Investigating the Metabolism of ACT-541468, Utilizing a Microtracer and Accelerator Mass Spectrometry in The First-in-Humans Trial.
In conclusion, ACT-541468 is extensively metabolized predominantly by oxidative transformations. PMID: 30727881 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - February 6, 2019 Category: Drugs & Pharmacology Authors: Muehlan C, Fischer H, Zimmer D, Aissaoui H, Grimont J, Boss C, Croft M, van Gerven J, Krähenbühl S, Dingemanse J Tags: Curr Drug Metab Source Type: research

Clinical Implications Of Methotrexate Pharmacogenetics In Childhood Acute Lymphoblastic Leukaemia.
Abstract In the past two decades, a great body of research has been published regarding the effects of genetic polymorphisms on methotrexate (MTX)-induced toxicity and efficacy. Of particular interest is the role of this compound in childhood acute lymphoblastic leukaemia (ALL), where it is a pivotal drug in the different treatment protocols, both at low and high doses. MTX acts on a variety of target enzymes in the folates cycle, as well as being transported out and into of the cell by several transmembrane proteins. This review aims to summarize the current knowledge concerning the clinical impact of polymorphis...
Source: Current Drug Metabolism - January 30, 2019 Category: Drugs & Pharmacology Authors: Gervasini G, Mota-Zamorano S Tags: Curr Drug Metab Source Type: research

Recent Advances on Prediction of Human Papillomaviruses Risk Types.
CONCLUSION: From the prediction accuracy, we get that the classification results are more accurate by establishing mathematical models. Thus, adopting mathematical methods to predict risk type of HPV will be the main goal of research in the future. PMID: 30657038 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - January 17, 2019 Category: Drugs & Pharmacology Authors: Yao Y, Xu H, Li M, Qi Z, Liao B Tags: Curr Drug Metab Source Type: research

Effects of CYP2C8 and SLCO1B1 genetic polymorphisms on repaglinide pharmacokinetics: A systematic review and meta-analysis.
Abstract OBJECTIVE: The purpose of this systematic review and meta-analysis was to summarize the potential impact of CYP2C8 and SLCO1B1 genetic polymorphisms on repaglinide pharmacokinetics. METHOD: A systematic search was conducted using electronic databases. Eligible studies reported data from pharmacokinetic evaluations of repaglinide in healthy adults according to different categories of CYP2C8 and SLCO1B1 genetic polymorphisms. RESULTS: Six studies including a total of 191 participants met the inclusion criteria. We noted that CYP2C8 *1/*3 carriers exhibited lower AUC(0-∞) (SMD: -0.77; 95%CI: ...
Source: Current Drug Metabolism - January 10, 2019 Category: Drugs & Pharmacology Authors: Zhou S, Xiang Q, Mu G, Ma L, Chen S, Xie Q, Zhang Z, Cui Y Tags: Curr Drug Metab Source Type: research

A metabonomics approach to drug toxicology in liver disease and its application in Traditional Chinese Medicine.
CONCLUSION: Metabonomics has great advantages in all aspects of the therapy of liver diseases, with good prospects for clinical application. PMID: 30599107 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - December 31, 2018 Category: Drugs & Pharmacology Authors: Su G, Wang H, Bai J, Chen G, Pei Y Tags: Curr Drug Metab Source Type: research

GHB Pharmacology and Toxicology: From Metabolism and Pharmacokinetics to Applications: In Clinical and Forensic Toxicology.
zzi G Abstract PMID: 30484395 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - December 1, 2018 Category: Drugs & Pharmacology Authors: Busardò FP, Vergallo GM, Plazzi G Tags: Curr Drug Metab Source Type: research

Progress in the Consideration of Possible Sex Differences in Drug Interaction Studies.
CONCLUSION: This review has shown that only limited progress had been made with the inclusion of both sexes in DDI studies. PMID: 30488793 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - November 28, 2018 Category: Drugs & Pharmacology Authors: Naidoo P, Chetty M Tags: Curr Drug Metab Source Type: research

