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https://www.readbyqxmd.com/read/29778492/tanovea%C3%A2-for-the-treatment-of-lymphoma-in-dogs
#1
REVIEW
Erik De Clercq
Tanovea® (first named GS-9219, then VDC-1101, generic name: rabacfosadine) is a pro-prodrug or "double" prodrug of PMEG [9-(2-phosphonylmethoxyethyl)guanine], which has been conditionally approved by the US FDA (Food and Drug Administration) for the treatment of lymphoma in dogs. Tanovea has been demonstrated to be effective against non-Hodgkin's lymphoma (NHL) in dogs, as well as canine cutaneous T-cell lymphoma, spontaneous canine multiple myeloma, naïve canine multicentric lymphoma and relapsed canine B-cell lymphoma...
May 17, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29778401/high-intensity-focused-ultrasound-the-fundamentals-clinical-applications-and-research-trends
#2
I A Shehata Elhelf, H Albahar, U Shah, A Oto, E Cressman, M Almekkawy
Diagnostic ultrasound has been clinically used for decades. More recently, high intensity focused ultrasound (HIFU) has been developed for therapeutic use as a non-invasive technique for tissue ablation. HIFU is also being investigated for advanced applications at the cellular level. Under guidance by magnetic resonance or ultrasound imaging, HIFU can achieve precise biological effects in tissue with a high safety profile. In this article, we discuss the basic principles, advantages and limitations of HIFU...
May 17, 2018: Diagnostic and Interventional Imaging
https://www.readbyqxmd.com/read/29777871/pain-therapeutics-from-cone-snail-venoms-from-ziconotide-to-novel-non-opioid-pathways
#3
Helena Safavi-Hemami, Shane E Brogan, Baldomero M Olivera
There have been numerous attempts to develop non-opioid drugs for severe pain, but the vast majority of these efforts have failed. A notable exception is Ziconotide (Prialt®), approved by the FDA in 2004. In this review, we summarize the present status of Ziconotide as a therapeutic drug and introduce a wider framework: the potential of venom peptides from cone snails as a resource providing a continuous pipeline for the discovery of non-opioid pain therapeutics. An auxiliary theme that we hope to develop is that these venoms, already a validated starting point for non-opioid drug leads, should also provide an opportunity for identifying novel molecular targets for future pain drugs...
May 16, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29777783/accelerated-lipid-catabolism-and-autophagy-are-cancer-survival-mechanisms-under-inhibited-glutaminolysis
#4
Anna Halama, Michal Kulinski, Shaima S Dib, Shaza B Zaghlool, Kodappully S Siveen, Ahmad Iskandarani, Jonas Zierer, Kirti S Prabhu, Noothan J Satheesh, Aditya M Bhagwat, Shahab Uddin, Gabi Kastenmüller, Olivier Elemento, Steven S Gross, Karsten Suhre
Suppressing glutaminolysis does not always induce cancer cell death in glutamine dependent tumors because cells may switch to alternative energy sources. To reveal compensatory metabolic pathways, we investigated the metabolome-wide cellular response to inhibited glutaminolysis in cancer cells. Glutaminolysis inhibition with C.968 suppressed cell proliferation but was insufficient to induce cancer cell death. We found that lipid catabolism was activated as a compensation for glutaminolysis inhibition. Accelerated lipid catabolism, together with oxidative stress induced by glutaminolysis inhibition, triggered autophagy...
May 16, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29777201/novel-smoothened-inhibitors-for-therapeutic-targeting-of-na%C3%A3-ve-and-drug-resistant-hedgehog-pathway-driven-cancers
#5
Qing-Rou Li, Hui Zhao, Xue-Sai Zhang, Henk Lang, Ker Yu
The G protein-coupled receptor (GPCR) smoothened (SMO) is a key signaling component of the sonic hedgehog (Hh) pathway and a clinically validated target for cancer treatment. The FDA-approved SMO inhibitors GDC-0449/Vismodegib and LDE225/Sonidegib demonstrated clinical antitumor efficacy. Nevertheless, relatively high percentage of treated patients would eventually develop acquired cross resistance to both drugs. Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29776968/liraglutide-modulates-appetite-and-body-weight-via-glp-1r-expressing-glutamatergic-neurons
#6
Jessica M Adams, Hongjuan Pei, Darleen A Sandoval, Randy J Seeley, Rui B Chang, Stephen D Liberles, David P Olson
Glucagon-like peptide-1 receptor (GLP-1R) agonists are FDA-approved weight loss drugs. Despite their widespread use, the sites of action through which GLP-1R agonists (GLP1RAs) impact appetite and body weight are still not fully understood. Here, we determined whether GLP-1Rs in either GABAergic or glutamatergic neurons are necessary for the acute and chronic effects of the GLP1RA liraglutide on food intake, visceral illness, body weight and neural network activation. We found that mice lacking GLP-1Rs in vGAT -expressing GABAergic neurons responded identically to controls in all parameters measured, whereas deletion of GLP-1Rs in vGlut2 -expressing glutamatergic neurons eliminated liraglutide-induced weight loss and visceral illness and severely attenuated its effects on feeding...
