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https://www.readbyqxmd.com/read/29777772/improving-maraviroc-oral-bioavailability-by-formation-of-solid-drug-nanoparticles
#1
Alison C Savage, Lee M Tatham, Marco Siccardi, Trevor Scott, Manoli Vourvahis, Andrew Clark, Steve P Rannard, Andrew Owen
Oral drug administration remains the preferred approach for treatment of HIV in most patients. Maraviroc (MVC) is the first in class co-receptor antagonist, which blocks HIV entry into host cells. MVC has an oral bioavailability of approximately 33%, which is limited by poor permeability as well as affinity for CYP3A and several drug transporters. While once-daily doses are now the favoured option for HIV therapy, dose-limiting postural hypotension has been of theoretical concern when administering doses high enough to achieve this for MVC (particularly during coadministration of enzyme inhibitors)...
May 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29777765/in-vitro-and-in-vivo-evaluation-of-an-oral-sustained-release-hepatoprotective-caffeine-loaded-w-o-pickering-emulsion-formula-containing-wheat-germ-oil-and-stabilized-by-magnesium-oxide-nanoparticles
#2
Heba Elmotasem, Hala K Farag, Abeer A A Salama
The objective of this study was to innovate an effective oral sustained release hepatoprotective formula for - the water soluble drug - caffeine. Caffeine is rapidly absorbed and eliminated which dictates frequent administration to achieve adequate therapeutic effect. A w/o Pickering emulsion incorporating caffeine in the internal phase was primed. It contained wheat germ oil and was stabilized by synthesized magnesium oxide nanoparticles (MgO NPs). Components selection was based on their antioxidant, hepatoprotective and anticarcinogenic effects...
May 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29769797/protective-effects-of-erigeron-breviscapus-hand-mazz-ebhm-extract-in-retinal-neurodegeneration-models
#3
Jingyuan Zhu, Li Chen, Yun Qi, Jing Feng, Li Zhu, Yujing Bai, Huijuan Wu
Purpose: To investigate the neuroprotective effects of scutellarin, an active component of the multifunctional traditional Chinese herb Erigeron breviscapus (vant.) Hand.-Mazz. (EBHM), which has been used as a neuroprotective therapy for cerebrovascular diseases. We performed the experiments using in vitro and in vivo models of retinal neurodegeneration. Methods: In the in vitro experiments, we exposed BV-2 cells to low oxygen levels in an incubator for 24 and 48 h to generate hypoxia models...
2018: Molecular Vision
https://www.readbyqxmd.com/read/29767545/pharmacogenetics-of-novel-oral-anticoagulants-a-review-of-identified-gene-variants-future-perspectives
#4
Adna Ašić, Damir Marjanović, Jure Mirat, Dragan Primorac
Novel oral anticoagulants (NOACs) are becoming a therapy of choice in everyday clinical practice after almost 50 years during which warfarin and related coumarin derivatives were used as the main anticoagulants. Advantages of NOACs over standard anticoagulants include their predictable pharmacodynamics and pharmacokinetics, stable plasma concentrations and less drug-drug and food-drug interactions. However, pharmacogenetics has its place in administration of NOACs, as considerable interindividual variations have been detected...
