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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28331294/spotlight-on-blisibimod-and-its-potential-in-the-treatment-of-systemic-lupus-erythematosus-evidence-to-date
#1
REVIEW
Aleksander Lenert, Timothy B Niewold, Petar Lenert
B cells in general and BAFF (B cell activating factor of the tumor necrosis factor [TNF] family) in particular have been primary targets of recent clinical trials in systemic lupus erythematosus (SLE). In 2011, belimumab, a monoclonal antibody against BAFF, became the first biologic agent approved for the treatment of SLE. Follow-up studies have shown excellent long-term safety and tolerability of belimumab. In this review, we critically analyze blisibimod, a novel BAFF-neutralizing agent. In contrast to belimumab that only blocks soluble BAFF trimer but not soluble 60-mer or membrane BAFF, blisibimod blocks with high affinity all three forms of BAFF...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331293/risk-assessment-and-experimental-design-in-the-development-of-a-prolonged-release-drug-delivery-system-with-paliperidone
#2
Sonia Iurian, Luana Turdean, Ioan Tomuta
This study focuses on the development of a drug product based on a risk assessment-based approach, within the quality by design paradigm. A prolonged release system was proposed for paliperidone (Pal) delivery, containing Kollidon(®) SR as an insoluble matrix agent and hydroxypropyl cellulose, hydroxypropyl methylcellulose (HPMC), or sodium carboxymethyl cellulose as a hydrophilic polymer. The experimental part was preceded by the identification of potential sources of variability through Ishikawa diagrams, and failure mode and effects analysis was used to deliver the critical process parameters that were further optimized by design of experiments...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331292/an-open-label-two-period-comparative-study-on-pharmacokinetics-and-safety-of-a-combined-ethinylestradiol-gestodene-transdermal-contraceptive-patch
#3
Chao Zhang, Haiyan Li, Xin Xiong, Suodi Zhai, Yudong Wei, Shuang Zhang, Yuanyuan Zhang, Lin Xu, Li Liu
We investigated the pharmacokinetics and safety profiles of a newly developed combined ethinylestradiol (EE)/gestodene (GSD) transdermal contraceptive patch after a single-dose administration and compared with the market available tablet formulation in healthy adult subjects. An open-label, two-period comparative study was conducted in 12 healthy women volunteers. A single dose of the study combined EE/GE transdermal contraceptive patch and oral tablet (Milunet(®)) were administered. Blood samples at different time points after dose were collected, and concentrations were analyzed...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331291/pharmacokinetics-and-tolerability-of-da-8031-a-novel-selective-serotonin-reuptake-inhibitor-for-premature-ejaculation-in-healthy-male-subjects
#4
Dongseong Shin, SeungHwan Lee, Sojeong Yi, Seo Hyun Yoon, Joo-Youn Cho, Mi Young Bahng, In-Jin Jang, Kyung-Sang Yu
OBJECTIVE: DA-8031 is a selective serotonin reuptake inhibitor under development for the treatment of premature ejaculation. This is the first-in-human study aimed at evaluating the pharmacokinetics and tolerability of DA-8031 and its metabolites (M1, M2, M4, and M5) in the plasma and urine after administration of a single oral dose in healthy male subjects. METHODS: A dose block-randomized, double-blind, placebo-controlled, single ascending dose study was conducted...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331290/effects-of-dexamethasone-coadministered-with-oseltamivir-on-the-pharmacokinetics-of-oseltamivir-in-healthy-volunteers
#5
Kyungho Jang, Min-Kyoung Kim, Jaeseong Oh, SeungHwan Lee, Joo-Youn Cho, Kyung-Sang Yu, Tai Kiu Choi, Sang-Hyuk Lee, Kyoung Soo Lim
PURPOSE: Oseltamivir is widely used in the treatment and prophylaxis of influenza A and B viral infections. It is ingested as an oral prodrug that is rapidly metabolized by carboxylesterase 1 (CES1) to its active form, oseltamivir carboxylate. Dexamethasone is also used in the treatment of acute respiratory distress syndrome, a severe complication of influenza; however, its influence on the pharmacokinetics (PK) of oseltamivir is controversial. The aim of this study was to investigate the effects of coadministering oseltamivir and dexamethasone on the PK of oseltamivir in healthy volunteers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331289/transcriptome-analysis-of-endometrial-tissues-following-gnrh-agonist-treatment-in-a-mouse-adenomyosis-model
