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Id: biblio-1014244
Autor: Cabrera C, María Elena; Puga L, Bárbara; Torres, Vivianne; Salinas, Mauricio.
Título: Evaluación del tratamiento de linfoma de Hodgkin con esquema ABVD en Chile / Treatment of Hodgkin lymphoma: analysis of 915 patients
Fonte: Rev. méd. Chile;147(4):437-443, abr. 2019. tab, graf.
Idioma: es.
Resumo: Background: Hodgkin lymphoma has a high rate of curability, even in advanced stages. Aim: To assess the results of Hodgkin lymphoma treatment using the ABVD (doxorubicin, bleomycin, vinblastine, dacarbazine) chemotherapy regimen. Material and Methods: Analysis of a database held by the Chilean Ministry of Health, including all patients treated at accredited cancer treatment centers. Results: Data for 915 patients, median age 35 years (range 15-86 years) and followed for a median of 97 months (range 1-347 months) were analyzed. Forty-one percent had localized disease. Overall survival at five years for localized and advanced stages was 92% and 74%, respectively. The figures for progression free survival were 87% and 64%, respectively. Patients with relapse who received autologous stem cell transplantation (ASCT) had a five year overall survival of 92%, compared to 64% among those who did not undergo this procedure (p < 0.01). The Guarantees in Health Program set up by the Ministry of Health, was associated with earlier stage disease at diagnosis. Conclusions: The ABVD regimen achieves high rates of cure in localized stages of the disease but the results in advanced stages are not optimal. ASCT significantly improves survival in patients with relapse. The Guarantees in Health Program is associated with earlier diagnosis of the disease.
Descritores: Doença de Hodgkin/tratamento farmacológico
Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico
-Fatores de Tempo
Vimblastina/uso terapêutico
Bleomicina/uso terapêutico
Doença de Hodgkin/mortalidade
Doença de Hodgkin/patologia
Doxorrubicina/uso terapêutico
Chile
Resultado do Tratamento
Transplante de Células-Tronco Hematopoéticas/métodos
Intervalo Livre de Doença
Dacarbazina/uso terapêutico
Estimativa de Kaplan-Meier
Limites: Humanos
Masculino
Feminino
Adolescente
Adulto
Pessoa de Meia-Idade
Idoso
Idoso de 80 Anos ou mais
Adulto Jovem
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-1146685
Autor: Luna, Amalia; Molinari, Leisa; Ferrario, Damián; Galimberti, Gastón; Kowalczuk, Alicia.
Título: Nuevas posibilidades terapéuticas en melanoma metastásico / Novel therapeutics possibilities for metastatic melanoma
Fonte: Rev. Hosp. Ital. B. Aires (2004);36(3):84-90, sept. 2016. ilus.
Idioma: es.
Resumo: El melanoma ha experimentado un aumento constante en su tasa de incidencia en las últimas cinco décadas a nivel mundial. El pronóstico del paciente con melanoma se relaciona con el estadio de la enfermedad al momento del diagnóstico, con una sobrevida global media de 6,2 meses en pacientes con melanoma metastásico. El avance en las investigaciones sobre la biología y el comportamiento tumoral permitió el desarrollo de nuevas terapias con distintos mecanismos de acción y mayor eficacia. En esta revisión se abordan las terapias biológicas en melanoma metastásico, su mecanismo de acción y principales resultados en ensayos clínicos. (AU)

Melanoma has experienced a consistent increase in incidence over the past five decades worldwide. The prognosis of patients with melanoma is related to the stage of disease at diagnosis, with a median overall survival of 6.2 months in metastatic melanoma. Progress in research on tumor biology allowed the development of new therapies with different mechanisms of action and greater efficiency. In this review, biologic therapies in metastatic melanoma, its mechanism of action and main results in clinical trials are discussed. (AU)
Descritores: Terapia Biológica
Melanoma/terapia
Metástase Neoplásica/terapia
-Incidência
Proteína Quinase 1 Ativada por Mitógeno/antagonistas & inibidores
Dacarbazina/efeitos adversos
Dacarbazina/uso terapêutico
Inibidores de Proteínas Quinases/efeitos adversos
Inibidores de Proteínas Quinases/uso terapêutico
Ipilimumab/efeitos adversos
Ipilimumab/uso terapêutico
Antineoplásicos Imunológicos/efeitos adversos
Antineoplásicos Imunológicos/uso terapêutico
Vemurafenib/efeitos adversos
Vemurafenib/uso terapêutico
Nivolumabe/efeitos adversos
Nivolumabe/uso terapêutico
Imunoterapia
Limites: Humanos
Tipo de Publ: Revisão
Responsável: AR2.1 - Biblioteca Central


