Drugs of today
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Macitentan is a novel, dual endothelin receptor antagonist recently approved for the treatment of WHO Group I pulmonary arterial hypertension. Its pharmacologic mechanism of action as well as the pharmacokinetics, pharmacodynamics and potential drug-drug interactions have been demonstrated in multiple phase I and II trials. ⋯ The most common adverse events were rarely clinically significant, nor did they result in a high rate of discontinuation. Of note, macitentan is contraindicated in pregnant women due to embryo-fetal toxicity.
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The annual congress of the European Association of Urology in Stockholm was packed with mixed poster/oral sessions wherein innovative clinical and preclinical research aimed at improving the care of patients with urinary tract diseases was reported and open for discussion. Not everything that was reported during the meeting can be captured in a single report, but the following text will guide readers through the most significant new findings directly related with pharmacotherapy for overactive bladder, urinary tract cancer and other common medical conditions that endanger the quality of life and life expectancy of many patients worldwide.
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The causes of inflammatory bowel diseases, such as ulcerative colitis (UC) and Crohn's disease (CD), remain to be elucidated. However, characteristic inflammation of the gastrointestinal mucosa is caused by infiltration of T lymphocytes into the submucosal layer. Inhibiting this immune response is a promising therapeutic target. ⋯ Regulatory applications are under review in the U. S. and E. U. for its use in the treatment of patients with UC and CD, with decisions expected in mid-2014.
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Ibrutinib is a novel oral tyrosine kinase inhibitor that irreversibly binds and inhibits tyrosine-protein kinase BTK (Bruton tyrosine kinase). BTK has been found to be important in the function of B-cell receptor signaling and therefore in the maintenance and expansion of various B-cell malignancies including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). Targeting BTK with ibrutinib has been found to be an effective strategy in treating these malignancies. ⋯ S. Food and Drug Administration granted accelerated approval for ibrutinib in November 2013 for patients with MCL who had received at least one prior therapy and in February 2014 for patients with CLL who had received at least one prior therapy. This review will discuss the preclinical pharmacology, pharmacokinetics and clinical efficacy to date of ibrutinib in the treatment of CLL and MCL.
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Pulmonary hypertension (PH) is a progressive disease that is accompanied by a poor prognosis. Pulmonary vasoconstriction is facilitated through multiple pathways and results in increased pulmonary vascular pressure leading to cell proliferation, vascular remodeling, right ventricular hypertrophy/failure, and ultimately death. ⋯ Preclinical studies have demonstrated safety and efficacy with significant clinical trials supporting its advancement into phase IV trials. Although long-term safety and efficacy and place in therapy remain to be established, riociguat presents as an exciting new option for the treatment of PH and potentially has additional indications in the near future.