#6
Song Guo, Xiaowei Lu, Ruihuan Gu, Di Zhang, Yijuan Sun, Yun Feng
PURPOSE: Adenomyosis is a common, benign gynecological condition of the female reproductive tract characterized by heavy menstrual bleeding and dysmenorrhea. Gonadotropin-releasing hormone (GnRH) agonists are one of the medications used in adenomyosis treatment; however, their underlying mechanisms are poorly understood. Moreover, it is difficult to obtain endometrial samples from women undergoing such treatment. To overcome this, we generated an adenomyosis mouse model, which we treated with an GnRH agonist to determine its effect on pregnancy outcomes...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331288/development-of-venetoclax-for-therapy-of-lymphoid-malignancies
#7
REVIEW
Huayuan Zhu, Alexandru Almasan
B-cell lymphoma-2 (BCL-2) family dysfunction and impairment of apoptosis are common in most B-cell lymphoid malignancies. Venetoclax (Venclexta™, formerly ABT-199, GDC-0199) is a highly selective BCL-2 inhibitor, which mimics its BCL-2 homology 3-domain to induce apoptosis. It was approved for treatment of previously treated chronic lymphocytic leukemia (CLL) patients with 17p deletion early in 2016. It has also been in clinical trials for other B-cell lymphoid malignancies. Unlike the other recently approved targeted agents idelalisib and ibrutinib, so far there has been no relapse reported in some patients...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331287/does-remifentanil-attenuate-renal-ischemia-reperfusion-injury-better-than-dexmedetomidine-in-rat-kidney
#8
E Erkılıç, E Kesimci, F Alaybeyoğlu, I Kılınç, R Tural, A Yazgan, T Gümüş, A Sepici Dinçel, E G Dumlu, O Kanbak
BACKGROUND: Ischemia-reperfusion (I/R) injury is a common cause of patient morbidity and mortality in the perioperative period. Patients undergoing long-lasting, abdominal, and urogenital surgeries with risk factors such as advanced age, peripheral artery disease, diabetes mellitus, renovascular disease, and congestive heart failure are candidates for acute kidney injury (AKI) due to impaired renal perfusion and decreased functional renal reserve. Pharmacological agents with multiple functions and anti-oxidative and anti-inflammation properties may be promising preventative strategies for AKI...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28293103/protective-influence-of-hyaluronic-acid-on-focal-adhesion-kinase-activity-in-human-skin-fibroblasts-exposed-to-ethanol
#9
Magdalena Donejko, Edyta Rysiak, Elżbieta Galicka, Robert Terlikowski, Edyta Katarzyna Głażewska, Andrzej Przylipiak
AIM: The aim of this study was to evaluate the effect of ethanol and hyaluronic acid (HA) on cell survival and apoptosis in cultured human skin fibroblasts. Regarding the mechanism of ethanol action on human skin fibroblasts, we investigated cell viability and apoptosis, expression of focal adhesion kinase (FAK), and the influence of HA on those processes. MATERIALS AND METHODS: Studies were conducted in confluent human skin fibroblast cultures that were treated with 25 mM, 50 mM, and 100 mM ethanol or with ethanol and 500 µg/mL HA...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28293102/paclitaxel-loaded-star-shaped-copolymer-nanoparticles-for-enhanced-malignant-melanoma-chemotherapy-against-multidrug-resistance
#10
Yongsheng Su, Jian Hu, Zhibin Huang, Yubin Huang, Bingsheng Peng, Ni Xie, Hui Liu
Malignant melanoma (MM) is the most dangerous type of skin cancer with annually increasing incidence and death rates. However, chemotherapy for MM is restricted by low topical drug concentration and multidrug resistance. In order to surmount the limitation and to enhance the therapeutic effect on MM, a new nanoformulation of paclitaxel (PTX)-loaded cholic acid (CA)-functionalized star-shaped poly(lactide-co-glycolide) (PLGA)-D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) nanoparticles (NPs) (shortly PTX-loaded CA-PLGA-TPGS NPs) was fabricated by a modified method of nanoprecipitation...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28293101/new-developments-in-the-management-of-partial-onset-epilepsy-role-of-brivaracetam
#11
REVIEW
Giangennaro Coppola, Giulia Iapadre, Francesca Felicia Operto, Alberto Verrotti