May 18, 2018: Diabetes
https://www.readbyqxmd.com/read/29775725/anti-hepatitis-c-virus-activity-and-synergistic-effect-of-nymphaea-alba-extracts-and-bioactive-constituents-in-liver-infected-cells
#7
Sidra Rehman, Usman Ali Ashfaq, Bushra Ijaz, Sheikh Riazuddin
BACKGROUND: Without an effective vaccine, hepatitis C virus (HCV) remains a global threat, inflicting 170-300 million carriers worldwide at risk of cirrhosis and hepatocellular carcinoma (HCC). Though various direct acting antivirals have been redeemed the hepatitis C treatment, a few restraints persist including possible side effects, viral resistance emergence, excessive cost which restricts its availability to a common person. HYPOTHESIS: There is no preventive HCV vaccine available today so the discovery of potent antiviral natural flora and their bioactive constituents may help to develop preventive cures against HCV infection...
May 15, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29775057/analysis-of-improved-nutritional-composition-of-potential-functional-food-okara-after-probiotic-solid-state-fermentation
#8
Sulagna Gupta, Jaslyn J L Lee, Wei Ning Chen
Okara is a major agro-waste, generated as a byproduct from the soymilk and tofu industry. Since okara has a high nutritive value, reusing it as a substrate for solid state biofermentation is an economical and environmental friendly option. Rhizopus oligosporus and Lactobacillus plantarum were the probiotic FDA-approved food-grade cultures used in this study. The study revealed that biofermenting okara improves its nutritional composition. It was found that the metabolomic composition (by GC-MS analysis) and antioxidant activity (by DPPH test) improved after the microbial fermentations...
May 18, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29774778/an-overview-of-glycopyrrolate-eflow%C3%A2-cs-in-copd
#9
Edward Kerwin, Gary T Ferguson
COPD is highly prevalent in the US and globally, requiring new treatment strategies due to the high disease burden and increase in the aging population. Here, we profile the newly FDA-approved LONHALA MAGNAIR (glycopyrrolate [GLY]/eFlow® Closed System [CS]; 25 mcg twice daily), a nebulized long-acting muscarinic antagonist (LAMA) for the long-term maintenance treatment of COPD, including chronic bronchitis and/or emphysema. Areas covered: An overview of COPD and the treatment landscape, focusing on GLY/eFlow CS, is reported by reviewing the published literature pertinent to the drug/device combination...
May 18, 2018: Expert Review of Respiratory Medicine
https://www.readbyqxmd.com/read/29774560/high-resolution-separation-of-monoclonal-antibodies-mixtures-and-their-charge-variants-by-an-alternative-and-generic-cze-method
#10
Alexandre Goyon, Yannis Nicolas Francois, Olivier Colas, Alain Beck, Jean Luc Veuthey, Davy Guillarme
The determination of mAb critical quality attributes (CQA) is crucial for their successful application in health diseases. A generic CZE method was developed for the high-resolution separation of various mAb charge variants, which are often recognized as important CQA. A dynamic coating of the capillary was obtained with polyethylene oxide (PEO), whereas Bis-Tris allowed the analysis of mAbs under native conditions at pH 7.0. The effect of PEO and Bis-Tris concentrations, as well as the nature of the acidic counter ion on the method performance were systematically studied...
