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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28615927/p-tsa-promoted-syntheses-of-5h-benzo-h-thiazolo-2-3-b-quinazoline-and-indeno-1-2-d-thiazolo-3-2-a-pyrimidine-analogs-molecular-modeling-and-in-vitro-antitumor-activity-against-hepatocellular-carcinoma
#1
Amit K Keshari, Ashok K Singh, Vinit Raj, Amit Rai, Prakruti Trivedi, Balaram Ghosh, Umesh Kumar, Atul Rawat, Dinesh Kumar, Sudipta Saha
In our efforts to address the rising incidence of hepatocellular carcinoma (HCC), we have made a commitment to the synthesis of novel molecules to combat Hep-G2 cells. A facile and highly efficient one-pot, multicomponent reaction has been successfully devised utilizing a p-toluenesulfonic acid (p-TSA)-catalyzed domino Knoevenagel/Michael/intramolecular cyclization approach for the synthesis of novel 5H-benzo[h]thiazolo[2,3-b]quinazoline and indeno[1,2-d] thiazolo[3,2-a]pyrimidine analogs bearing a bridgehead nitrogen atom...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28579758/development-of-antiproliferative-long-circulating-liposomes-co-encapsulating-doxorubicin-and-curcumin-through-the-use-of-a-quality-by-design-approach
#2
Lucia Ruxandra Tefas, Bianca Sylvester, Ioan Tomuta, Alina Sesarman, Emilia Licarete, Manuela Banciu, Alina Porfire
The aim of this work was to use the quality-by-design (QbD) approach in the development of long-circulating liposomes co-loaded with curcumin (CUR) and doxorubicin (DOX) and to evaluate the cytotoxic potential of these liposomes in vitro using C26 murine colon carcinoma cell line. Based on a risk assessment, six parameters, namely the phospholipid, CUR and DOX concentrations, the phospholipid:cholesterol molar ratio, the temperature during the evaporation and hydration steps and the pH of the phosphate buffer, were identified as potential risk factors for the quality of the final product...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28579757/profile-of-sarilumab-and-its-potential-in-the-treatment-of-rheumatoid-arthritis
#3
REVIEW
Maria Gabriella Raimondo, Martina Biggioggero, Chiara Crotti, Andrea Becciolini, Ennio Giulio Favalli
In recent years the use of biotechnological agents has drastically revolutionized the therapeutic approach and the progression of rheumatoid arthritis (RA). In particular, interleukin-6 (IL-6) has been demonstrated as a pivotal cytokine in the pathogenesis of the disease by contributing to both the innate and the adaptive immune system perturbation, and to the production of acute-phase proteins involved in the systemic expression of the disorder. The first marketed IL-6 blocker was tocilizumab, a humanized anti-IL-6 receptor (anti-IL-6R) monoclonal antibody...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28579756/effect-of-a-food-supplement-containing-berberine-monacolin-k-hydroxytyrosol-and-coenzyme-q10-on-lipid-levels-a-randomized-double-blind-placebo-controlled-study
#4
Sergio D'Addato, Luciana Scandiani, Giuliana Mombelli, Francesca Focanti, Federica Pelacchi, Enrica Salvatori, Giorgio Di Loreto, Alessandro Comandini, Pamela Maffioli, Giuseppe Derosa
PURPOSE: To evaluate the ability of the new food supplement, Body Lipid (BL), containing red yeast rice, berberine, coenzyme Q10 and hydroxytyrosol, to lower the LDL-C in patients with mild-to-moderate hypercholesterolemia and to assess the overall safety profile of the product. METHODS: In this multicenter, randomized, double-blind, placebo and active comparator (the marketed Armolipid Plus(®) [AM]) controlled study, 158 hypercholesterolemic patients were randomized following a 4-week dietary run-in period...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28579755/past-and-current-perspective-on-new-therapeutic-targets-for-type-ii-diabetes
#5
REVIEW
Pradip D Patil, Umesh B Mahajan, Kalpesh R Patil, Sandip Chaudhari, Chandragouda R Patil, Yogeeta O Agrawal, Shreesh Ojha, Sameer N Goyal
