Drugs in R&D

http://link.springer.com/journal/40268

List of Papers (Total 346)

Safety and Efficacy of 0.5% Carbomer 980 Gel for Treatment of Symptoms of Common Cold: Results of 2 Randomized Trials

BackgroundTwo studies of intranasal 0.5% carbomer 980 gel were conducted evaluating nasal tolerability in healthy volunteers and safety and efficacy in adults with common cold symptoms.MethodsStudy 1 randomly assigned healthy adults to 0.5% carbomer 980 gel (n = 20) or placebo (n = 10) administered intranasally four times daily for 7 days. Nasal examinations were conducted at...

Bortezomib for the Treatment of Hematologic Malignancies: 15 Years Later

Bortezomib is a dipeptidyl boronic acid that selectively inhibits the ubiquitin proteasome pathway, which plays a role in the degradation of many intracellular proteins. It is the first-in-class selective and reversible inhibitor of the 26S proteasome, with antiproliferative and antitumor activity. It exerts its anti-neoplastic action mainly via the inhibition of the nuclear...

Multikinase Abl/DDR/Src Inhibition Produces Optimal Effects for Tyrosine Kinase Inhibition in Neurodegeneration

Background and objectivesInhibition of Abelson (Abl) tyrosine kinase as a therapeutic target has been gaining attention in neurodegeneration. Post-mortem Alzheimer’s and Parkinson’s disease brains show that the levels of several other tyrosine kinases, including Discoidin Domain Receptors (DDR1/2) are elevated. Knockdown of these tyrosine kinases with shRNA reduces neurotoxic...

Effects of Food on the Bioavailability of Amphetamine in Healthy Adults After Administration of SHP465 Mixed Amphetamine Salts Extended-Release Capsules

Background and objectiveSHP465 mixed amphetamine salts extended release is a once-daily, single-entity, mixed amphetamine salts capsule product for attention-deficit/hyperactivity disorder. The objective of this study was to evaluate amphetamine pharmacokinetics following SHP465 mixed amphetamine salts under three administration conditions.MethodsHealthy adults (n = 16) enrolled...

Ulcerative Colitis: Shifting Sands

Ulcerative colitis (UC) is a chronic inflammatory bowel disease associated with considerable disease burden. We review some current misconceptions about UC in adults with the aim of optimizing care for patients. Although UC and Crohn’s disease (CD) are considered discrete diseases, distinctions between them are not always clear-cut and phenotypes may change over time. Patient...

S-1 in Patients with Advanced Esophagogastric Adenocarcinoma: Results from the Safety Compliance Observatory on Oral fluoroPyrimidines (SCOOP) Study

Background and ObjectivesS-1-based regimens have been shown to be as effective as other fluoropyrimidine-based regimens with a better safety profile in patients with advanced esophagogastric adenocarcinoma. However, real-world data on S-1 in European patients with advanced esophagogastric adenocarcinoma are lacking. The Safety Compliance Observatory on Oral fluoroPyrimidines...

Inhaled Loxapine for the Management of Acute Agitation in Bipolar Disorder and Schizophrenia: Expert Review and Commentary in an Era of Change

Agitation is a common and costly phenomenon associated with a number of psychiatric conditions including schizophrenia and bipolar disorder. Early identification and prompt intervention to relieve the symptoms of agitation are essential to avoid symptomatic escalation and emergence of aggressive behaviour. Recent consensus guidelines emphasise the need for non-coercive management...

Should Cytochrome P450 Inducers be Used to Accelerate Clearance of Brodifacoum from Poisoned Patients?

A recent multi-state outbreak of life-threatening bleeding following inhalation of synthetic cannabinoids has been attributed to contamination with the long-acting anticoagulant rodenticide (LAAR) brodifacoum, a second-generation, highly potent, long-acting derivative of the commonly used blood thinner warfarin. While long-term treatment with high-dose vitamin K1 restores...

Assessment of Taste and Grittiness of Riomet® ER Strawberry, Riomet® ER Grape, Riomet® Cherry, and Metformin Immediate-Release Tablets in Healthy Subjects

ObjectiveThis study was conducted to evaluate the taste and grittiness of two formulations of Riomet® ER (metformin hydrochloride for extended release [ER] oral suspension 100 mg/mL) differing only in their flavoring agents (strawberry and grape) in comparison with two commercially available immediate-release (IR) formulations of metformin, Riomet® Cherry (metformin hydrochloride...

Post-Marketing Surveillance of Silodosin in Patients with Benign Prostatic Hyperplasia and Poor Response to Existing Alpha-1 Blockers: The SPLASH Study

ObjectivesOur objective was to investigate the effectiveness and safety of silodosin in patients with benign prostatic hyperplasia (BPH) who switched to silodosin from another α1 blocker because of inadequate response.MethodsThis was a prospective observational study conducted at 715 medical facilities in Japan in patients with BPH who received an α1 blocker other than silodosin...

Suvorexant (Belsomra® Tablets 10, 15, and 20 mg): Japanese Drug-Use Results Survey

BackgroundWe report on the results of a Japanese postmarketing drug-use survey of suvorexant (Belsomra®) tablets.MethodsA survey with a ≤ 6-month observation period after the start of administration was conducted, targeting insomnia patients who were treated with suvorexant for the first time in Japan. Information on the safety and efficacy of the drug product was collected. The...