May 16, 2018: Personalized Medicine
https://www.readbyqxmd.com/read/29766501/impact-of-gastrointestinal-disease-states-on-oral-drug-absorption-implications-for-formulation-design-a-pearrl-review
#5
REVIEW
Angela Effinger, Caitriona M O'Driscoll, Mark McAllister, Nikoletta Fotaki
OBJECTIVES: Drug product performance in patients with gastrointestinal (GI) diseases can be altered compared to healthy subjects due to pathophysiological changes. In this review, relevant differences in patients with inflammatory bowel diseases, coeliac disease, irritable bowel syndrome and short bowel syndrome are discussed and possible in vitro and in silico tools to predict drug product performance in this patient population are assessed. KEY FINDINGS: Drug product performance was altered in patients with GI diseases compared to healthy subjects, as assessed in a limited number of studies for some drugs...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29748212/tas-114-a-first-in-class-dual-dutpase-dpd-inhibitor-demonstrates-potential-to-improve-therapeutic-efficacy-of-fluoropyrimidine-based-chemotherapy
#6
Wakako Yano, Tatsushi Yokogawa, Takeshi Wakasa, Keisuke Yamamura, Akio Fujioka, Kunihiro Yoshisue, Eiji Matsushima, Seiji Miyahara, Hitoshi Miyakoshi, Junko Taguchi, Khoon Tee Chong, Yayoi Takao, Masayoshi Fukuoka, Kenichi Matsuo
5-Fluorouracil (5-FU) is an antimetabolite and exerts antitumor activity via intracellularly and physiologically complicated metabolic pathways. In this study, we designed a novel small molecule inhibitor, TAS-114, which targets the intercellular metabolism of 5-FU to enhance antitumor activity and modulates catabolic pathway to improve the systemic availability of 5-FU. TAS-114 strongly and competitively inhibited deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase), a gatekeeper protein preventing aberrant base incorporation into DNA, and enhanced the cytotoxicity of fluoropyrimidines in cancer cells; however, it had little intrinsic activity...
May 10, 2018: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29744867/p-glycoprotein-mdr1-abcb1-restricts-brain-accumulation-and-cytochrome-p450-3a-cyp3a-limits-oral-availability-of-the-novel-alk-ros1-inhibitor-lorlatinib
#7
Wenlong Li, Rolf W Sparidans, Yaogeng Wang, Maria C Lebre, Els Wagenaar, Jos H Beijnen, Alfred H Schinkel
Lorlatinib (PF-06463922) is a promising oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor currently in Phase III clinical trials for treatment of non-small cell lung cancer (NSCLC) containing an ALK rearrangement. With therapy-resistant brain metastases a major concern in NSCLC, lorlatinib was designed to have high membrane and blood-brain barrier permeability. We investigated the roles of the multidrug efflux transporters ABCB1 and ABCG2, and the multispecific drug-metabolizing enzyme CYP3A in plasma pharmacokinetics and tissue distribution of lorlatinib using genetically modified mouse strains...
May 9, 2018: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/29742693/a-successful-treatment-of-severe-systemic-lupus-erythematosus-caused-by-occult-pulmonary-infection-associated-with-hemophagocytic-syndrome-a-case-report
#8
Weihong Shi, Mingyang Duan, Ligang Jie, Weifeng Sun
RATIONALE: A 27-year-old woman with a history of systemic lupus erythaematosus (SLE) developed hemophagocytic syndrome (HPS) secondary due to an unrecognized infection that led to severe SLE with a prolonged recovery. PATIENT CONCERNS: The patient showed a high spiking fever and myalgia. Laboratory data revealed pancytopenia and immunological abnormalities. Pulse methylprednisone plus intravenous immunoglobulin (IVIG) failed to improve the clinical symptoms and laboratory data...
May 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29740925/metformin-directly-targets-the-h3k27me3-demethylase-kdm6a-utx
#9
Elisabet Cuyàs, Sara Verdura, Laura Llorach-Pares, Salvador Fernández-Arroyo, Fedra Luciano-Mateo, Noemí Cabré, Jan Stursa, Lukas Werner, Begoña Martin-Castillo, Benoit Viollet, Jiri Neuzil, Jorge Joven, Alfons Nonell-Canals, Melchor Sanchez-Martinez, Javier A Menendez
Metformin, the first drug chosen to be tested in a clinical trial aimed to target the biology of aging per se, has been clinically exploited for decades in the absence of a complete understanding of its therapeutic targets or chemical determinants. We here outline a systematic chemoinformatics approach to computationally predict biomolecular targets of metformin. Using several structure- and ligand-based software tools and reference databases containing 1,300,000 chemical compounds and more than 9,000 binding sites protein cavities, we identified 41 putative metformin targets including several epigenetic modifiers such as the member of the H3K27me3-specific demethylase subfamily, KDM6A/UTX...
