Read by QxMD icon Read

Current Drug Metabolism

Clemens Muehlan, Hartmut Fischer, Dieter Zimmer, Hamed Aissaoui, Julien Grimont, Christoph Boss, Marie Croft, Joop van Gerven, Stephan Krähenbühl, Jasper Dingemanse
As part of an integrated and innovative approach to accelerate the clinical development of the dual receptor antagonist ACT-541468, 6 healthy subjects in one cohort in a first-in-humans (FIH) study received an oral dose of 50 mg non-labeled ACT-541468 together with a microtracer amount of 250 nCi of 14C-labeled ACT-541468 to investigate its absorption, distribution, metabolism, and excretion (ADME). Using accelerator mass spectrometry (AMS), radiochromatograms were constructed for fractionated plasma, urine, and feces samples...
February 6, 2019: Current Drug Metabolism
Guillermo Gervasini, Sonia Mota-Zamorano
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...
January 30, 2019: Current Drug Metabolism
Yuhua Yao, Huimin Xu, Manzhi Li, Zhaohui Qi, Bo Liao
BACKGROUND: Some studies have shown that human papillomavirus (HPV) is strongly associated with cervical cancer. As we all know, cervical cancer still remains the fourth most common cancer, affecting women worldwide. Thus, it is both challenging and essential to detect risk types of human papillomaviruses. METHODS: In order to discriminate whether HPV type is highly risky or not, many epidemiological and experimental methods have been proposed recently. For HPV risk type prediction, there also have been a few computational studies which are all based on machine learning (ML) techniques, but adopt different feature extraction methods...
January 17, 2019: Current Drug Metabolism
Shuang Zhou, Qian Xiang, Guangyan Mu, Lingyue Ma, Shuqing Chen, Qiufen Xie, Zhuo Zhang, Yimin Cui
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...
January 10, 2019: Current Drug Metabolism
Guangyue Su, Haifeng Wang, Jiao Bai, Gang Chen, Yuehu Pei
BACKGROUND: The progression of liver disease causes metabolic transformation in vivo and thus affects corresponding endogenous small molecular compounds. Metabonomics is a powerful technology which is able to assess global low-molecular-weight endogenous metabolites in a biological system. This review is intended to provide an overview of a metabonomics approach to the drug toxicology of diseases of the liver. METHODS: The regulation of, and relationship between, endogenous metabolites and diseases of the liver is discussed in detail...
December 31, 2018: Current Drug Metabolism
Panjasaram Naidoo, Manoranjenni Chetty
BACKGROUND: Anecdotal evidence suggests that there may be sex differences in Drug-drug Interactions (DDI) involving specific drugs. Regulators have provided general guidance for the inclusion of females in clinical studies. Some clinical studies have reported sex differences in the Pharmacokinetics (PK) of CYP3A4 substrates, suggesting that DDI involving CYP3A4 substrates could potentially show sex differences. OBJECTIVE: The aim of this review was to investigate whether recent prospective DDI studies have included both sexes and whether there was evidence for the presence or absence of sex differences with the DDIs...
November 28, 2018: Current Drug Metabolism
Anjali Chauhan, Devendra Sillu, Shekhar Agnihotri
BACKGROUND: The limitless presence of pharmaceutical contaminants in discharged wastewater has emerged as a threat to aquatic species and humans. Their presence in drinking water has although raised substantial concerns, very little is known about the fate and ecological impacts of these pollutants. As a result, these pollutants are inevitably introduced to our food chain at trace concentrations. Unfortunately, the conventional wastewater treatment techniques are unable to treat pharmaceuticals completely with practical limitations...
November 26, 2018: Current Drug Metabolism
Pal Patel, Nikita Meghani, Krupa Kansara, Ashutosh Kumar
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 with reference to cancer and rheumatoid arthritis...
November 26, 2018: Current Drug Metabolism
Naga Veera Srikanth Vallabani, Sanjay Singh, Ajay Karakoti
BACKGROUND: Biomedical applications of Magnetic Nanoparticles (MNPs) are creating major impact in disease diagnosis and nanomedicine or a combined platform called theranostics. A significant progress has been made to engineer novel and hybrid MNPs for their multifunctional modalities such as imaging, biosensors, chemotherapeutic or photothermal and antimicrobial agents. MNPs are successfully applied in biomedical applications due to their unique and tunable properties such as superparamagnetism, stability, and biocompatibility...
November 22, 2018: Current Drug Metabolism
Salman Shakil, Ashraful Hasan, Satya Ranjan Sarker
BACKGROUND: Breast cancer is the second leading cause of death in women worldwide. The extremely fast rate of metastasis and ability to develop resistance mechanism to all the conventional drugs make them very difficult to treat which are the causes of high morbidity and mortality of breast cancer patients. Scientists throughout the world have been focusing on the early detection of breast tumor so that treatment can be started at the very early stage. Moreover, conventional treatment processes such as chemotherapy, radiotherapy, and local surgery suffer from various limitations including toxicity, genetic mutation of normal cells, and spreading of cancer cells to healthy tissues...