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Id: biblio-1012074
Autor: Corrêa, Flávia de Miranda; Guerra, Renata Leborato; Fernandes, Ricardo Ribeiro Alves; Souza, Mirian Carvalho de; Zimmermann, Ivan Ricardo.
Título: Terapia-alvo versus dacarbazina no tratamento de primeira linha do melanoma avançado não cirúrgico e metastático: análise de impacto orçamentário na perspectiva do Sistema Único de Saúde, 2018-2020 / Terapia dirigida versus dacarbazina en el tratamiento de primera línea del melanoma avanzado no quirúrgico y metastásico: análisis de impacto presupuestario en la perspectiva del Sistema Nacional de Salud de Brasil, 2018-2020 / Target therapy versus dacarbazine in first-line treatment of advanced non-surgical and metastatic melanoma: budget impact analysis from the perspective of the Brazilian National Health System, 2018-2020
Fonte: Epidemiol. serv. saúde;28(2):e2018325, 2019. tab, graf.
Idioma: en; pt.
Resumo: Objetivo: estimar o impacto orçamentário incremental da terapia-alvo para tratamento de primeira linha do melanoma avançado não cirúrgico e metastático, em comparação à dacarbazina. Métodos: análise de impacto orçamentário na perspectiva do Sistema Único de Saúde (SUS) do Brasil; a partir de dados demográficos e estimativas da incidência, foi delimitada a população no horizonte temporal de três anos (2018-2020) e estimados os custos diretos médicos; foi considerado cenário de referência o tratamento com dacarbazina, e como cenários alternativos a terapia-alvo com vemurafenibe, dabrafenibe, vemurafenibe + cobimetinibe e dabrafenibe + trametinibe; a avaliação das incertezas foi conduzida mediante análise por cenários. Resultados: o impacto orçamentário incremental variou de R$ 451.867.881,00 a R$ 768.860.968,00, representando 0,70 a 1,53% dos gastos anuais totais com medicamentos ambulatoriais no SUS; no melhor e no pior cenário, os resultados variaram de R$ 289.160.835,00 a R$ 1.107.081.926,00. Conclusão: a terapia-alvo, comparada à dacarbazina, implica impacto excessivo no orçamento, desfavorecendo eventual incorporação.

Objetivo: estimar el impacto presupuestario incremental de la terapia dirigida para tratamiento de primera línea del melanoma avanzado no quirúrgico y metastásico comparado con la dacarbazina. Métodos: análisis de impacto presupuestario, en la perspectiva del Sistema Único de Salud (SUS) de Brasil; a partir de datos demográficos y estimaciones de incidencia se delimitó la población en un horizonte temporal de tres años (2018-2020) y se estimaron los costos directos médicos. El escenario de referencia fue el tratamiento con dacarbazina y los escenarios alternativos la terapia dirigida con vemurafenib, dabrafenib, vemurafenib + cobimetinib y dabrafenib + trametinib; la evaluación de incertidumbre se llevó a cabo mediante análisis por escenarios. Resultados: el impacto presupuestario incremental varió de R$ 451.867.881,00 a R$ 768.860.968,00, representando 0,70 a 1,53% de gastos anuales totales con medicamentos de ambulatorios en el SUS; en el mejor y el peor escenario los resultados variaron de R$ 289.160.835,00 a R$ 1.107.081.926,00. Conclusión: el uso de terapia dirigida comparado a la dacarbazina implica en impacto excesivo en el presupuesto, desfavoreciendo una eventual incorporación.