May 8, 2018: Aging Cell
https://www.readbyqxmd.com/read/29725991/retreatment-with-pegloticase-after-a-gap-in-therapy-in-patients-with-gout-a-report-of-four-cases
#10
Allan H Morton, Tony Hosey, Brian LaMoreaux
INTRODUCTION: Pegloticase, a potent uricolytic biologic enzyme, has been shown to be an effective therapeutic option in patients with uncontrolled gout. However, there are limited data on clinical response after a gap in therapy and retreatment with pegloticase. CASE SERIES: This report describes four patients with chronic gout who were successfully managed with pegloticase and were retreated following a gap in therapy. Patient charts from a practice-based rheumatology clinic were retrospectively analyzed; four male patients, aged 70-75 years, with chronic gout and a more than 4-week gap in pegloticase therapy were reviewed...
May 3, 2018: Rheumatology and Therapy
https://www.readbyqxmd.com/read/29723068/advances-in-the-discovery-of-cathepsin-k-inhibitors-on-bone-resorption
#11
Jun Lu, Maolin Wang, Ziyue Wang, Zhongqi Fu, Aiping Lu, Ge Zhang
Cathepsin K (Cat K), highly expressed in osteoclasts, is a cysteine protease member of the cathepsin lysosomal protease family and has been of increasing interest as a target of medicinal chemistry efforts for its role in bone matrix degradation. Inhibition of the Cat K enzyme reduces bone resorption and thus, has rendered the enzyme as an attractive target for anti-resorptive osteoporosis therapy. Over the past decades, considerable efforts have been made to design and develop highly potent, excellently selective and orally applicable Cat K inhibitors...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29713542/systematic-review-of-antioxidant-types-and-doses-in-male-infertility-benefits-on-semen-parameters-advanced-sperm-function-assisted-reproduction-and-live-birth-rate
#12
Ahmad Majzoub, Ashok Agarwal
Objective: To explore the current evidence concerning the effect of oral antioxidant supplementation on various male fertility outcomes, as antioxidants are widely available compounds that are commonly used for the treatment of male infertility. Materials and methods: PubMed, Medline and Cochrane electronic databases were searched according to a modified Preferred Reporting Items for Systemic Reviews and Meta-Analyses (PRISMA) guidelines looking for studies investigating the effect of antioxidant therapy on infertile men...
March 2018: Arab Journal of Urology
https://www.readbyqxmd.com/read/29713181/minodronate-for-the-treatment-of-osteoporosis
#13
REVIEW
Tsuyoshi Ohishi, Yukihiro Matsuyama
Minodronate is a third-generation bisphosphonate that was developed and approved for clinical use in osteoporosis therapy in Japan. The mechanism of action for suppressing bone resorption is the inhibition of farnesyl pyrophosphate synthase, a key enzyme in the mevalonic acid metabolic pathway of osteoclasts, to induce apoptosis of the cells. Minodronate is the strongest inhibitor of bone resorption among the currently available oral bisphosphonates. Large randomized, placebo-controlled, double-blind clinical trials have revealed an increase in bone mineral density of both the lumbar spine and femoral neck over 3 years of daily minodronate therapy and risk reduction in vertebral fractures over 2 years of therapy...
2018: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/29712435/prolyl-hydroxylase-inhibitors-a-breakthrough-in-the-therapy-of-anemia-associated-with-chronic-diseases
#14
Amit Arvind Joharapurkar, Vrajesh Bhaskarbhai Pandya, Vishal J Patel, Ranjit C Desai, Mukul R Jain
Chronic kidney disease, cancer, chronic inflammatory disorders, nutritional and genetic deficiency can cause anemia. Hypoxia causes induction of hypoxia-inducible factor (HIF), which stimulates erythropoietin (EPO) synthesis. Prolyl hydroxylase domain (PHD) enzyme inhibition can stabilize hypoxia-inducible factor (HIF). HIF stabilization also decreases hepcidin, a hormone of hepatic origin, which regulates iron homeostasis. PHD inhibitors represent the novel pharmacological treatment of anemia of chronic diseases...
