therapeutic drugs. While the majority of transporter-related pharmacogenetic research has been in regards to classic genes encoding the outward-directed ATP-binding cassette (ABC) transporters, such as ABCB1 (Pglycoprotein), ABCC2 (MRP2), and ABCG2 (BCRP), more studies have been conducted in recent years evaluating genes encoding solute carriers (SLC) that mediate the cellular uptake of drugs, such as SLCO1B1 (OATP1B1) and SLC22A1 (OCT1). The distribution of ABC and SLC transporters in tissues key to pharmacokinetics, such as intestine (absorption), blood-brain-barrier (distribution), liver (metabolism), and kidneys (excretion), strongly suggests that genetic variation associated with changes in protein expression or function of these transporters may have a substantial impact on systemic drug exposure and toxicity. In this current article, we will review recent advances in understanding the contribution of critical ABC and SLC transporters to interindividual pharmacokinetic and dynamic variability of substrate drugs.
Export Options
About this article
Cite this article as:
Franke M. R., Gardner R. E. and Sparreboom A., Pharmacogenetics of Drug Transporters, Current Pharmaceutical Design 2010; 16 (2) . https://dx.doi.org/10.2174/138161210790112683
DOI https://dx.doi.org/10.2174/138161210790112683 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Guide of Hypertensive Crisis Pharmacotherapy
Cardiovascular & Hematological Disorders-Drug Targets Ribozymes in the Age of Molecular Therapeutics
Current Molecular Medicine Preface
Current Cardiology Reviews Methylglyoxal and Advanced Glycation Endproducts: New Therapeutic Horizons?
Recent Patents on Cardiovascular Drug Discovery Immunophilins in Nervous System Degeneration and Regeneration
Current Topics in Medicinal Chemistry Novel Design and Synthesis of Modified Structure of Carvedilol
Recent Patents on Cardiovascular Drug Discovery Renovascular Hypertension: Novel Insights
Current Hypertension Reviews Formulation and In Vitro Evaluation of Solid Lipid Microparticles of Candesartan Cilexetil Floating Tablets
Drug Delivery Letters Catecholamines, Sympathetic Innervation and Immunity: Role in Experimental and Rheumatoid Arthritis
Letters in Drug Design & Discovery Isoprenoid Metabolism as a Therapeutic Target in Gram-Negative Pathogens
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: Perspectives of Antiarrhythmic Therapy: New Trails, Challenges and Pitfalls)
Current Pharmaceutical Design Port-a-Patch and Patchliner: High Fidelity Electrophysiology for Secondary Screening and Safety Pharmacology
Combinatorial Chemistry & High Throughput Screening Development of Physical Disability in Older Adults
Current Aging Science Smoking and Cardiovascular System: Cellular Features of the Damage
Current Pharmaceutical Design Cellular Senescence in Ageing, Age-Related Disease and Longevity
Current Vascular Pharmacology Therapeutic Utilisations of Vasopressin and Oxytocin in Mood Disorders
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Properties of the Mesenchymal Endometriotic Stem Cell in the Context of the Immune System and Analysis of its Role in Endometriosis
Recent Patents on Regenerative Medicine A PHACES Syndrome Unmasked by Propranolol Interruption in a Tetralogy of Fallot Patient: Case Report and Extensive Review on New Indications of Beta Blockers
Current Medicinal Chemistry Pharmacological Characterisation of Spider Antimicrobial Peptides
Protein & Peptide Letters Urocortins: Putative Role in Cardiovascular Disease
Current Medicinal Chemistry - Cardiovascular & Hematological Agents