Early toxicity screening and selection of lead compounds for parasitic diseases

dc.creatorNogueira, Renata Campos
dc.creatorCosta, José Fernando Oliveira
dc.creatorSá, Matheus Santos de
dc.creatorSantos, Ricardo Ribeiro dos
dc.creatorSoares, Milena Botelho Pereira
dc.date2014-11-28T18:21:24Z
dc.date2014-11-28T18:21:24Z
dc.date2009
dc.date.accessioned2023-09-26T20:46:38Z
dc.date.available2023-09-26T20:46:38Z
dc.identifierNOGUEIRA, R. C. et al. Early toxicity screening and selection of lead compounds for parasitic diseases. Current Drug Targets, v. 10, n. 3, p. 291-298, 2009.
dc.identifier1873-5592
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/9009
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8863683
dc.descriptionDespite many advances made in disease mechanisms knowledge and drug discovery and development processes, the election of promising lead compounds continues to be a challenge. Efficient techniques are required for lead selection of hit compounds selected through in vitro pharmacological studies, in order to generate precise low cost throughput data with minimal amount of compound to support the right decision making. In this context, the selection of lead compounds with physicochemical parameters that will benefit orally bioavailable drugs are crucial for patients compliance and cost effectiveness, as well as for successful pharmacology. A concept based in Lipinski’s rules point out the importance of analyzing these informations in early stages. A hepatocyte screening system may provide data on many processes such as drug-drug interaction, metabolite formation, drug toxicity and ADME profile of a hit. Drug-induced liver injury is the most frequent reason for the withdrawal of an approved drug from the market and hepatocytes have a central role in the metabolism of xenobiotics. Cytotoxicity screening assays can also give some information about toxicity early drug discovery process. A set of goals in lead compound selection must be shared between all areas involved so the chances of success can be improved in translational research.
dc.formatapplication/pdf
dc.languageeng
dc.publisherBentham Science Publishers Ltd
dc.rightsopen access
dc.subjectToxicity screening
dc.subjectLead compound
dc.subjectParasitic diseases
dc.subjectDrug discovery
dc.subjectAntiparasitários/toxicidade
dc.subjectDesenho de Drogas
dc.subjectDoenças Parasitárias/quimioterapia
dc.subjectAnimais
dc.subjectAntiparasitários/farmacocinética
dc.subjectAntiparasitários/farmacologia
dc.subjectAvaliação Pré-Clínica de Medicamentos
dc.subjectInterações de Medicamentos
dc.subjectHepatócitos/efeitos de drogas
dc.subjectHepatócitos/metabolismo
dc.subjectHumanos
dc.subjectTestes de Toxicidade
dc.titleEarly toxicity screening and selection of lead compounds for parasitic diseases
dc.typeArticle


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