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https://www.readbyqxmd.com/read/28544992/pharmacokinetics-pharmacodynamics-and-tolerability-of-usl261-midazolam-nasal-spray-randomized-study-in-healthy-geriatric-and-non-geriatric-adults
#1
Alexander K Berg, Michael J Myrvik, Peter J Van Ess
AIM: Characterize pharmacokinetics, pharmacodynamics, and safety/tolerability of USL261 in geriatric adults to inform its potential for treating bouts of increased seizure activity. METHODS: Phase 1, randomized, double-blind, 2-way crossover study in healthy geriatric (≥65years; n=18) and non-geriatric (18-40years; n=12) adults evaluated single USL261 doses (2.5 and 5.0mg) administered intranasally. Pharmacokinetic parameters were estimated for midazolam and 1-hydroxymidazolam (active metabolite), including area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax), time to Cmax (Tmax), and half-life (t1/2)...
May 22, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28544814/optimization-of-liposomal-topotecan-for-use-in-treating-neuroblastoma
#2
Lina Chernov, Rebecca J Deyell, Malathi Anantha, Nancy Dos Santos, Roger Gilabert-Oriol, Marcel B Bally
The purpose of this work was to develop an optimized liposomal formulation of topotecan for use in the treatment of patients with neuroblastoma. Drug exposure time studies were used to determine that topotecan (Hycamtin) exhibited great cytotoxic activity against SK-N-SH, IMR-32 and LAN-1 neuroblastoma human cell lines. Sphingomyelin (SM)/cholesterol (Chol) and 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC)/Chol liposomes were prepared using extrusion methods and then loaded with topotecan by pH gradient and copper-drug complexation...
May 23, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28544589/methionine-tumor-starvation-by-erythrocyte-encapsulated-methionine-gamma-lyase-activity-controlled-with-per-os-vitamin-b6
#3
Fabien Gay, Karine Aguera, Karine Sénéchal, Angie Tainturier, Willy Berlier, Delphine Maucort-Boulch, Jérôme Honnorat, Françoise Horand, Yann Godfrin, Vanessa Bourgeaux
Erymet is a new therapy resulting from the encapsulation of a methionine gamma-lyase (MGL; EC number 4.4.1.11) in red blood cells (RBC). The aim of this study was to evaluate erymet potential efficacy in methionine (Met)-dependent cancers. We produced a highly purified MGL using a cGMP process, determined the pharmacokinetics/pharmacodynamics (PK/PD) properties of erymet in mice, and assessed its efficacy on tumor growth prevention. Cytotoxicity of purified MGL was tested in six cancer cell lines. CD1 mice were injected with single erymet product supplemented or not with vitamin B6 vitamer pyridoxine (PN; a precursor of PLP cofactor)...
May 23, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28544581/a-comparison-of-the-pharmacokinetics-of-methylphenidate-extended-release-orally-disintegrating-tablets-with-a-reference-extended-release-formulation-of-methylphenidate-in-healthy-adults
#4
Ann Childress, Jeffrey G Stark, Russ McMahen, Dorothy Engelking, Carolyn Sikes
Extended-release (ER) methylphenidate (MPH) is a first-line treatment for attention-deficit/hyperactivity disorder. A methylphenidate extended-release orally disintegrating tablet (MPH XR-ODT) has recently been developed. This was a randomized, open-label, 3-period, 3-treatment study comparing the bioavailability and absorption of 2 MPH XR-ODT formulations with an MPH ER reference medication. Here we report the 2 treatments comparing the commercial MPH XR-ODT formulation and reference medication. Following a ≥10-hour fast, 42 healthy adults received 60 mg of reference medication or MPH XR-ODT (2 × 30 mg)...
May 25, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28544344/fed-and-fasted-administration-of-a-novel-extended-release-methylphenidate-orally-disintegrating-tablet-formulation-for-the-treatment-of-adhd
#5
Richard H Weisler, Jeffrey G Stark, Carolyn Sikes
Extended-release methylphenidate is a first-line treatment for attention-deficit/hyperactivity disorder. A methylphenidate extended-release orally disintegrating tablet (MPH XR-ODT) has recently been developed. Here we report an open-label, randomized, 2-period, 2-treatment crossover study to determine the effect of food on the bioavailability of a single 60-mg dose of MPH XR-ODT in healthy adults. Blood samples were collected predose through 36 hours postdose. Maximum plasma concentration (Cmax ), time to maximum plasma concentration (Tmax ), terminal elimination half-life (T1/2 ), overall systemic exposure (AUClast and AUCinf ), and partial areas under the concentration curve (AUC0-3 , AUC3-7 , and AUC7-12 ) were calculated...