Objective: to estimate the incremental budget impact of target therapy for first-line treatment of advanced non-surgical and metastatic melanoma compared to dacarbazine treatment. Methods: budget impact analysis, from the Brazilian National Health System (SUS) perspective; based on demographic data and incidence estimates, the population over a three-year time horizon (2018-2020) was delimited and the direct medical costs were estimated; the reference scenario was treatment with dacarbazine, and the alternative scenarios were target therapy with vemurafenib, dabrafenib, vemurafenib + cobimetinib and dabrafenib + trametinib; uncertainty assessment was conducted through scenario analysis. Results: the incremental budget impact ranged from R$ 451,867,881.00 to R$ 768,860,968.00, representing 0.70 to 1.53% of total SUS annual outpatient drugs expenditure; in best and worst scenario, results ranged from R$ 289,160,835.00 to R$ 1,107,081,926.00. Conclusion: the use of target therapy compared to dacarbazine implies an excessive impact on the budget, this bring unfovorable to its possible incorporation.
Descritores: Custos e Análise de Custo/tendências
Dacarbazina/administração & dosagem
Dacarbazina/uso terapêutico
Terapia de Alvo Molecular/métodos
Terapia de Alvo Molecular/tendências
Melanoma/tratamento farmacológico
Melanoma/epidemiologia
-Neoplasias Cutâneas/tratamento farmacológico
Sistema Único de Saúde
Saúde Pública/tendências
Custos de Cuidados de Saúde/tendências
Metástase Neoplásica/tratamento farmacológico
Antineoplásicos/economia
Limites: Humanos
Responsável: BR275.1 - Biblioteca


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Id: lil-553370
Autor: Costa, Patrícia Luiza Nunes da.
Título: O microambiente tumoral como alvo terapêutico: avaliação do efeito de antagonistas do receptor de bradicinina tipo 1 em melanoma murino / Tumor microenvironment as therapeutic target: evaluation of the effect of bradkinin receptor 1 antagonists in murine melanoma.
Fonte: São Paulo; s.n; 2009. 182 p. ilus, tab.
Idioma: pt.
Tese: Apresentada a Fundação Antônio Prudente para obtenção do grau de Doutor.
Resumo: O microambiente tumoral tem sido considerado um importante alvo para terapias anticâncer. Recentemente, o receptor de bradicinina tipo 1 (BKR1), o qual é expresso em leucócitos e células endoteliais, foi implicado na progressão de diversos cânceres, incluindo o melanoma... Dois diferentes métodos foram utilizados na seleção de genes diferencialmente expressos (differentially expressed genes -DEGs): o test “t de Student” e o teste Limma. Um total de 87 DEGs foram selecionadas com fold change >1,5 e valor de p<0,05. Alguns desses genes, envolvidos em importantes processos como angiogênese, invasão, metástase e quimioresistência, têm sido validados por PCR em tempo real, como: transglutaminase-2, HSP-1b, neuropilina-2, serpine 1, fator de crescimento do tecido conjuntivo (Ctgf) e serglicina. Em um segundo conjunto de experimentos foi avaliado o efeito de antagonistas de BKR1 em alterações de permeabilidade vascular e distribuição de droga fluorescente (doxorrubicina) no microambiente do tumor. Os antagonistas de BKR1, R-954 e R-715, causaram redução da penetração de doxorrubicina no microambiente tumoral após tratamento por 2 horas, precedido ou não de tratamento crônico (diário), entretanto após 6 horas de tratamento foi observado um aumento da quantidade de doxorrubicina, comparado ao controle, seguido de redução após 24 horas de tratamento. Já em tumores EMT6 (sarcoma mamário murino) após 2 horas de tratamento com esses antagonistas foi possível observar um aumento da quantidade de doxorrubicina no microambiente tumoral. Esses resultados sugerem mecanismos pelos quais as complexas interações entre as células tumorais e as células do hospedeiro podem resultar na resistência tumoral aos quimioterápicos e a consequente falha dos tratamentos convencionais.