Two Glucose-Lowering Mechanisms of Canagliflozin Depending on Body Weight Changes in Drug-Naïve Subjects with Type 2 Diabetes

ObjectivesThe aim of this study was to investigate the relations between the changes in body weight and those of glycemic and non-glycemic parameters in drug-naïve subjects with type 2 diabetes mellitus (T2DM) treated with canagliflozin monotherapy.MethodsSubjects received 50–100 mg/day canagliflozin monotherapy for 3 months (n = 36), and were then divided into two groups: (1...

Isavuconazole Kinetic Exploration for Clinical Practice

BackgroundIsavuconazole is a new antifungal prodrug for the treatment of invasive aspergillosis and mucormycosis. As no clear pharmacokinetic-pharmacodynamic relationship has been established for patients, therapeutic drug monitoring is not currently required. However, as isavuconazole is a new drug, clinicians are sometimes sceptical about the exposure achieved in their patients...

Rivaroxaban versus Warfarin in Patients with Mechanical Heart Valve: Rationale and Design of the RIWA Study

IntroductionMechanical heart valves (MHV) are extremely durable, but they require permanent use of anticoagulation to prevent thromboembolic events. The only approved therapeutic options are vitamin K antagonists (VKAs), such as warfarin. As a drug class, clinical management is difficult, therefore new alternatives need to be evaluated.MethodsRIWA is a phase II/III, prospective...

Treatment of Disfiguring Cutaneous Lesions in Neurofibromatosis-1 with Everolimus: A Phase II, Open-Label, Single-Arm Trial

BackgroundCutaneous neurofibromas cause disfigurement and discomfort in individuals with neurofibromatosis type 1 (NF-1).MethodsThe primary objective of this phase II, open-label, single-arm trial was to assess whether orally administered everolimus reduced the surface volume of cutaneous neurofibromas in patients with NF-1.ResultsOf 22 patients who took the study drug, 17...

Critical Review of the Use of Second-Generation Antipsychotics in Obsessive–Compulsive and Related Disorders

Currently, all second-generation antipsychotics are approved for schizophrenia. Many are also approved for bipolar disorder, with some also approved as adjunctive treatment for depression and autism-related irritability. Second-generation antipsychotics are increasingly being prescribed for indications other than those approved by the Food and Drug Administration, such as in...

Risks and Benefits of Sodium Polystyrene Sulfonate for Hyperkalemia in Patients on Maintenance Hemodialysis

BackgroundConcerns about sodium overload when using sodium polystyrene sulfonate (Na-resin) as an ion-exchange resin for the treatment of hyperkalemia led our institution to gradually shift to the use of calcium polystyrene sulfonate (Ca-resin). However, as serum potassium levels were insufficiently controlled and patients experienced constipation, we returned to using Na-resin...

The Effectiveness of Intravenous Golimumab Administered Directly After Infliximab in Rheumatoid Arthritis Patients

PurposeFor patients with rheumatoid arthritis (RA) who do not respond or lose response to anti-tumor necrosis factor (TNF) biologics, switching to a different anti-TNF can be an effective means to manage symptoms and disease progression. This study examined the utilization and effectiveness of intravenous golimumab within a real-world population of patients with RA switching...

Population Pharmacokinetic Modelling of Ceftazidime and Avibactam in the Plasma and Epithelial Lining Fluid of Healthy Volunteers

ObjectivesOur objective was to develop population pharmacokinetic (PK) models for ceftazidime and avibactam in the plasma and epithelial lining fluid (ELF) of healthy volunteers and to compare ELF concentrations to plasma PK/pharmacodynamic (PD) targets.MethodsPlasma and ELF population PK models were developed for ceftazidime and avibactam concentration data from 42 subjects...

Evaluation of Cardiovascular Disease Risk in HIV-1–Infected Patients Treated with Darunavir

IntroductionWe evaluated cardiovascular disease (CVD) risk associated with darunavir treatment and examined the demographic/clinical characteristics of darunavir users based on data from Janssen-sponsored clinical trials, post-marketing pharmacovigilance databases, and administrative claims databases.MethodsFirst, selected CVD events [myocardial infarction, stroke, sudden death...

Octreotide Use in Neonates: A Case Series

Background and ObjectiveOctreotide is a somatostatin analogue and has been used off-label for a variety of conditions. There are no specific guidelines for the use of octreotide in neonates and its safety and efficacy have not been systematically evaluated. The objective of this study is to present our experience of using octreotide therapy in neonates.MethodsThis is a...

Pharmacokinetics of the Oral Selective CXCR2 Antagonist AZD5069: A Summary of Eight Phase I Studies in Healthy Volunteers

ObjectiveThe aim of this study was to summarise the pharmacokinetic findings from eight phase I studies in healthy volunteers given oral AZD5069, a selective small-molecule CXCR2 antagonist.Methods240 healthy volunteers across eight phase I studies received single (0.1–200 mg) or multiple once- or twice-daily (10–120 mg) oral AZD5069 as solution, suspension, capsules or tablets...