May 25, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28544263/impact-of-a-product-specific-reference-standard-for-the-measurement-of-a-pegylated-rfviii-activity-the-swiss-multicentre-field-study
#6
O Bulla, A Poncet, L Alberio, L M Asmis, A Gähler, L Graf, M Nagler, J-D Studt, D A Tsakiris, P Fontana
INTRODUCTION: Measuring factor VIII (FVIII) activity can be challenging when it has been modified, such as when FVIII is pegylated to increase its circulating half-life. Use of a product-specific reference standard may help avoid this issue. AIM: Evaluate the impact of using a product-specific reference standard for measuring the FVIII activity of BAX 855 - a pegylated FVIII - in eight of Switzerland's main laboratories. METHODS: Factor VIII-deficient plasma, spiked with five different concentrations of BAX 855, plus a control FVIII sample, was sent to the participating laboratories...
May 24, 2017: Haemophilia: the Official Journal of the World Federation of Hemophilia
https://www.readbyqxmd.com/read/28544109/express-with-caution-epitope-tags-and-cdna-variants-effects-on-herg-channel-trafficking-half-life-and-function
#7
Marika L Osterbur Badhey, Alexander C Bertalovitz, Thomas V McDonald
INTRODUCTION: Genetic mutations in KCNQ2 which encodes hERG, the alpha subunit of the potassium channel responsible for the IKr current, cause Long QT Syndrome, an inherited cardiac arrhythmia disorder. Electrophysiology techniques are used to correlate genotype with molecular phenotype to determine which mutations identified in patients diagnosed Long QT Syndrome are disease causing, and which are benign. These investigations are usually done using heterologous expression in cell lines, and often, epitope fusion tags are used to enable isolation and identification of the protein of interest...
May 24, 2017: Journal of Cardiovascular Electrophysiology
https://www.readbyqxmd.com/read/28544031/ubiquitin-specific-protease-8-is-a-novel-prognostic-marker-in-early-stage-lung-adenocarcinoma
#8
Yunjung Kim, Aya Shiba-Ishii, Tomoki Nakagawa, Ryan Edbert Husni, Shingo Sakashita, Tomoyo Takeuchi, Masayuki Noguchi
Alterations of epidermal growth factor receptor (EGFR) expression frequently occur in early-stage lung adenocarcinoma. Ubiquitin-specific protease 8 (USP8) has been reported to stabilize EGFR protein at the plasma membrane through the recycling pathway. Here, we examined the correlation between USP8 expression and the expression or mutation status of EGFR, as well as the clinicopathological features of lung adenocarcinoma and patient outcome. Expression of EGFR and USP8 in surgically resected specimens of lung adenocarcinoma (82 cases) was examined by immunohistochemistry...
May 19, 2017: Pathology International
https://www.readbyqxmd.com/read/28543773/degradation-of-heme-oxygenase-1-by-the-immunoproteasome-in-astrocytes-a-potential-interferon-%C3%AE-dependent-mechanism-contributing-to-hiv-neuropathogenesis
#9
Colleen E Kovacsics, Alexander J Gill, Surendra S Ambegaokar, Benjamin B Gelman, Dennis L Kolson
Induction of the detoxifying enzyme heme oxygenase-1 (HO-1) is a critical protective host response to cellular injury associated with inflammation and oxidative stress. We previously found that HO-1 protein expression is reduced in brains of HIV-infected individuals with HIV-associated neurocognitive disorders (HAND) and in HIV-infected macrophages, where this reduction associates with enhanced glutamate release and neurotoxicity. Because HIV-infected macrophages are a small component of the cellular content of the brain, the reduction of macrophage HO-1 expression likely accounts for a small portion of brain HO-1 loss in HIV infection...
May 22, 2017: Glia
https://www.readbyqxmd.com/read/28543707/viable-bacteria-persist-on-antibiotic-spacers-following-two-stage-revision-for-periprosthetic-joint-infection
#10
Dongzhu Ma, Robert M Q Shanks, Charles M Davis, David W Craft, Thomas K Wood, Brian R Hamlin, Kenneth L Urish
Treatment in periprosthetic joint infection (PJI) remains challenging. The failure rate of two-stage revision and irrigation and debridement with component retention in PJI suggests that biofilm cells have a high tolerance to antibiotic chemotherapy. Previous work has demonstrated that biofilm cells have high antibiotic tolerance in vitro, but there is little clinical evidence to support these observations. The aim of this study was to determine if retrieved antibiotic spacers from two-stage revision total knee arthroplasty for PJI have evidence of remaining viable bacteria...