Nanotherapeutics for the treatment of cancer and arthritis.
Abstract Nanotechnology is gaining significant attention worldwide for the treatment of complex disease such as AIDS (acquired immune deficiency syndrome), cancer and rheumatoid arthritis. Nanomedicine is the application of nanotechnology used for diagnosis and treatment for the disease that includes the preservation and improvement of human health by covering an area such as drug delivery using nanocarriers, nanotheranostics and nanovaccinology. The present article provides an insight on several aspects of nanomedicine such as usages of multiple type of nanocarriers, their status, advantages and disadvantages wit...
Source: Current Drug Metabolism - November 26, 2018 Category: Drugs & Pharmacology Authors: Patel P, Meghani N, Kansara K, Kumar A Tags: Curr Drug Metab Source Type: research

Removal of Pharmaceutical Contaminants in Wastewater using Nanomaterials: A Comprehensive Review.
CONCLUSION: The recommendations provided in this article will be useful to adopt novel strategies for on-site removal of the emerging contaminants in pharmaceutical effluents and related industries. PMID: 30479212 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - November 26, 2018 Category: Drugs & Pharmacology Authors: Chauhan A, Sillu D, Agnihotri S Tags: Curr Drug Metab Source Type: research

Magnetic Nanoparticles: Current Trends and Future Aspects in Diagnostics and Nanomedicine.
CONCLUSION: MNPs have found widespread use as contrast agents in imaging modalities, as tools for bio-sensing, and as therapeutic and theranostics agents. Multiple formulations of MNPs are in clinical testing and may be accepted in clinical settings in near future. PMID: 30465498 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - November 22, 2018 Category: Drugs & Pharmacology Authors: Vallabani NVS, Singh S, Karakoti A Tags: Curr Drug Metab Source Type: research

Iron oxide nanoparticles for breast cancer theranostics.
CONCLUSION: This review mainly focuses on the versatile applications of superparamagnetic iron oxide nanoparticles on the diagnosis, treatment, and detecting progress of breast cancer treatment. Their wide application is because of their excellent superparamagnetic, biocompatible and biodegradable properties. PMID: 30465497 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - November 21, 2018 Category: Drugs & Pharmacology Authors: Shakil S, Hasan A, Sarker SR Tags: Curr Drug Metab Source Type: research

Metabolic Pathway of Cyclosporine A and Its Correlation with Nephrotoxicity.
Abstract Cyclosporine A (CsA) is widely used for organ transplantation and autoimmune disorders. However, CsA nephrotoxicity is a serious side effect that limits the clinical use of CsA. Notably, the metabolism of CsA has a close relationship with this disease in renal-transplant patients. The major metabolic pathways of CsA in humans are hydroxylation (AM1 and AM9) and N-demethylation (AM4N). Normally, these metabolites are relatively less toxic than CsA. However, the metabolism of CsA in the kidneys is much weaker than that in the liver, which explains why CsA is so toxic to the kidneys. CYP3A families, especial...
Source: Current Drug Metabolism - October 31, 2018 Category: Drugs & Pharmacology Authors: Wu Q, Kuca K Tags: Curr Drug Metab Source Type: research

Recent advances in machine learning methods for predicting heat shock proteins.
Abstract As molecular chaperones, heat shock proteins (HSPs) not only play key roles in protein folding and maintaining protein stabilities, but also linked with multiple kinds of diseases. Therefore, HSPs have been regarded as the focus of drug design. Since HSPs from different families play distinct functions, accurately classifying the families of HSPs is the key step to clearly understand their biological functions. In contrast to labor-intensive and cost-ineffective experimental methods, accurately computational classification of HSP families has emerged to be an alternative approach. In this work, we reviewe...
Source: Current Drug Metabolism - October 30, 2018 Category: Drugs & Pharmacology Authors: Chen W, Feng P, Liu T, Jin D Tags: Curr Drug Metab Source Type: research

Nutritional Deficiencies after Gastric Bypass: Mechanisms Involved and Strategies to Improve Oral Supplement Disposition.
CONCLUSION: Oral supplement disposition is altered following RYGB. As a result, patients are required to take complex regimens of oral supplementation indefinitely. The dosage which confers optimum health benefit while avoiding potential toxicity and tolerability issues remains unknown. Novel preparations are needed to optimally address post-RYGB nutritional deficiencies. PMID: 30362417 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 26, 2018 Category: Drugs & Pharmacology Authors: Mangan A, Roux CL, Miller NG, Docherty N Tags: Curr Drug Metab Source Type: research

