Download Antiviral Drugs: From Basic Discovery Through Clinical by Wieslaw M. Kazmierski PDF

By Wieslaw M. Kazmierski

This booklet makes a speciality of new small molecule ways to strive against viral infections. The chapters describe the invention and improvement from bench in the course of the health facility of particularly recently-approved antiviral medicines and compounds in complex medical improvement. equipped via a deadly disease (such as HIV, HCV, RSV, influenza, HBV and CMV) and written by means of best educational and commercial professionals within the box, the booklet presents a different chance to review, comprehend and practice discovery and improvement ideas and studying with no the necessity for someone to investigate, study and synthesize all big sourcing references.  issues exhibit demanding situations and suggestions of matters encountered, offering tremendous event gathered over decades of analysis that would be really worthwhile to simple and bench scientists in addition to clinicians as they proceed studying and constructing new medicinal drugs and cures.

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Extra resources for Antiviral Drugs: From Basic Discovery Through Clinical Trials

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5 (F) times the human exposure with 300 mg/day atazanavir with ritonavir. 9 times the human exposure with 300 mg/day atazanavir with ritonavir, or 400 mg/day atazanavir dose, respectively. In the embryo–fetal development studies, atazanavir produced no adverse embryonic or fetal effects at maternally toxic doses (up to 1920 mg/kg per day in rats and 60 mg/kg per day in rabbits). 0 times the human exposure at 300 mg/day atazanavir with ritonavir or 400 mg/day atazanavir, respectively. In a study of pre- and postnatal development in rats exposed to atazanavir (50, 220, and 1000 mg/kg per day), findings were limited to mean body weight gain suppression in the F1 generation from 4 days of age through the early postweaning growth period at the maternally toxic dose of 1000 mg/kg per day.

In summary, atazanavir demonstrated no selective developmental toxicity and no effects on reproductive function or fertility at exposures generally equivalent to that in humans at the recommended daily dose of atazanavir or ritonavir. Genetic Toxicity The genotoxic potential of atazanavir was evaluated in a battery of in vitro and in vivo test systems. All in vitro assays were conducted with and without metabolic activation (rat liver S9 fraction). Atazanavir was not mutagenic in either the bacterial mutagenicity screening assay or in the definitive Ames reverse-mutation study.

Diarrhea was two to three times more common in the nelfinavir group (61% of subjects) than in the atazanavir groups (23 to 30% of subjects), and jaundice occurred only in atazanavir-treated subjects (6, 6, and 12% in the 200-, 400-, and 500-mg groups, respectively). There was minimal effect on blood lipids parameters at all atazanavir doses, in contrast to the nelfinavir arm, which experienced an increase from baseline in total cholesterol, triglycerides, and fasting low-density lipoprotein (LDL) cholesterol levels.

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