Loss of pancreatic β-cell function is a hallmark of Type-II diabetes mellitus (DM). It is a chronic metabolic disorder that results from defects in both insulin secretion and insulin action. Recently, United Kingdom Prospective Diabetes Study reported that Type-II DM is a progressive disorder. Although, DM can be treated initially by monotherapy with oral agent; eventually, it may require multiple drugs. Additionally, insulin therapy is needed in many patients to achieve glycemic control. Pharmacological approaches are unsatisfactory in improving the consequences of insulin resistance...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28572721/outcome-of-stroke-patients-receiving-different-doses-of-recombinant-tissue-plasminogen-activator
#6
Cheung-Ter Ong, Yi-Sin Wong, Chi-Shun Wu, Yu-Hsiang Su
BACKGROUND AND PURPOSE: Intravenous recombinant tissue plasminogen activator (tPA) at a dose of 0.9 mg/kg body weight is associated with a high hemorrhagic transformation (HT) rate. Low-dose tPA (0.6 mg/kg) may have a lower hemorrhage rate but the mortality and disability rates at 90 days cannot be confirmed as non-inferior to standard-dose tPA. Whether the doses 0.7 and 0.8 mg/kg have better efficacy and safety needs further investigation. Therefore, this study is to compare the efficacy and safety of each dose of tPA (0...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28572720/an-in-silico-high-throughput-screen-identifies-potential-selective-inhibitors-for-the-non-receptor-tyrosine-kinase-pyk2
#7
Tomer Meirson, Abraham O Samson, Hava Gil-Henn
The non-receptor tyrosine kinase proline-rich tyrosine kinase 2 (Pyk2) is a critical mediator of signaling from cell surface growth factor and adhesion receptors to cell migration, proliferation, and survival. Emerging evidence indicates that signaling by Pyk2 regulates hematopoietic cell response, bone density, neuronal degeneration, angiogenesis, and cancer. These physiological and pathological roles of Pyk2 warrant it as a valuable therapeutic target for invasive cancers, osteoporosis, Alzheimer's disease, and inflammatory cellular response...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553083/cisplatin-induces-protective-autophagy-through-activation-of-becn1-in-human-bladder-cancer-cells
#8
Ji-Fan Lin, Yi-Chia Lin, Te-Fu Tsai, Hung-En Chen, Kuang-Yu Chou, Thomas I-Sheng Hwang
PURPOSE: Cisplatin-based chemotherapy is the first line treatment for several cancers including bladder cancer (BC). Autophagy induction has been implied to contribute to cisplatin resistance in ovarian cancer; and a high basal level of autophagy has been demonstrated in human bladder tumors. Therefore, it is reasonable to speculate that autophagy may account for the failure of cisplatin single treatment in BC. This study investigated whether cisplatin induces autophagy and the mechanism involved using human BC cell lines...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553082/ten-years-of-biosimilars-in-europe-development-and-evolution-of-the-regulatory-pathways
#9
REVIEW
Martin Schiestl, Markus Zabransky, Fritz Sörgel
A biosimilar is defined by the European Medicines Agency as a biological medicine that is similar to another biological medicine that has already been authorized for use. A science-based regulatory framework to ensure high-quality biosimilars has been established in Europe since 2005 and is monitored and updated on an ongoing basis. The guiding principle of a biosimilar development program is to establish similarity between the biosimilar and the reference medicine by the best possible means, ensuring that the previously proven safety and efficacy of the reference medicinal product also applies to the biosimilar...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553081/ten-years-of-biosimilar-recombinant-human-growth-hormone-in-europe
#10
REVIEW
Paul Saenger
Recombinant human growth hormone (rhGH) has been in clinical use for more than 30 years. With the expiration of patent exclusivity for the first wave of rhGH products and other biopharmaceuticals, the opportunity emerged for the development of biosimilar medicines. A biosimilar is defined by the European Medicines Agency (EMA) as a biological medicine that is similar to another biological medicine that has already been authorized for use. The EMA led the way (well ahead of the Food and Drug Administration in the US) in developing the biosimilar concept, and the type of science-based regulatory framework required to ensure high-quality, safe, and effective biosimilar medicines; the provisions for approval of biosimilars have been in place in Europe since 2005...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553080/ten-years-of-clinical-experience-with-biosimilar-human-growth-hormone-a-review-of-safety-data