May 17, 2018: Electrophoresis
https://www.readbyqxmd.com/read/29774446/contemporary-review-of-peyronie-s-disease-treatment
#11
REVIEW
Edward Capoccia, Laurence A Levine
PURPOSE: To analyze the literature on the current treatment options for Peyronie's disease (PD). RECENT FINDINGS: Intracavernosal injection therapy using collagenase clostridium histolyticum (CCH) has been widely adopted since its FDA approval in 2013. Based on the current evidence, it appears to be moderately efficacious for men with mild curvatures. Although a recent study has shown similar outcomes using a modified protocol requiring fewer injections, CCH remains an expensive medication...
May 17, 2018: Current Urology Reports
https://www.readbyqxmd.com/read/29774180/survival-prediction-based-on-qualitative-mri-diffusion-signature-in-patients-with-recurrent-high-grade-glioma-treated-with-bevacizumab
#12
Pradeep Goyal, Mary Tenenbaum, Sonali Gupta, Puneet S Kochar, Alok A Bhatt, Manisha Mangla, Yogesh Kumar, Rajiv Mangla
Background: Bevacizumab was approved by the FDA for the treatment of recurrent or progressive glioblastoma (GBM). Imaging responses are typically assessed by gadolinium-enhanced MRI. We sought to determine the significance of qualitative diffusion signature (manifest as variable degree of dark signal) on ADC maps in recurrent gliomas after treatment with bevacizumab. Methods: We performed an institutional review board (IRB) approved retrospective study on patients who underwent MRI of the brain after 8 weeks of receiving bevacizumab for recurrent glioma...
April 2018: Quantitative Imaging in Medicine and Surgery
https://www.readbyqxmd.com/read/29774132/natural-products-a-hope-for-glioblastoma-patients
#13
REVIEW
Raghupathy Vengoji, Muzafar A Macha, Surinder K Batra, Nicole A Shonka
Glioblastoma (GBM) is one of the most aggressive malignant tumors with an overall dismal survival averaging one year despite multimodality therapeutic interventions including surgery, radiotherapy and concomitant and adjuvant chemotherapy. Few drugs are FDA approved for GBM, and the addition of temozolomide (TMZ) to standard therapy increases the median survival by only 2.5 months. Targeted therapy appeared promising in in vitro monolayer cultures, but disappointed in preclinical and clinical trials, partly due to the poor penetration of drugs through the blood brain barrier (BBB)...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29774128/systematic-review-and-meta-analysis-of-selected-toxicities-of-approved-alk-inhibitors-in-metastatic-non-small-cell-lung-cancer
#14
Rubens Barros Costa, Ricardo L B Costa, Sarah M Talamantes, Jason B Kaplan, Manali A Bhave, Alfred Rademaker, Corinne Miller, Benedito A Carneiro, Devalingam Mahalingam, Young Kwang Chae
Introduction: Anaplastic lymphoma kinase ( ALK ) inhibitors are the mainstay treatment for patients with non-small cell lung carcinoma (NSCLC) harboring a rearrangement of the ALK gene or the ROS1 oncogenes. With the recent publication of pivotal trials leading to the approval of these compounds in different indications, their toxicity profile warrants an update. Materials and Methods: A systematic literature search was performed in July 2017. Studies evaluating US FDA approved doses of one of the following ALK inhibitors: Crizotinib, Ceritinib, Alectinib or Brigatinib as monotherapy were included...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29774051/alosetron-use-in-clinical-practice-significant-improvement-in-irritable-bowel-syndrome-symptoms-evaluated-using-the-us-food-and-drug-administration-composite-endpoint
#15
Brian E Lacy, Jean Paul Nicandro, Emil Chuang, David L Earnest
Background: Alosetron is approved to treat women with severe IBS and diarrhea (IBS-D) who have failed standard therapy. In our study, we aimed to evaluate alosetron efficacy using new US Food and Drug Administration (FDA) endpoints and utilization in clinical practice. Methods: This prospective, open-label, multicenter, observational 12-week study evaluated women with severe IBS-D enrolled in the alosetron prescribing program. The coprimary FDA endpoints were changes from baseline in stool consistency and abdominal pain severity...
