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Drug efficacy

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https://www.readbyqxmd.com/read/27911475/carboplatin-complexed-and-crgd-conjugated-unimolecular-nanoparticles-for-targeted-ovarian-cancer-therapy
#1
Yuyuan Wang, Liwei Wang, Guojun Chen, Shaoqin Gong
Platinum-based chemotherapy has been widely used to treat cancers including ovarian cancer; however, it suffers from dose-limiting toxicity. Judiciously designed drug nanocarriers can enhance the anticancer efficacy of platinum-based chemotherapy while reducing its systemic toxicity. Herein the authors report a stable and water-soluble unimolecular nanoparticle constructed from a hydrophilic multi-arm star block copolymer poly(amidoamine)-b-poly(aspartic acid)-b-poly(ethylene glycol) (PAMAM-PAsp-PEG) conjugated with both cRGD (cyclo(Arg-Gly-Asp-D-Phe-Cys) peptide and cyanine5 (Cy5) fluorescent dye as a platinum-based drug nanocarrier for targeted ovarian cancer therapy...
December 1, 2016: Macromolecular Bioscience
https://www.readbyqxmd.com/read/27911474/is-chelation-therapy-efficient-for-the-treatment-of-intravenous-metallic-mercury-intoxication
#2
Daniela Pelclova, Stepanka Vlckova, Ondrej Bezdicek, Manuela Vaneckova, Pavel Urban, Petr Ridzon, Pavel Diblik, Tomas Navratil, Pavlina Klusackova, Kamil Vlcek, Olga Benesova, Pavel Trestik, Jiri Homolka, Sergey Zakharov
The efficacy of treatment for intravenous elemental mercury intoxication has not been fully studied with regard to clinical outcomes, and treatment recommendations vary. We treated a 41-year-old man with a history of drug abuse and depression who attempted suicide using 1 mL (13.53 g) metallic Hg i.v. He was admitted to the hospital two months later for dyspnoea and thoracic pain and was diagnosed with pneumonia. Hg deposits were seen in the lungs and extra-pulmonary organs. His blood level (372 μg/L) exceeded the population level of 5 μg/L by more than 70-fold...
December 2, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/27910962/baricitinib-jak-inhibition-for-rheumatoid-arthritis
#3
J Gras
Rheumatoid arthritis (RA), a chronic autoimmune inflammatory disease characterized by inflammation and joint destruction, is associated with pain, progressive disability, systemic comorbidities and early death. Conventional disease-modifying antirheumatic drugs (DMARDs) and biological DMARDs (bDMARDs) have been able to achieve remission or a very low disease activity status for RA. Nevertheless, since many patients do not reach a sufficient response with DMARDs or present with unacceptable side effects, new therapies are needed...
October 2016: Drugs of Today
https://www.readbyqxmd.com/read/27910899/glial-pannexin1-contributes-to-tactile-hypersensitivity-in-a-mouse-model-of-orofacial-pain
#4
Regina Hanstein, Menachem Hanani, Eliana Scemes, David C Spray
Drug studies in animal models have implicated pannexin1 (Panx1) in various types of pain, including trigeminal hypersensitivity, neuropathic pain and migraine. However, the tested drugs have limited specificity and efficacy so that direct evidence for Panx1 contribution to pain has been lacking. We here show that tactile hypersensitivity is markedly attenuated by deletion of Panx1 in a mouse model of chronic orofacial pain; in this model, trigeminal ganglion Panx1 expression and function are markedly enhanced...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27910877/a-comprehensive-map-of-molecular-drug-targets
#5
Rita Santos, Oleg Ursu, Anna Gaulton, A Patrícia Bento, Ramesh S Donadi, Cristian G Bologa, Anneli Karlsson, Bissan Al-Lazikani, Anne Hersey, Tudor I Oprea, John P Overington
The success of mechanism-based drug discovery depends on the definition of the drug target. This definition becomes even more important as we try to link drug response to genetic variation, understand stratified clinical efficacy and safety, rationalize the differences between drugs in the same therapeutic class and predict drug utility in patient subgroups. However, drug targets are often poorly defined in the literature, both for launched drugs and for potential therapeutic agents in discovery and development...