#11
REVIEW
Maria Victoria Borrás Pérez, Berit Kriström, Tomasz Romer, Mieczyslaw Walczak, Nadja Höbel, Markus Zabransky
Safety concerns for recombinant human growth hormone (rhGH) treatments include impact on cancer risk, impact on glucose homeostasis, and the formation of antibodies to endogenous/exogenous GH. Omnitrope(®) (biosimilar rhGH) was approved by the European Medicines Agency in 2006, with approval granted on the basis of comparable quality, safety, and efficacy to the reference medicine (Genotropin(®)). Additional concerns that may exist in relation to biosimilar rhGH include safety in indications granted on the basis of extrapolation and the impact of changing to biosimilar rhGH from other rhGH treatments...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553079/ten-years-clinical-experience-with-biosimilar-human-growth-hormone-a-review-of-efficacy-data
#12
REVIEW
Juan Pedro López-Siguero, Roland Pfäffle, Philippe Chanson, Mieczyslaw Szalecki, Nadja Höbel, Markus Zabransky
In 2006, the European Medicines Agency (EMA) approved Omnitrope(®) as a biosimilar recombinant human growth hormone (rhGH), on the basis of comparable quality, safety, and efficacy to the reference medicine (Genotropin(®), Pfizer). Data continue to be collected on the long-term efficacy of biosimilar rhGH from several on-going postapproval studies. Particular topics of interest include efficacy in indications granted on the basis of extrapolation, and whether efficacy of growth hormone treatment is affected when patients are changed to biosimilar rhGH from other rhGH products...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553078/effects-of-metformin-extended-release-compared-to-immediate-release-formula-on-glycemic-control-and-glycemic-variability-in-patients-with-type-2-diabetes
#13
Giuseppe Derosa, Angela D'Angelo, Davide Romano, Pamela Maffioli
PURPOSE: The purpose of this study is to evaluate, in a randomized clinical trial, the effects of metformin immediate release (IR) compared with metformin extended release (XR) on the gastrointestinal tolerability and glycemic control. MATERIALS AND METHODS: We enrolled 253 Caucasian patients with type 2 diabetes not well controlled by diet (glycated hemoglobin [HbA1c] >7.0% and <8.5%). Patients were randomized to metformin IR or metformin XR for a period of 6 months at the maximum tolerated dose...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553077/spotlight-on-dupilumab-in-the-treatment-of-atopic-dermatitis-design-development-and-potential-place-in-therapy
#14
REVIEW
Angelo Massimiliano D'Erme, Marco Romanelli, Andrea Chiricozzi
Atopic dermatitis (AD) is among the most common inflammatory skin diseases in children and adults in industrialized countries. Up to one-third of adults (probably a smaller proportion in childhood) suffer from moderate-to-severe AD, whose recommended treatment is usually based on systemic therapies. The currently available therapeutics are limited, and AD management becomes challenging in most cases. Over the last few years, new advances in the understanding of AD pathogenic mechanisms and inflammatory pathways have led to the identification of specific therapeutic targets and new molecules have been tested...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553076/higher-dose-of-palonosetron-versus-lower-dose-of-palonosetron-plus-droperidol-to-prevent-postoperative-nausea-and-vomiting-after-eye-enucleation-and-orbital-hydroxyapatite-implant-surgery-a-randomized-double-blind-trial
#15
Xiao Hu, Fang Tan, Lan Gong