Currently, a number of novel anticonvulsant drugs, the so-called third generation, are in various stages of development. Several of them are already available or in ongoing clinical trials. These new compounds should take advantage of new insights into the basic pathophysiology of epileptogenesis, drug metabolism and drug interactions. Many of them still need to be further evaluated mainly in real-world observational trials and registries. Among newer anticonvulsant drugs for partial-onset seizures (POSs), rufinamide, lacosamide, eslicarbazepine and perampanel are those new treatment options for which more substantial clinical evidence is currently available, both in adults and, to some extent, in children...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28293100/adenosine-a2a-receptor-agonist-prevents-cardiac-remodeling-and-dysfunction-in-spontaneously-hypertensive-male-rats-after-myocardial-infarction
#12
Jaqueline S da Silva, Daniele Gabriel-Costa, Roberto T Sudo, Hao Wang, Leanne Groban, Emanuele B Ferraz, José Hamilton M Nascimento, Carlos Alberto M Fraga, Eliezer J Barreiro, Gisele Zapata-Sudo
BACKGROUND: This work evaluated the hypothesis that 3,4-methylenedioxybenzoyl-2-thienylhydrazone (LASSBio-294), an agonist of adenosine A2A receptor, could be beneficial for preventing cardiac dysfunction due to hypertension associated with myocardial infarction (MI). METHODS: Male spontaneously hypertensive rats (SHR) were randomly divided into four groups (six animals per group): sham-operation (SHR-Sham), and myocardial infarction rats (SHR-MI) were treated orally either with vehicle or LASSBio-294 (10 and 20 mg...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28280303/in-silico-discovery-and-in-vitro-activity-of-inhibitors-against-mycobacterium-tuberculosis-7-8-diaminopelargonic-acid-synthase-mtb-bioa
#13
Junie B Billones, Maria Constancia O Carrillo, Voltaire G Organo, Jamie Bernadette A Sy, Nina Abigail B Clavio, Stephani Joy Y Macalino, Inno A Emnacen, Alexandra P Lee, Paul Kenny L Ko, Gisela P Concepcion
Computer-aided drug discovery and development approaches such as virtual screening, molecular docking, and in silico drug property calculations have been utilized in this effort to discover new lead compounds against tuberculosis. The enzyme 7,8-diaminopelargonic acid aminotransferase (BioA) in Mycobacterium tuberculosis (Mtb), primarily involved in the lipid biosynthesis pathway, was chosen as the drug target due to the fact that humans are not capable of synthesizing biotin endogenously. The computational screening of 4...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28280302/defective-dna-repair-mechanisms-in-prostate-cancer-impact-of-olaparib
#14
REVIEW
Francesca De Felice, Vincenzo Tombolini, Francesco Marampon, Angela Musella, Claudia Marchetti
The field of prostate oncology has continued to change dramatically. It has truly become a field that is intensely linked to molecular genetic alterations, especially DNA-repair defects. Germline breast cancer 1 gene (BRCA1) and breast cancer 2 gene (BRCA2) mutations are implicated in the highest risk of prostate cancer (PC) predisposition and aggressiveness. Poly adenosine diphosphate ribose polymerase (PARP) proteins play a key role in DNA repair mechanisms and represent a valid target for new therapies. Olaparib is an oral PARP inhibitor that blocks DNA repair pathway and coupled with BRCA mutated-disease results in tumor cell death...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28280301/eteplirsen-in-the-treatment-of-duchenne-muscular-dystrophy
#15
REVIEW
Kenji Rowel Q Lim, Rika Maruyama, Toshifumi Yokota
Duchenne muscular dystrophy is a fatal neuromuscular disorder affecting around one in 3,500-5,000 male births that is characterized by progressive muscular deterioration. It is inherited in an X-linked recessive fashion and is caused by loss-of-function mutations in the DMD gene coding for dystrophin, a cytoskeletal protein that stabilizes the plasma membrane of muscle fibers. In September 2016, the US Food and Drug Administration granted accelerated approval for eteplirsen (or Exondys 51), a drug that acts to promote dystrophin production by restoring the translational reading frame of DMD through specific skipping of exon 51 in defective gene variants...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28280300/improvement-of-skin-condition-in-striae-distensae-development-characterization-and-clinical-efficacy-of-a-cosmetic-product-containing-punica-granatum-seed-oil-and-croton-lechleri-resin-extract