Anti-leishmanial Nanotherapeutics: A Current Perspective.
Abstract Leishmaniasis is a dreaded disease caused by protozoan parasites belonging to the genus Leishmania which results in significant morbidity and mortality worldwide. There are no vaccines available currently for the treatment of Leishmaniasis and chemotherapy still remains the mainstay for anti-leishmanial therapeutics. However, toxicity, reduced bioavailability, high cost and chemoresistance are the principal problems which limit the use of the available drugs. In this context, anti-leishmanial nanotherapeutics may show the way for effective treatment of this dreaded disease. In this review, we discuss the ...
Source: Current Drug Metabolism - October 22, 2018 Category: Drugs & Pharmacology Authors: Shah A, Gupta SS Tags: Curr Drug Metab Source Type: research

Effects of Gut Microbiota on Drug Metabolism and Guidance for Rational Drug Use under Hypoxic Conditions at High Altitudes.
CONCLUSION: This review provides an overview of the effects of gut microbiota on drug metabolism and provides guidance for rational drug use under hypoxic conditions at high altitudes. PMID: 30338735 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 19, 2018 Category: Drugs & Pharmacology Authors: Zhang J, Zhang J, Wang R, Jia Z Tags: Curr Drug Metab Source Type: research

Survey of Machine Learning Techniques for Prediction of the Isoform Specificity of Cytochrome P450 Substrates.
CONCLUSION: Both single-label and multi-label classification methods have demonstrated good performance on modelling and prediction of the isoform specificity of substrates based on their quantitative descriptors. PMID: 30338736 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 18, 2018 Category: Drugs & Pharmacology Authors: Xiong Y, Qiao Y, Kihara D, Zhang HY, Zhu X, Wei DQ Tags: Curr Drug Metab Source Type: research

Machine Learning in Quantitative Protein-Peptide Affinity Prediction: Implications for Therapeutic Peptide Design.
CONCLUSION: There is still a long way to go before establishment of general, reliable and efficient machine leaning-based protein-peptide affinity predictors. PMID: 30317994 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 12, 2018 Category: Drugs & Pharmacology Authors: Li Z, Miao Q, Yan F, Meng Y, Zhou P Tags: Curr Drug Metab Source Type: research

Advances and Application of a Novel Oral Anticoagulant in Specific Populations: Dabigatran Etexilate.
Abstract Dabigatran etexilate (DE) was approved by the FDA in 2010 to reduce the risk of stroke and systemic embolism in adults with non-valvular atrial fibrillation (NVAF). Compared with warfarin, a traditional anticoagulant drug, DE exhibits a shorter half-life, improved dose-effect relationship, fewer food and drug interactions, and can be taken orally without monitoring the conventional coagulation index. DE can also prevent or reduce the severity of adverse events, such as attenuated drug efficacy or bleeding. It is convenient for patients to take DE due to low levels of individual variation. We review the ph...
Source: Current Drug Metabolism - October 11, 2018 Category: Drugs & Pharmacology Authors: Xu D, Su C, Pan J Tags: Curr Drug Metab Source Type: research

The Development of Machine Learning Methods in Cell-Penetrating Peptides Identification: A Brief Review.
CONCLUSION: In this review, the last studies on CPP identification using machine learning method were reported. We also discussed the future development direction of CPP recognition with computational methods. PMID: 30317992 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 10, 2018 Category: Drugs & Pharmacology Authors: Wei HH, Yang W, Tang H, Lin H Tags: Curr Drug Metab Source Type: research

Drug-drug interactions of P-gp substrates unrelated to CYP metabolism.
Abstract In this decade, it is known that the role of several drug transporters is to act as a key player in drug disposition, and then they can affect clinical significances. Nevertheless, most of the drug-drug interaction (DDI) studies have been related to cytochrome P450s (CYPs), and these are followed by in vitro and in vivo drug-interactive reports on drug-transporters, which are accumulating. In addition, when both substrate drugs of CYPs and drug transporters (e.g., P-glycoprotein, P-gp) are related to DDIs, it remains that the mechanisms of DDIs will be quite ambiguous in assessing how much the CYPs and/or...
Source: Current Drug Metabolism - October 3, 2018 Category: Drugs & Pharmacology Authors: Akamine Y, Yasui-Furukori N, Uno T Tags: Curr Drug Metab Source Type: research