December 2, 2016: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/27910808/magnesium-and-depression
#6
Anna Serefko, Aleksandra Szopa, Ewa Poleszak
Magnesium is one of the most important elements in the human body and is involved in a number of biochemical processes crucial for the proper functioning of the cardiovascular, alimentary, endocrine, and osteoarticular systems. It also plays a vital modulatory role in brain biochemistry, influencing several neurotransmission pathways associated with the development of depression. Personality changes, including apathy, depression, agitation, confusion, anxiety, and delirium are observed when there is a deficiency of this element...
March 1, 2016: Magnesium Research: Official Organ of the International Society for the Development of Research on Magnesium
https://www.readbyqxmd.com/read/27910784/hepatoprotective-effect-of-tricholoma-giganteum-agaricomycetes-in-a-nonalcoholic-fatty-liver-disease-rat-model
#7
Ramar Govindaraj, Michael Gabriel Paulraj, Erenius Toppo, Perumal Pandikumar, Savarimuthu Ignacimuthu, Naif Abdhullah Al-Dhabi
Different concentrations of standardized ethanolic extract from the basidiocarps of Tricholoma giganteum Massee (TgEtOH) were screened for hepatoprotective effects in an animal model of rats with nonalcoholic fatty liver disease (NAFLD) fed a high-fat and high-fructose diet. After 4 weeks of treatment with TgEtOH, the relative liver weights, serum lipid concentrations, and biochemical profiles were found to be normal in treated animals compared with those given a standard drug. The macroscopic and histopathological studies clearly indicated that 200 mg/kg of ethanolic extract was effective in ameliorating the abnormalities of NAFLD...
2016: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/27910742/review-article-fabricated-microparticles-an-innovative-method-to-minimize-the-side-effects-of-nsaids-in-arthritis
#8
Shaivad Shabee Hulhasan Abadi, Afrasim Moin, Gangadharappa Hosahalli Veerabhadrappa
Microparticles are polymeric bodies ranging 1-1000 µm that constitute a variety of forms such as microcapsules, microspheres, microcages, microshells, microrods, biosensors microparticles, radiolabeled microparticles, and so forth. This review focuses on general microparticles, mainly microcapsules and microspheres. Nonsteriodal anti-inflammatory drugs (NSAIDs) are one of the mostcommonly prescribed medications in the world. Most of the NSAIDs available have severe side effects. With increased awareness of NSAID-induced gastrointestinal (GI) side effects, safety has become a priority in treatment of arthritis and other inflammatory diseases with NSAIDs...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27910740/oral-squamous-cell-carcinoma-current-treatment-strategies-and-nanotechnology-based-approaches-for-prevention-and-therapy
#9
Sankalp A Gharat, Munira Momin, Chintan Bhavsar
Oral squamous cell carcinoma (OSCC) is the most common type of oral cancer; it involves damage to oral epithelial cells due to accumulation of multiple genetic mutations in the cells. OSCC remains major cause of morbidity and mortality in patients with head and neck cancers. Tobacco, smoking, alcohol consumption alone or with chewing tobacco, and betel quid are potential carcinogens contributing to the high occurrence of OSCC. Current treatment modalities for OSCC like chemoradiotherapy, surgery, EGFR inhibitors and COX-2 inhibitors, and photodynamic therapy have led to the major problems related to non-specific cell death...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27910739/overview-on-therapeutic-applications-of-microparticulate-drug-delivery-systems
#10
Swarna Bale, Amit Khurana, A Shiva Shankar Reddy, Mandip Singh, Chandraiah Godugu
Research in novel drug delivery systems is being explored competitively in order to attain maximum therapeutic effect while minimizing the adverse effects. Despite several advancements in pharmaceutical formulations, one of the major challenges still persisting is sustained drug release. Microencapsulation enacts as an intelligent approach with a strong therapeutic impact and is in demand globally in medical technology due to its specific and attractive properties, including biocompatibility, stability, target specificity, uniform encapsulation, better compliance, and controlled and sustained release patterns that are responsible for diminishing the toxicity and dosage frequency...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27910713/sn-38-loading-capacity-of-hydrophobic-polymer-blend-nanoparticles-formulation-optimization-and-efficacy-evaluation
#11
Simona Dimchevska, Nikola Geskovski, Gjorgji Petruševski, Marina Chacorovska, Riste Popeski-Dimovski, Sonja Ugarkovic, Katerina Goracinova
One of the most important problems in nanoencapsulation of extremely hydrophobic drugs is poor drug loading due to rapid drug crystallization outside the polymer core. The effort to use nanoprecipitation, as a simple one-step procedure with good reproducibility and FDA approved polymers like Poly(lactic-co-glycolic acid) (PLGA) and Polycaprolactone (PCL), will only potentiate this issue. Considering that drug loading is one of the key defining characteristics, in this study we attempted to examine whether the nanoparticle core composed of two hydrophobic polymers will provide increased drug loading for 7-Ethyl-10-hydroxy-camptothecin (SN-38), relative to nanoparticles prepared using individual polymers...