OBJECTIVE: Postoperative nausea and vomiting (PONV) is commonly observed after eye enucleation and orbital hydroxyapatite implant surgery. This prospective, randomized, double-blind trial was conducted to investigate the hypothesis that compared with monotherapy using a higher dose of palonosetron, using a lower dose of palonosetron in combination with droperidol could reduce the incidence of PONV and achieve similar prophylaxis against PONV after the aforementioned surgery. PATIENTS AND METHODS: A total of 129 patients who were in the American Society of Anesthesiologists Classes I and II, aged between 18 and 70 years, and scheduled for eye enucleation and orbital hydroxyapatite implant surgery, were enrolled in this study...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553075/fabrication-characterization-and-in-vitro-evaluation-of-silibinin-nanoparticles-an-attempt-to-enhance-its-oral-bioavailability
#16
Muhammad Umar Khayam Sahibzada, Abdul Sadiq, Shahzeb Khan, Hani S Faidah, Naseemullah, Muhammad Khurram, Muhammad Usman Amin, Abdul Haseeb
BACKGROUND: Silibinin has gained in importance in the past few decades as a hepatoprotector and is used widely as oral therapy for toxic liver damage, liver cirrhosis, and chronic inflammatory liver diseases, as well as for the treatment of different types of cancers. Unfortunately, it has low aqueous solubility and inadequate dissolution, which results in low oral bioavailability. MATERIALS AND METHODS: In this study, nanoparticles (NPs) of silibinin, which is a hydrophobic drug, were manufactured using two cost-effective methods...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553074/design-synthesis-and-biological-evaluation-of-novel-ef24-and-ef31-analogs-as-potential-i%C3%AE%C2%BAb-kinase-%C3%AE-inhibitors-for-the-treatment-of-pancreatic-cancer
#17
Xuemeng Xie, Jinfu Tu, Heyi You, Bingren Hu
Given the important role that inhibitory kappa B (IκB) kinase β (IKKβ) plays in pancreatic cancer (PC) development and progression, inhibitors targeting IKKβ are believed to be increasingly popular as novel anti-PC therapies. Two synthetic molecules, named EF24 and EF31, exhibited favorable potential in terms of inhibition of both IKKβ activity and PC cell proliferation. Aiming to enhance their cellular efficacy and to analyze their structure-activity relationship, four series of EF24 and EF31 analogs were designed and synthesized...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28553073/involvement-of-nf-%C3%AE%C2%BAb-and-hsp70-signaling-pathways-in-the-apoptosis-of-mda-mb-231-cells-induced-by-a-prenylated-xanthone-compound-%C3%AE-mangostin-from-cratoxylum-arborescens-retraction
#18
(no author information available yet)
[This retracts the article on p. 1629 in vol. 8.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28546740/new-developments-in-managing-opioid-addiction-impact-of-a-subdermal-buprenorphine-implant
#19
REVIEW
MariaLisa Itzoe, Michael Guarnieri
Opioid addiction to prescription and illicit drugs is a serious and growing problem. In the US alone, >2.4 million people suffer from opioid use disorder. Government and pharmaceutical agencies have begun to address this crisis with recently released and revised task forces and medication-assisted therapies (MAT). For decades, oral or intravenous (IV) MATs have helped patients in their recovery by administration of opioid agonists (methadone, buprenorphine, oxycodone), antagonists (naltrexone, naloxone), and combinations of the two (buprenorphine/naloxone)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28533680/preparation-characterization-and-in-vitro-vivo-studies-of-oleanolic-acid-loaded-lactoferrin-nanoparticles
#20
Xiaojing Xia, Haowei Liu, Huixia Lv, Jing Zhang, Jianping Zhou, Zhiying Zhao
Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailability owing to low solubility (<1 μg/mL) and biomembrane permeability. We developed a novel OA nanoparticle (OA-NP)-loaded lactoferrin (Lf) nanodelivery system with enhanced in vitro OA dissolution and improved oral absorption and bioavailability. The OA-NPs were prepared using NP albumin-bound technology and characterized using dynamic light scattering, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro dissolution test...
2017: Drug Design, Development and Therapy
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