Survey of Drug Oxidation Activities in Liver and Intestine Microsomes of Individual Common Marmosets, a New Nonhuman Primate Animal Model.
CONCLUSION: The marmoset could be a model animal for humans with respect to the first-pass extraction of terfenadine and related substrates. These findings provide a foundation for understanding individual pharmacokinetic and toxicological results in nonhuman primates as preclinical models and will help to further support understanding of the molecular mechanisms of human P450 function. PMID: 30280664 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 3, 2018 Category: Drugs & Pharmacology Authors: Uehara S, Oshio T, Nakanishi K, Tomioka E, Suzuki M, Inoue T, Uno Y, Sasaki E, Yamazaki H Tags: Curr Drug Metab Source Type: research

A Review of Recent Advances and Research on Drug Target Identification Methods.
Abstract From a therapeutic viewpoint, understanding how drugs bind and regulate the functions of their target proteins to protect against disease is crucial. The identification of drug targets plays a significant role in drug discovery and in studying the mechanisms of diseases. The development of methods to identify drug targets has become a popular issue in this field of research. Originally, scientists used biological experiments to identify drug targets. However, recently, an increasing number of scientists use computational methods to identify drug targets. Although thousands of drug targets are estimated to...
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Hu Y, Zhao T, Zhang N, Zhang Y, Cheng L Tags: Curr Drug Metab Source Type: research

A Review of Theranostics Applications and Toxicities of Carbon Nanomaterials.
CONCLUSION: In brief, this review article discusses the numerous theranostics applications and toxicities of CNMs. Biomolecules-functionalized oxygenated GO and CNTs are more efficacious than the other CNMs with abridged cellular toxicity. PMID: 30251600 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Gupta N, Rai DB, Jangid AK, Kulhari H Tags: Curr Drug Metab Source Type: research

Influence of CYP3A and ABCB1 Single Nucleotide Polymorphisms on the Pharmacokinetics/Pharmacodynamics of Tacrolimus in pediatric patients.
Abstract Single nucleotide polymorphisms (SNPs) are the most common variants in many genes, which are also promising markers in relation to drug responses in pharmacogenomics studies. Tacrolimus is a primary immunosuppressant used for the prevention of organ rejection in pediatric organ transplantation. Tacrolimus, transported out of cells via P-glycoprotein (ABCB1), is also a metabolic substrate for cytochrome P450 (CYP) 3A enzymes, especially the CYP3A4 and the CYP3A5. The SNP of these genes have been studied extensively in adult population, but there is no systematic review in children. In this paper, we focus ...
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Yang M, Wang M, Gui H, Mao C Tags: Curr Drug Metab Source Type: research

Replacing GHB with GBL in recreational settings: a new trend in chemsex.
CONCLUSIONS: GBL currently represents a growing public health issue since the substance relatively cheaper and easier to obtain than GHB. Improvement and implementation of laws and policies to place GBL under control are needed to limit its diffusion, the eventual health threat for users and its non -negligible abuse liability and dependence risk. PMID: 30251602 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Busardo FP, Gottardi M, Tini A, Minutillo A, Marinelli E, Zaami S Tags: Curr Drug Metab Source Type: research

Cancer Nanotechnology: A New Revolution for Cancer Diagnosis and Therapy.
Conclusion- This review highlights various approaches of cancer nanotechnology in the advancement of cancer therapy. PMID: 30227814 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 18, 2018 Category: Drugs & Pharmacology Authors: Chaturvedi VK, Singh A, Singh VK, Singh MP Tags: Curr Drug Metab Source Type: research

The role of xenobiotic receptors on hepatic glycolipid metabolism.
Abstract PXR (pregnane X receptor) and CAR (constitutive androstane receptor) are termed as xenobiotic receptors, which are known as core factors in the regulation of the transcription of metabolic enzymes and drug transporters. However, accumulating evidence has shown that PXR and CAR exert their effects on energy metabolism through the regulation of gluconeogenesis, lipogenesis, and β-oxidation. Therefore, PXR and CAR may become new therapeutic targets for metabolic syndrome, including obesity and diabetes. In this review, we will summarize recent advances to show how xenobiotic receptors regulate energy me...
Source: Current Drug Metabolism - September 18, 2018 Category: Drugs & Pharmacology Authors: Chen K, Zhong J, Hu L, Li R, Duc Q, Cai J, Li Y, Gao Y, Cui X, Yang X, Wu X, Yao L, Dai J, Wang Y, Jin H Tags: Curr Drug Metab Source Type: research