December 2, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27910185/drug-eluting-balloon-angioplasty-for-below-the-knee-lesions-in-end-stage-renal-disease-patients-with-critical-limb-ischemia-midterm-results
#12
Burak Teymen, Süleyman Aktürk
BACKGROUND: The 1-year restenosis rate after standard balloon angioplasty (BA) of long lesions in below-the-knee arteries may be as high as 70%. Our aim was to investigate the efficacy and safety of paclitaxel drug-eluting balloon (DEB) for treatment of below the knee lesions in end stage renal disease patients (ESRD) with critical limb ischemia (CLI). METHODS: Our study is a retrospective, single-center study. Inclusion criteria were ESRD, critical limb ischemia (Rutherford class 4 or higher) and significant stenosis or occlusion of at least 1 below-the-knee vessel...
December 2, 2016: Journal of Interventional Cardiology
https://www.readbyqxmd.com/read/27910055/selective-pressure-regulated-retroinfusion-for-gene-therapy-application-in-ischemic-heart-disease
#13
Rabea Hinkel, Christian Kupatt
Coronary heart disease is still the leading cause of death in industrialized nations. Even though revascularization strategies such as coronary artery bypass graft surgery, percutaneous coronary intervention and enhanced drug therapy significantly improved the outcome, about 30 % of patients develop chronic heart failure. Ischemic heart disease and heart failure are characterized by an adverse remodeling of the heart, featuring cardiomyocyte hypertrophy, increased fibrosis and capillary rarefaction. Therefore, gene therapeutic approaches for the treatment of heart failure, such as the modulating contractile function or therapeutic neovascularization, seem to be promising...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#14
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27909988/predicting-the-abuse-liability-of-entactogen-class-new-and-emerging-psychoactive-substances-via-preclinical-models-of-drug-self-administration
#15
Shawn M Aarde, Michael A Taffe
Animal models of drug self-administration are currently the gold standard for making predictions regarding the relative likelihood that a recreational drug substance will lead to continued use and addiction. Such models have been found to have high predictive accuracy and discriminative validity for a number of drug classes including ethanol, nicotine, opioids, and psychostimulants such as cocaine and methamphetamine. Members of the entactogen class of psychostimulants (drugs that produce an "open mind state" including feelings of interpersonal closeness, intimacy and empathy) have been less frequently studied in self-administration models...
December 2, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27909980/omalizumab-in-severe-refractory-vernal-keratoconjunctivitis-in-children-case-series-and-review-of-the-literature
#16
Serge Doan, Flore Amat, Eric Gabison, Sarah Saf, Isabelle Cochereau, Jocelyne Just
INTRODUCTION: Vernal keratoconjunctivis (VKC) is a severe form of pediatric ocular allergy, characterized by acute and chronic corneoconjunctival inflammation that may lead to visual sequelae. Although topical immunosuppressive drugs such as cyclosporine are usually effective, some severe forms may be refractory and require prolonged steroid therapy. Very few papers report the use of omalizumab in VKC in the literature. In the present study, we describe our clinical experience with omalizumab in severe VKC children...