May 19, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28543367/successful-treatment-of-methicillin-susceptible-staphylococcus-aureus-osteomyelitis-with-oritavancin
#11
Dino J Delaportas, Sandy J Estrada, Matthew Darmelio
Staphylococcus aureus remains the most common causative pathogen in osteomyelitis. New or alternate therapies are often needed to adequately treat S. aureus infections in patients with drug allergies, treatment failures, or drug interactions. Oritavancin is a novel long-acting lipoglycopeptide approved by the Food and Drug Administration (FDA) in 2014 for the treatment of Acute Bacterial Skin and Skin Structure Infections (ABSSSI). With a terminal half-life of 8 to 10 days, oritavancin dosing regimens with infrequent parenteral administration now exist to treat infectious diseases such as osteomyelitis that would otherwise require daily dosing of intravenous antimicrobials for weeks; however clinical experience is lacking...
May 23, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28542406/human-igg3-with-extended-half-life-does-not-improve-fc-gamma-receptor-mediated-cancer-antibody-therapies-in-mice
#12
Rens Braster, Simran Grewal, Remco Visser, Helga K Einarsdottir, Marjolein van Egmond, Gestur Vidarsson, Marijn Bögels
BACKGROUND: Current anti-cancer therapeutic antibodies that are used in the clinic are predominantly humanized or fully human immunoglobulin G1 (IgG1). These antibodies bind with high affinity to the target antigen and are efficient in activating the immune system via IgG Fc receptors and/or complement. In addition to IgG1, three more isotypes are present in humans, of which IgG3 has been found to be superior compared to human IgG1 in inducing antibody dependent cell cytotoxicity (ADCC), phagocytosis or activation of complement in some models...
2017: PloS One
https://www.readbyqxmd.com/read/28541524/metal-bound-clamp-tag-inhibits-proteolytic-cleavage
#13
Michaela L McNiff, Jennifer S Chadwick
Biologics can be an improvement to small molecule drugs, providing high specificity for an identified target, lowering toxicity and limiting side effects. To achieve effective delivery, the biologic must have sufficient time to reach the target tissue. A prolonged half-life in the circulating environment is desired, but often serum stability is limited by proteases. Proteolysis in the serum causes degradation and inactivation as the biologic is fragmented and more rapidly cleared from the body. To improve the circulating half-life, large, hydrophilic polymers may be conjugated or stable fusion tags may be engineered to increase the effective size of the peptide and to hinder degradation by proteases...
May 25, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/28541147/pharmacokinetics-of-cefazolin-for-prophylactic-administration-to-dogs
#14
Omar J Gonzalez, Walter C Renberg, James K Roush, Butch KuKanich, Matt Warner
OBJECTIVE To evaluate pharmacokinetics of cefazolin after IV injection of cefazolin (22 mg/kg) and after simultaneous IV and IM injections of cefazolin (total dose, 44 mg/kg) to dogs. ANIMALS 12 adult Beagles. PROCEDURES Dogs (6/group) were assigned to receive a single injection of cefazolin (IV group; 22 mg/kg, IV) or simultaneous injections (IV + IM group; 22 mg/kg, IV, and 22 mg/kg, IM). Interstitial fluid was collected over a 5-hour period by use of ultrafiltration probes for pharmacokinetic analysis. RESULTS Mean cefazolin concentration in the interstitial fluid at 1, 1...
June 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28541145/pharmacokinetics-of-butorphanol-tartrate-in-a-long-acting-poloxamer-407-gel-formulation-administered-to-hispaniolan-amazon-parrots-amazona-ventralis
#15
Delphine Laniesse, David Sanchez-Migallon Guzman, Heather K Knych, Dale A Smith, Cornelia Mosley, Joanne R Paul-Murphy, Hugues Beaufrère
OBJECTIVE To determine pharmacokinetics of butorphanol tartrate incorporated into poloxamer 407 (P407) after SC administration to Hispaniolan Amazon parrots (Amazona ventralis). ANIMALS 11 adult Hispaniolan Amazon parrots (6 males and 5 females; 11 to 27 years old). PROCEDURES A sterile formulation of butorphanol in P407 (But-P407) 25% (percentage determined as [weight of P407/weight of diluent] × 100]) was created (8.3 mg/mL). Five preliminary experiments (2 birds/experiment) were performed to determine the ideal dose for this species...