Advanced Glycation End Products (AGEs), Glutathione and Breast Cancer: Factors, Mechanism and Therapeutic Interventions.
CONCLUSION: This review provides a strong platform to comprehend the etiology, mechanism and production of AGEs and glutathione along with the agents which can block their production, paving a way for the therapeutic intervention and an amicable solution to treat and manage breast cancer. PMID: 30207227 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 11, 2018 Category: Drugs & Pharmacology Authors: Sharma AK, Sharma VR, Gupta GK, Ashraf GM, Kamal MA Tags: Curr Drug Metab Source Type: research

Novel Nanoparticles for Tumor Targeting Drug Delivery.
PMID: 30187836 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 8, 2018 Category: Drugs & Pharmacology Authors: Gao H Tags: Curr Drug Metab Source Type: research

Targeting Virus-host Protein Interactions: Feature Extraction and Machine Learning Approaches.
We describe the pivotal and representative features extracted from relevant sources of biological data, mainly include sequence signatures, known domain interactions, protein motifs and protein structure information, which are the basis of the virus-host PPI prediction. We focus on state-of-the-art machine learning algorithms that are used to build binary prediction models for the classification of virus-host protein pairs and discuss their abilities, weakness and future directions. PMID: 30156155 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 29, 2018 Category: Drugs & Pharmacology Authors: Zheng N, Wang K, Zhan W, Deng L Tags: Curr Drug Metab Source Type: research

Molecular Design of Peptide-Fc Fusion Drugs.
Abstract Peptide-Fc fusion drugs are a category of biological therapeutics in which the Fc region of an antibody is genetically fused to a peptide of interest. In this review, we summarize the key steps in peptide-Fc fusion technology and stress the main computational resources, tools, and methods that have been used in the rational design of peptide-Fc fusion drugs. Additionally, open questions about the computer-aided molecular design of peptide-Fc are raised. Answers to these questions by future research will certainly help make the transition from peptide leads to drugs on the market quicker and cheaper. ...
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Ning L, He B, Zhou P, Derda R, Huang J Tags: Curr Drug Metab Source Type: research

Recent advances in the machine learning-based drug-target interaction prediction.
This study provides the guide to the development of computational methods for the drug-target interaction prediction. PMID: 30129407 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Zhang W, Lin W, Zhang D, Wang S, Shi J, Niu Y Tags: Curr Drug Metab Source Type: research

The Impact of Carboxylesterases in Drug Metabolism and Pharmacokinetics.
Abstract Carboxylesterases (CES) play a critical role in catalyzing hydrolysis of esters, amides, carbamates and thioesters, and bioconverting prodrugs and soft drugs. Human CES1 is one of the most highly expressed drug metabolizing enzymes in the liver, while human intestine only expresses CES2. The unique tissue distribution of CES enzymes provides great opportunities to design prodrugs or soft drugs for tissue targeting. CES enzymes have moderate to high inter-individual variability and exhibit low to no expression in the fetus, but increase substantially during the first few months of life. The CES genes are h...
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Di L Tags: Curr Drug Metab Source Type: research

Survey of Machine Learning Techniques in Drug Discovery.
Abstract Drug discovery, which is the process of discovering new candidate medications, is very important for pharmaceutical industries. At its current stage, discovering new drugs is still an expensive and time-consuming process, requiring Phases I, II and III for clinical trials. Recently, machine learning techniques in Artificial Intelligence (AI), especially the deep learning techniques which allow a computational model to generate multiple layers, have been widely applied and achieved state-of-the-art performance in various fields, such as speech recognition, image classification, bioinformatics, etc. One pot...
Source: Current Drug Metabolism - August 19, 2018 Category: Drugs & Pharmacology Authors: Stephenson N, Shane E, Chase J, Rowland J, Ries D, Justice N, Zhang J, Chan L, Cao R Tags: Curr Drug Metab Source Type: research

Interindividual Variability in Drug Metabolizing Enzymes.
PMID: 30117390 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 17, 2018 Category: Drugs & Pharmacology Authors: Volpe DA Tags: Curr Drug Metab Source Type: research