#16
Cătălina Bogdan, Sonia Iurian, Ioan Tomuta, Mirela Moldovan
Striae distensae are a frequent skin condition associated with pregnancy, weight change or lack of skin elasticity. The aim of this research was to obtain a topical product containing herbal active ingredients with documented antioxidant and anti-inflammatory activity (Punica granatum seed oil and Croton lechleri resin extract) and demonstrate its positive effect on prevention and treatment of striae distensae. First, the cream base formulation was optimized through experimental design. Secondly, the cream containing the two active ingredients was investigated in an interventional nonrandomized clinical trial...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28260864/combined-application-of-dexamethasone-and-hyperbaric-oxygen-therapy-yields-better-efficacy-for-patients-with-delayed-encephalopathy-after-acute-carbon-monoxide-poisoning
#17
Wenping Xiang, Hui Xue, Baojun Wang, Yuechun Li, Jun Zhang, Changchun Jiang, Furu Liang, Jiangxia Pang, Lehua Yu
BACKGROUND: Delayed encephalopathy after acute carbon monoxide (CO) poisoning (DEACMP) commonly occurs after recovering from acute CO poisoning. This study was performed to assess the efficacy of the combined application of dexamethasone and hyperbaric oxygen (HBO) therapy in patients with DEACMP. PATIENTS AND METHODS: A total of 120 patients with DEACMP were recruited and randomly assigned into the experimental group (receiving dexamethasone 5 mg/day or 10 mg/day plus HBO therapy) and control group (HBO therapy as monotherapy)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28260863/pharmacokinetic-interactions-between-glimepiride-and-rosuvastatin-in-healthy-korean-subjects-does-the-slco1b1-or-cyp2c9-genetic-polymorphism-affect-these-drug-interactions
#18
Choon Ok Kim, Eun Sil Oh, Hohyun Kim, Min Soo Park
To improve cardiovascular outcomes, dyslipidemia in patients with diabetes needs to be treated. Thus, these patients are likely to take glimepiride and rosuvastatin concomitantly. Therefore, this study aimed to evaluate the pharmacokinetic (PK) interactions between these two drugs in healthy males and to explore the effect of SLCO1B1 and CYP2C9 polymorphisms on their interactions in two randomized, open-label crossover studies. Glimepiride was studied in part 1 and rosuvastatin in part 2. Twenty-four participants were randomly assigned to each part...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28260862/sofosbuvir-velpatasvir-regimen-promises-an-effective-pan-genotypic-hepatitis-c-virus-cure
#19
REVIEW
Fazia Mir, Alp S Kahveci, Jamal A Ibdah, Veysel Tahan
Hepatitis C virus (HCV) is a global pandemic, with nearly 200 million infected patients worldwide. HCV is the most common blood-borne infection in the US with numerous health implications including liver fibrosis, cirrhosis, and hepatocellular cancer. Traditional genotype-based HCV therapies with interferon resulted in moderate success in the sustained elimination of viral genome. Recent clinical trials of the once-daily combination tablet of sofosbuvir, a nonstructural (NS) 5B polymerase inhibitor, and velpatasvir, an NS5A inhibitor, demonstrate sustained virologic response rates of about 95%, regardless of prior treatment experience or presence of cirrhosis across all HCV genotypes...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28260861/polyphosphoester-nanoparticles-as-biodegradable-platform-for-delivery-of-multiple-drugs-and-sirna
#20
Hadeel Elzeny, Fuwu Zhang, Esraa N Ali, Heba A Fathi, Shiyi Zhang, Richen Li, Mohamed A El-Mokhtar, Mostafa A Hamad, Karen L Wooley, Mahmoud Elsabahy
Delivery of multiple therapeutics and/or diagnostic agents to diseased tissues is challenging and necessitates the development of multifunctional platforms. Among the various strategies for design of multifunctional nanocarriers, biodegradable polyphosphoester (PPE) polymers have been recently synthesized via a rapid and simple synthetic strategy. In addition, the chemical structure of the polymer could be tuned to form nanoparticles with varying surface chemistries and charges, which have shown exceptional safety and biocompatibility as compared to several commercial agents...
2017: Drug Design, Development and Therapy
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