June 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28540472/modelling-malpighian-tubule-crystals-within-the-predatory-soil-mite-pergamasus-longicornis-mesostigmata-parasitidae
#16
Clive E Bowman
The occurrence of refractive crystals (aka guanine) is characterised in the Malpighian tubules of the free-living predatory parasitiform soil mite Pergamasus longicornis (Berlese) from a temporal series of histological sections during and after feeding on larval dipteran prey. The tubular system behaves as a single uniform entity during digestion. Malpighian mechanisms are not the 'concentrative' mechanism sought for the early stasis in gut size during the second later phase of prey feeding. Nor are Malpighian changes associated with the time of 'anal dabbing' during feeding...
May 24, 2017: Experimental & Applied Acarology
https://www.readbyqxmd.com/read/28539836/dual-delivery-of-ngf-and-bfgf-coacervater-ameliorates-diabetic-peripheral-neuropathy-via-inhibiting-schwann-cells-apoptosis
#17
Rui Li, Jianfeng Ma, Yanqing Wu, Matthew Nangle, Shuang Zou, Yiyang Li, Jiayu Yin, Yingzheng Zhao, Helin Xu, Hongyu Zhang, Xiaokun Li, Qing Song Ye, Jian Wang, Jian Xiao
Diabetic neuropathy is a kind of insidious complications that impairs neural and vascular function and ultimately leads to somatic and visceral denervation. Basic fibroblast growth factor (bFGF) and nerve growth factor (NGF) are important neurotrophic factors for stimulating angiogenesis and improving peripheral nerve function. Administrating a single factor has good therapeutic effect on diabetic peripheral neuropathy (DPN). However, the short half-life and rapid diffusion of growth factors under physiological conditions limits its clinical applications...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/28539253/documenting-the-kinetic-time-course-of-lambda-cyhalothrin-metabolites-in-orally-exposed-volunteers-for-the-interpretation-of-biomonitoring-data
#18
Rania Khemiri, Jonathan Côté, Hamadi Fetoui, Michèle Bouchard
Lambda-cyhalothrin is a pyrethroid pesticide largely used in agriculture. Exposure assessment can be performed by measuring key urinary metabolites. For a proper use of biomonitoring data, it is however important to gain information on the toxicokinetics of these key biomarkers of exposure. A human volunteer study was performed to document the plasma and urinary time courses of major lambda-cyhalothrin metabolites. Seven volunteers ingested 0.025mgkg(-1) body weight of lambda-cyhalothrin. Blood samples were withdrawn prior to dosing and at fixed time periods over the 72 h-period following ingestion and complete urine voids were collected pre-exposure and at pre-established intervals over 84h post-dosing...
May 21, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28538700/stability-profiles-and-therapeutic-effect-of-cu-zn-superoxide-dismutase-chemically-coupled-to-o-quaternary-chitosan-derivatives-against-dextran-sodium-sulfate-induced-colitis
#19
Nan Zhao, Zhaolong Feng, Meng Shao, Jichao Cao, Fengshan Wang, Chunhui Liu
Superoxide dismutase (SOD) has attracted considerable attention on treatment of reactive oxygen species (ROS)-related disorders. We previously conjugated Cu/Zn SOD to O-quaternary chitosan derivatives (O-HTCC) to yield a polymer-enzyme conjugate O-HTCC-SOD that demonstrated superior therapeutic effect to native SOD. The present study demonstrated that O-HTCC-SOD had wider pH activity range, better thermal stability, excellent long-term stability for storage, as well as unique reinstatement of activity exposure to proteolytic degradation that was helpful for longer half-life in vivo...
May 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28538080/formulation-and-characterization-of-lutetium-177-labeled-stannous-tin-colloid-for-radiosynovectomy
#20
Geetanjali Arora, Manoranjan Singh, Pragati Jha, Sarthak Tripathy, Chandrasekhar Bal, Anirban Mukherjee, Shamim A Shamim
OBJECTIVE: Easy large-scale production, easy availability, cost-effectiveness, long half-life, and favorable radiation characteristics have made lutetium-177 (Lu) a preferred radionuclide for use in therapy. Lutetium-177-labeled stannous (Lu-Sn) colloid particles were formulated for application in radiosynovectomy, followed by in-vitro and in-vivo characterization. METHODS: Stannous chloride (SnCl2) solution and Lu were heated together, the pH was adjusted, and the particles were recovered by centrifugation...
May 19, 2017: Nuclear Medicine Communications
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