Preclinical Pharmacokinetics of Triptolide: A Potential Antitumor Drug.
Abstract Triptolide, a bioactive component in Tripterygium wilfordii extracts, possess strong anti-proliferative activity on all 60-national cancer institute (NCI) cancer cell lines. The antitumor property of triptolide has made it become a promising anti-cancer drug. However, the widespread use of triptolide in the clinical practice is greatly limited for its multi-organ toxicity and narrow therapeutic window. All the toxic characteristics of triptolide are associated with the pharmacokinetics especially its distribution and accumulation in the target organ. The article presents a comprehensive review of the prec...
Source: Current Drug Metabolism - August 16, 2018 Category: Drugs & Pharmacology Authors: Song W, Liu M, Wu J, Zhai H, Chen Y, Peng Z Tags: Curr Drug Metab Source Type: research

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, reality or dream in managing patients with cardiovascular disease.
Abstract Statins have been a major keystone in the management of patients with atherosclerotic cardiovascular disease. The benefits of inhibiting HMG CoA reductase, via statins, were translated into reduction in LDL-c (cholesterol) with proportionate decrease in cardiovascular events in response to the magnitude of LDL-c reduction. Despite major advances in pharmacological treatments, including the use of high-dose statins, there are urgent need to further reduce future cardiovascular risk. This is in particularly important since 1 out of 5 high-risk atherosclerotic patients who achieve low LDL-c return with a sec...
Source: Current Drug Metabolism - August 16, 2018 Category: Drugs & Pharmacology Authors: Alkhalil M Tags: Curr Drug Metab Source Type: research

Chinese Herbal Medicine Hepatotoxicity: The Evaluation and Recognization Based on Large-scale Evidence Ddatabase.
Abstract This review summarizes the current research status of hepatotoxicity and points out that drug induced liver injury (DILI) remains an important scientific problem that urgently needs to be solved. Due to the special nature of Chinese Herbal medicine and the complexity of its clinical use, it is difficult to identify and evaluate its toxicity and resulting herb induced liver injury (HILI). At the same time, due to a lack of specific indicators, the direct and indirect long-term effects of Chinese Herbal Medicine on the liver are also difficult to be clinically determined. At present, the Roussel Uclaf Causa...
Source: Current Drug Metabolism - August 13, 2018 Category: Drugs & Pharmacology Authors: Liu Z, He X, Wang L, Zhang Y, Hai Y, Gao R Tags: Curr Drug Metab Source Type: research

Understanding and Preventing Adverse Effects of Tacrolimus Metabolization in Transplant Patients.
PMID: 30081785 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 6, 2018 Category: Drugs & Pharmacology Authors: Frohlich E Tags: Curr Drug Metab Source Type: research

Xenobiotic conjugation with dicarboxylic acids.
Abstract Although it is believed widely that the various routes of xenobiotic metabolism are now all known and effectively understood, occasionally there emerges a metabolite that signals a novel biotransformation pathway, especially where the xenobiotic may in some way interact with the myriad processes of intermediary metabolism. There are a few reports in the literature where saturated short-chain dicarboxylic acids have been exploited as conjugating agents and these unusual xenobiotic metabolites subsequently excreted intact in the urine. Examples of this as yet relatively rare Phase II reaction occurring in m...
Source: Current Drug Metabolism - August 3, 2018 Category: Drugs & Pharmacology Authors: Mitchell SC, Steventon GB Tags: Curr Drug Metab Source Type: research

Drug-drug interactions of angiotensin converting enzyme inhibitors mediated by metabolizing enzymes and transporters.
CONCLUSION: Inhibition of metabolizing enzymes and transporter system can markedly alter the concentrations of ACE inhibitors. The genetic polymorphisms in the enzymes in some of the specific isoforms seem to explain the inter-individual differences in ACE inhibitors metabolism, and also the inter-individual variation in the pharmacokinetics of ACE inhibitors may be caused by changes in transporter function. Understanding the knowledge of how ACE inhibitors are metabolized and transported is important in predicting and managing DDIs. The data on the roles of drug metabolizing enzymes and transporters in the DDIs of ACE inh...
Source: Current Drug Metabolism - July 30, 2018 Category: Drugs & Pharmacology Authors: Sun P, Liu K Tags: Curr Drug Metab Source Type: research

Interdisciplinary Research Efforts to Advance Neuropsychopharmacology and Mental Health.
PMID: 30039756 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 26, 2018 Category: Drugs & Pharmacology Authors: Scola G Tags: Curr Drug Metab Source Type: research