November 21, 2018: Current Drug Metabolism
Qinghua Wu, Kamil Kuca
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...
October 31, 2018: Current Drug Metabolism
Wei Chen, Pengmian Feng, Tao Liu, Dianchuan Jin
Background: 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...
October 30, 2018: Current Drug Metabolism
Aisling Mangan, Carel Le Roux, Nana Gletsu Miller, Neil Docherty
BACKGROUND: Nutritional deficiencies are common following Roux-en-Y gastric bypass (RYGB). Aetiology is diverse; including unresolved preoperative deficiency, post-operative malabsorption and reduced food intake. Iron and calcium/vitamin D deficiency are particularly troublesome following RYGB. Currently, treatment strategies recommend the prescription of complex regimens of supplements with high doses for those who become deficient. Meanwhile, debate exists regarding the absorption capacity of these post-operatively and their efficacy in treating deficiency...
October 26, 2018: Current Drug Metabolism
Aditi Shah, Souvik Sen Gupta
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...
October 22, 2018: Current Drug Metabolism
Juanhong Zhang, Junmin Zhang, Rong Wang, Zhengping Jia
BACKGROUND: Modern features of drug development such as low permeability, low solubility, and improved release affect the interplay of the gut microbiota and drug metabolism. In recent years, studies have established the impact of plateau hypoxia on gut microbiota, where drug use by plateau populations is affected by hypoxia-induced changes in intestinal microflora-mediated drug metabolism. METHODS: In this review, we summarized the effects of gut microbiota on drug metabolism, and of plateau hypoxia on the intestinal flora, with the aim of providing guidance for the rational use of drugs in high-altitude populations...
October 19, 2018: Current Drug Metabolism
Yi Xiong, Yanhua Qiao, Daisuke Kihara, Hui-Yuan Zhang, Xiaolei Zhu, Dong-Qing Wei
BACKGROUND: Determination or prediction of the absorption, distribution, metabolism, and excretion (ADME) properties of drug candidates and drug-induced toxicity play crucial roles in drug discovery and development. Metabolism is one of the most complicated pharmacokinetic properties to be understood and predicted. However, experimental determination of the substrate binding, selectivity, sites and rates of metabolism is time- and recourse- consuming. In the phase I metabolism of foreign compounds (i...
October 18, 2018: Current Drug Metabolism
Zhongyan Li, Qingqing Miao, Fugang Yan, Yang Meng, Peng Zhou
BACKGROUND: Protein-peptide recognition plays an essential role in the orchestration and regulation of cell signaling networks, which is estimated to be responsible for up to 40% of biological interaction events in the human interactome and has recently been recognized as a new and attractive druggable target for drug development and disease intervention. METHODS: We present a systematic review on the application of machine learning techniques in the quantitative modeling and prediction of protein-peptide binding affinity, particularly focusing on its implications for therapeutic peptide design...
October 12, 2018: Current Drug Metabolism
Delai Xu, Cujin Su, Jie Pan
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...
October 11, 2018: Current Drug Metabolism
Huan-Huan Wei, Wuritu Yang, Hua Tang, Hao Lin
BACKGROUND: Cell-penetrating peptides (CPPs) are important short peptides that facilitate cellular intake or uptake of various molecules. CPPs can transport drug molecules through the plasma membrane and send these molecules to different cellular organelles. Thus, CPP identification and related mechanisms have been extensively explored. In order to reveal the penetration mechanisms of a large number of CPPs, it is necessary to develop convenient and fast methods for CPPs identification...
October 10, 2018: Current Drug Metabolism
Shotaro Uehara, Toru Oshio, Kazuyuki Nakanishi, Etsuko Tomioka, Miyu Suzuki, Takashi Inoue, Yasuhiro Uno, Erika Sasaki, Hiroshi Yamazaki
BACKGROUND: Common marmosets (Callithrix jacchus) are potentially useful nonhuman primate models for preclinical studies. Information for major drug-metabolizing cytochrome P450 (P450) enzymes is now available that supports the use of this primate species as an animal model for drug development. Here, we collect and provide an overview of information on the activities of common marmoset liver and intestine microsomes with respect to 28 typical human P450 probe oxidations. RESULTS: Marmoset P450 2D6/8-dependent R-metoprolol O-demethylation activities in liver microsomes were significantly correlated with those of midazolam 1'- and 4-hydroxylations, testosterone 6β-hydroxylation, and progesterone 6β-hydroxylation, which are probe reactions for marmoset P450 3A4/5/90...
October 3, 2018: Current Drug Metabolism
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"