Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/9009
Title: Early toxicity screening and selection of lead compounds for parasitic diseases
Authors: Nogueira, Renata Campos
Costa, José Fernando Oliveira
Sá, Matheus Santos de
Santos, Ricardo Ribeiro dos
Soares, Milena Botelho Pereira
Affilliation: Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, Brasil
Abstract: Despite 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.
Keywords: Toxicity screening
Lead compound
Parasitic diseases
Drug discovery
DeCS: Antiparasitários/toxicidade
Desenho de Drogas
Doenças Parasitárias/quimioterapia
Animais
Antiparasitários/farmacocinética
Antiparasitários/farmacologia
Avaliação Pré-Clínica de Medicamentos
Interações de Medicamentos
Hepatócitos/efeitos de drogas
Hepatócitos/metabolismo
Humanos
Testes de Toxicidade
Issue Date: 2009
Publisher: Bentham Science Publishers Ltd
Citation: NOGUEIRA, 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.
ISSN: 1873-5592
Copyright: open access
Appears in Collections:BA - IGM - Artigos de Periódicos

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