December 1, 2016: Ophthalmology and Therapy
https://www.readbyqxmd.com/read/27909950/hatt-a-phase-iv-single-arm-open-label-study-of-sorafenib-in-taiwanese-patients-with-advanced-hepatocellular-carcinoma
#17
Shi-Ming Lin, Sheng-Nan Lu, Ping-Tsung Chen, Long-Bin Jeng, Shinn-Cherng Chen, Chi-Tan Hu, Sien-Sing Yang, Marie-Aude Le Berre, Xuan Liu, David Y Mitchell, Klaas Prins, Joachim Grevel, Carol A E Peña, Gerold Meinhardt
BACKGROUND: Sorafenib significantly improves survival in patients with advanced hepatocellular carcinoma (HCC). This phase IV study assessed sorafenib efficacy/safety in Taiwanese patients with advanced HCC and Child-Pugh A status. METHODS: All patients received 400 mg sorafenib BID. Safety, efficacy, sorafenib pharmacokinetics, and Child-Pugh progression were evaluated. A hand-foot skin reaction (HFSR) prevention substudy assessed HFSR incidence and grade/severity and time to HFSR in 29 and 34 patients randomized to corticosteroid and noncorticosteroid ointments, respectively, and in 88 nonrandomized patients...
December 1, 2016: Hepatology International
https://www.readbyqxmd.com/read/27909713/age-associated-differences-in-transporter-gene-expression-in-kidneys-of-male-rats
#18
Yong-Ji Xu, Yang Wang, Yuan-Fu Lu, Shang-Fu Xu, Qin Wu, Jie Liu
Kidney transporters are involved in the secretion and reabsorption of endogenous and exogenous molecules. Numerous factors may influence their expression and affect drug disposition, efficacy and toxicity. The present study aimed to examine the development‑ and age‑associated variations in primary renal transporters in rats, including 6 uptake transporters: Organic anion transporter (OAT) 1 and 3, organic cation transporter (OCT) 1, 2 and 3 and organic anion‑transporting polypeptide (OATP) 4C1, and 6 efflux transporters: Multidrug resistance protein 1 (MDR1), breast cancer resistance protein (BCRP), multidrug resistance‑associated protein (MRP) 2 and 4, and multidrug and toxin extrusion protein (MATE) 1 and 2‑K...
November 28, 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27909503/first-and-second-generation-cryoballoon-ablation-efficacy-restoring-and-maintaining-sinus-rhythm-in-patients-electrically-selected-and-treated-for-long-standing-persistent-atrial-fibrillation-after-acute-complete-electrical-disconnection-of-pulmonary-veins
#19
Jesus M Paylos Md PhD, Luis Azcona Md, Lourdes Lacal Md, Marisol Paradela Md, Carmen Cilleros Md, Ildefonso Del Campo Md, Clara Ferrero Rn Carlos Martínez Md PhD, Aracelis Morales Md
Introduction Cryoballoon ablation (CB) has proven effective to treatment of patients (pts) with atrial fibrillation (AF). However, the isolated efficacy of CB to treat pts with long-standing persistent atrial fibrillation (LSPAF) is less know. We analyzed the acute results and the long-term follow-up of our pts suffering LSPAF and initially treated with CB. Methods A cohort of 44 pts, 37 male (84%) mean age (60±10 year) suffering LSPAF were treated with first (CB1): 15pts, and second (CB2): 29 pts, generation CB...
April 2016: Journal of Atrial Fibrillation
https://www.readbyqxmd.com/read/27909097/induction-of-migraine-like-photophobic-behavior-in-mice-by-both-peripheral-and-central-cgrp-mechanisms
#20
Bianca N Mason, Eric A Kaiser, Adisa Kuburas, Maria-Cristina M Loomis, John A Latham, Leon F Garcia-Martinez, Andrew F Russo
: The neuropeptide calcitonin gene-related peptide (CGRP) is a key player in migraine. While migraine can be treated using CGRP antagonists that act peripherally, the relevant sites of CGRP action remain unknown. To address the role of CGRP both within and outside the central nervous system, we used CGRP-induced light aversive behavior in mice as a measure of migraine-associated photophobia. Peripheral (intraperitoneal, IP) injection of CGRP resulted in light aversive behavior in wild-type CD1 mice similar to aversion previously seen following central (intracerebroventricular, ICV) injection...
December 1, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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