Essential Oils: Extraction techniques, Pharmaceutical and Therapeutic potential - A review.
CONCLUSION: This manuscript reviewed the major research studies in the field and discussed several research findings on the chemical composition of essential oils, methods of oil extraction, and application of these oils in pharmaceutical and therapeutic fields. These essential oils can be used as anticancer, antimicrobial, antiviral, and as skin permeation enhancer agents. PMID: 30039757 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 23, 2018 Category: Drugs & Pharmacology Authors: Aziz ZAA, Ahmad A, Setapar SHM, Karakucuk A, Azim MM, Lokhat D, Kamal MA, Ashraf GM Tags: Curr Drug Metab Source Type: research

Genetic determinants of vitamin D-related disorders; focus on vitamin D receptor.
Abstract The endocrine system of vitamin D is involved in an extensive variety of biological processes such as bone metabolism, regulation of cell proliferation and differentiation and modulation of the immune response. The active form of vitamin D, 25-hydroxyvitamin D, binds to vitamin D receptor (VDR) controlling the synthesis of many different proteins. Although numerous studies reported polymorphism in the VDR gene, the impact of the polymorphic alleles on VDR protein function remains unknown. BsmI, ApaI, and TaqI are the three adjacent single nucleotide polymorphisms in intron 8/exon nine at the 3' end of the...
Source: Current Drug Metabolism - July 23, 2018 Category: Drugs & Pharmacology Authors: Abouzid M, Karazniewicz-Lada M, Glowka F Tags: Curr Drug Metab Source Type: research

Drug-Induced Nephrotoxicity and Drug Metabolism in Renal Failure.
PMID: 30009693 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 17, 2018 Category: Drugs & Pharmacology Authors: Huang J Tags: Curr Drug Metab Source Type: research

Thiazide Therapy in Chronic Kidney Disease: Renal and Extra Renal Targets.
Abstract Thiazides are the most commonly used medications for the treatment of mild and moderate hypertension. Despite their recognized effect, the mechanism by which thiazides reduce systemic blood pressure remains uncertain. The prevailing belief is that thiazides reduce blood pressure primarily via enhancement of salt excretion consequent to the inhibition of the Na-Cl cotransporter (NCC) in the distal convoluted tubules (DCT). However, recent reports point to a reduction in peripheral vascular resistance as a major mechanism of anti-hypertensive effect of thiazides. It is plausible that both mechanisms, renal ...
Source: Current Drug Metabolism - July 1, 2018 Category: Drugs & Pharmacology Authors: Pourafshar N, Alshahrani S, Karimi A, Soleimani M Tags: Curr Drug Metab Source Type: research

Optimization of Drugs Pharmacotherapy during Pregnancy Using Physiologically Based Pharmacokinetic Models - An Update.
CONCLUSION: More work is needed to fill the gaps in knowledge needed to more accurately and mechanistically simulate simultaneous exposure of the pregnant mother and her fetus/ embryo to drugs using pregnancy physiologically-based pharmacokinetic modeling approach. PMID: 29962340 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 1, 2018 Category: Drugs & Pharmacology Authors: Idkaidek N, Alsmadi MM Tags: Curr Drug Metab Source Type: research

Relevance of breast cancer resistance protein to brain distribution and central acting drugs: a pharmacokinetic perspective.
CONCLUSIONS: The clinical significance of BCRP in the disposition of drugs is currently undeniable. PMID: 29956624 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 29, 2018 Category: Drugs & Pharmacology Authors: Goncalves J, Bicker J, Alves G, Fortuna A, Falcao A Tags: Curr Drug Metab Source Type: research

Metabolism of Peptide Drugs and Strategies to Improve their Metabolic Stability.
Abstract Peptides are used increasingly as therapeutics and biomarkers because of the development of peptide synthesis technologies. Although peptides are associated with a variety of advantages that include high pharmaceutical activity and low toxicity, the therapeutic use of peptides is limited because of their poor metabolic stability in vivo. The main cause of this instability is that peptides are readily degraded by peptidases distributed widely in the body. This review summarizes peptidases present in the gastrointestinal tract, blood, liver, kidney, nasal cavity and placental barrier, and provides an overvi...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Yao JF, Yang H, Zhao YZ, Xue M Tags: Curr Drug Metab Source Type: research