2018: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/29773910/the-l-type-calcium-channel-blocker-isradipine-attenuates-cue-induced-cocaine-seeking-by-enhancing-dopaminergic-activity-in-the-ventral-tegmental-area-to-nucleus-accumbens-pathway
#16
Nii A Addy, Eric J Nunes, Shannon M Hughley, Keri M Small, Sarah J Baracz, Joshua L Haight, Anjali M Rajadhyaksha
Previous preclinical and clinical investigations have focused on the L-type calcium channel (LTCC) as a potential therapeutic target for substance abuse. While some clinical studies have examined the ability of LTCC blockers to alter cocaine's subjective effects, very few LTCC studies have examined cocaine relapse. Here, we examined whether ventral tegmental area (VTA)-specific or systemic administration of the LTCC inhibitor, isradipine, altered cocaine-seeking behavior in a rat model. Male Sprague-Dawley rats first received 10 days of cocaine self-administration training (2 h sessions), where active lever depression resulted in delivery of a ∼0...
May 3, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29773367/reduction-active-polymeric-prodrug-micelles-based-on-%C3%AE-cyclodextrin-polyrotaxanes-for-triggered-drug-release-and-enhanced-cancer-therapy
#17
Shuang Bai, Meili Hou, Xiaoxiao Shi, Jiucun Chen, Xiaoqian Ma, Yong-E Gao, Yajun Wang, Peng Xue, Yuejun Kang, Zhigang Xu
As one of the medical polymers approved by US Food and Drug Administration (FDA), poly(ethylene glycol) has low toxicity, high stability, good biocompatibility, unique physical and chemical properties. Cyclodextrin is an ideal candidate as a drug carrier due to its special structures and characteristics. These two materials were successfully assembled through chemosynthesis in combination with the hydrophilic poly(ethylene glycol) methyl ether methacrylate (OEGMA) chain and hydrophobic polymeric camptothecin (CPT) chain by atom transfer radical polymerization (ATRP)...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29772457/in-vitro-and-in-vivo-metabolic-investigation-of-the-palbociclib-by-uhplc-q-tof-ms-ms-and-in-silico-toxicity-studies-of-its-metabolites
#18
Balasaheb B Chavan, Shristy Tiwari, Shankar G, Rakesh D Nimbalkar, Prabha Garg, Srinivas R, M V N Kumar Talluri
Palbociclib (PAB) is a CDK4/6 inhibitor and U. S Food and Drug Administration (FDA) granted regular approval for the treatment of hormone receptor (HR) positive, metastatic breast cancer in combination with an aromatase inhibitor in postmenopausal women. Metabolite identification is a crucial aspect during drug discovery and development as the drug metabolites may be pharmacologically active or possess toxicological activity. As there are no reports on the metabolism studies of the PAB, the present study focused on investigation of the in vitro and in vivo metabolic fate of the drug...
May 14, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29772321/use-of-polidocanol-endovenous-microfoam-to-improve-hemodynamics-and-symptomology-in-patients-with-challenging-clinical-presentations-a-case-series
#19
Paul E Davis, John Phillips, Raghu Kolluri
BACKGROUND: We performed a retrospective review of treatment effects with FDA-approved Polidocanol endovenous microfoam (PEM, Varithena® 1%) on venous symptomology in ten (N=10) C3-C6 patients with chronic venous insufficiency (CVI) and concomitant complex disease/pathology that limited the use of endothermal ablation (ETA). METHODS: Pathology included: risk of bruising or bleeding, severe lipodermatosclerosis (LDS), Hydradenitis Suppurativa, chronic fibrosis of the vein from prior superficial thrombosis, risk for nerve injury and failed prior ETA...
May 14, 2018: Annals of Vascular Surgery
https://www.readbyqxmd.com/read/29772289/nose-to-brain-drug-delivery-an-update-on-clinical-challenges-and-progress-towards-approval-of-anti-alzheimer-drugs
#20
REVIEW
Mukta Agrawal, Swarnlata Saraf, Shailendra Saraf, Sophia G Antimisiaris, Mahavir Chougule, Sunday A Shoyele, Amit Alexander
According to the Alzheimer Association Report (2017), Alzheimer's disease (AD) is the 6th primary cause of death in the USA, which affects nearly 5.5 million people. In the year 2017 itself, the cost of AD treatment in the USA has been reported to rise to $259 billion. This statistic shows the severity of the disease in the USA which is very much similar across the globe. On the other hand, the treatment remains limited to a few conventional oral medications (approved by FDA). These are mainly acting superficially from mild to the moderate AD...
May 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
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