May 1, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29710546/pharmacokinetic-interaction-of-diosmetin-and-silibinin-with-other-drugs-inhibition-of-cyp2c9-mediated-biotransformation-and-displacement-from-serum-albumin
#15
Miklós Poór, Gabriella Boda, Violetta Mohos, Mónika Kuzma, Mónika Bálint, Csaba Hetényi, Tímea Bencsik
Diosmin and silibinin (SIL) are polyphenolic compounds which are the active components of several drugs and dietary supplements. After the oral administration of diosmin (flavonoid glycoside), only its aglycone diosmetin (DIO) reaches the systemic circulation. Both DIO and SIL form complexes with serum albumin and are able to inhibit several cytochrome P450 enzymes. Therefore, it is reasonable to hypothesize that these polyphenols may displace some drugs from serum albumin and inhibit their biotransformation, potentially leading to the disruption of drug therapy...
March 31, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29710045/antidiabetic-naphthoquinones-and-their-plant-resources-in-thailand
#16
Muhammad Ajmal Shah, James E Keach, Pharkphoom Panichayupakaranant
Diabetes mellitus is the seventh leading cause of death globally. Ninety percent of the diabetic population suffers from type-2 diabetes, which still needs an effective, safe and economical oral hypoglycemic therapy. Plants are rich sources of various therapeutic molecules. More than 400 medicinal plants of interesting phytochemical diversity have been reported for their antidiabetic potential. Naphthoquinones are a group of phytochemicals, which have a wide range of pharmacological potential, including antidiabetic activity...
2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29692238/advances-in-the-development-of-novel-factor-xa-inhibitors-a-patent-review
#17
Atul N Khadse, Mayank Kumar Sharma, Prashant R Murumkar, Sadhana J Rajput, Mange Ram Yadav
Development of new anticoagulants has been in constant demand throughout the world due to increasing rate of morbidity and mortality caused by thrombotic diseases. Factor Xa (FXa), one of the enzymes and validated target for anticoagulation, regulates the production of thrombin in the coagulation cascade. The importance of oral FXa inhibitors like rivaroxaban, apixaban and edoxaban in thromboembolic conditions is well supported by increasing number of patents and research publications during the recent years...
April 24, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29663576/neuroprotection-by-post-stroke-administration-of-an-oral-formulation-of-angiotensin-1-7-in-ischemic-stroke
#18
Douglas M Bennion, Chad H Jones, Lauren L Donnangelo, Justin T Graham, Jacob D Isenberg, Alex N Dang, Vermali Rodriguez, Ruben D M Sinisterra, Frederico B Sousa, Robson A S Santos, Colin Sumners
NEW FINDINGS: What is the central question of this study? Angiotensin-(1-7) decreases cerebral infarct volume and improves neurological function when delivered centrally prior to and during ischemic stroke. Here, we assessed the neuroprotective effects of angiotensin-(1-7) when delivered orally post-stroke. What is the main finding and its importance? We show that oral delivery of angiotensin-(1-7) attenuates cerebral damage induced by middle cerebral artery occlusion in rats, without affecting blood pressure or cerebral blood flow...
April 16, 2018: Experimental Physiology
https://www.readbyqxmd.com/read/29663414/bidirectional-pharmacokinetic-interaction-between-amodiaquine-and-pioglitazone-in-healthy-subjects
#19
Opeyemi Edema, Babatunde A Adeagbo, Ayorinde Adehin, Tiwalade A Olugbade
Amodiaquine (AQ) and pioglitazone (PGZ) are both metabolized by CYP2C8, an enzyme also inhibited by PGZ. These drugs are likely to be administered in instances of comorbidity of malaria with type 2 diabetes. This study, hence, evaluated the possibility of a drug interaction resulting from the concurrent use of both drugs. A 3-period crossover design in 10 healthy subjects, that assessed the disposition of AQ and PGZ alone and when coadministered, was implemented with the administration of single oral doses of AQ and PGZ...
April 17, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29661968/correction-oral-pharmacological-chaperone-migalastat-compared-with-enzyme-replacement-therapy-in-fabry-disease-18-month-results-from-the-randomised-phase-iii-attract-study
#20
(no author information available yet)
No abstract text is available yet for this article.
April 16, 2018: Journal of Medical Genetics
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