Tumor microenvironment has been considered an important target for anticancer therapies. Recently, the bradykinin receptor type 1 (BKR1), which is expressed on leukocytes and endothelial cells, has been implicated in the progression of several cancers, including melanoma. In this work we have shown that there is a delay in BKR1 knockout mice melanoma engraftment and we also observed higher survival rates in these animals compared to wild type mice. We have investigated the effects of selectives BKR1 antagonists evaluating its combination with the chemotherapeutic agent dacarbazine (DTIC). B16-F10 melanoma cells were injected subcutaneously in C57bl/6 mice, which were treated with DTIC (2mg/kg) every 3 days, R-954 (1mg/kg) daily, DTIC plus R-954 or PBS, as control. Mice were sacrificed at day 12 of treatment; tumors were excised and processed for RNA extraction. Treatments with R-954, DTIC or R-954 plus DTIC did not reduced tumor mass. However, the combined treatment increased the global survival of mice bearing tumor. Microarray experiments were performed using GeneChip Mouse 430 (Affymetrix). Data was normalized using the RMA method. Two different methods were employed for selection of differentially expressed genes (DEGs):the Student's T-test and the Limma package. A total of 87 DEGs were identified with fold change>1,5 and p value<0,05. Some of these genes, involved in important process as angiogenesis, invasion, metastasis and chemoresistance, had been validated by real time PCR as; transglutaminase-2, HSP-1b, neuropilin-2, serpine 1, connective tissue growth factor and serglycin. In a second set of experiments we evaluated the effect of antagonists BKR1 in vascular permeability alterations and distribution of fluorescent drug (doxorubicin) in tumor microenvironment. BKR1 antagonists, R-954 and R-715, caused a reduction of the penetration of doxorubicin in the tumor microenvironment after treatment for 2 hours, followed or not by chronic treatment (daily), but after 6 hours of treatment was observed an increase in the amount of doxorubicin, compared to the control, followed by reduction after 24 hours of treatment. However, in EMT6 tumors (murine mammary sarcoma) after 2 hours of treatment with these antagonists we observed an increased amount of doxorubicin in tumor microenvironment. These results suggest mechanisms by which the complex interactions between tumor and BKR1 positive host cells may result in tumor resistance to chemotherapeutic agents and the consequent failure of regular treatments.
Descritores: Camundongos
Dacarbazina
Melanoma
Tratamento Farmacológico
Receptores da Bradicinina
Limites: Ratos
Responsável: BR30.1 - Biblioteca
BR30.1


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Id: lil-107240
Autor: Perez, Clara; Salem, Ernesto; Travezan, Rodrigo.
Título: Tratamiento combinado del retinoblastoma avanzado en el Instituto Nacional de Enfermedades Neoplásicas / Advanced retinoblastoma mixed treatment in Instituto Nacional de Enfermedades Neoplásicas
Fonte: Rev. peru. oftalmol;9(2):38-49, 1983. tab, ilus.
Idioma: es.
Descritores: Retinoblastoma/tratamento farmacológico
Ciclofosfamida/uso terapêutico
Dacarbazina/uso terapêutico
-Epidemiologia
Hospitais Estaduais
Seleção Visual
Tipo de Publ: Estudo Comparativo
Responsável: PE1.1 - Oficina Universitária de Biblioteca


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Id: biblio-886195
Autor: Duzgun, Ozgul; Sarici, Inanc Samil; Gokcay, Serkan; Ates, Kivilcim Eren; Yılmaz, Mehmet Bertan.
Título: Effects of nivolumab in peritoneal carcinamatosis of malign melanoma in mouse model
Fonte: Acta cir. bras;32(12):1006-1012, Dec. 2017. tab, graf.
Idioma: en.
Resumo: Abstract Purpose: To evaluate the efficacy of nivolumab and comparison with dacarbazine (DTIC) on peritoneal carcinomatosis of malignant melanoma in mouse model. Methods: Mouse skin melanoma cells was injected under the capsule of the peritoneal surface in the left side of the abdomen. On postoperative day ten, mouses randomised into three groups. Group 1: Control, Group 2: HIPEC (Hyperthermic intraperitoneal chemotherapy) with DTIC and Group 3: HIPEC with Nivolumab. After the sacrification on postoperative day fifteen, peritoneum evaluated macroscopically and histopathologically by using peritoneal regression grading score (PRGS). Results: In the 15th day exploration, all animals developed extensive intraperitoneal tumor growth in Group 1. In Group 2 and Group 3 median tumor size was 0.7±0.3cm and 0.3±0.2cm respectively (p: 0.023). Peritoneal carcinomatosis index (PCI) were significantly lower in Group 3 than other groups (p: 0.019). The lowest total tumor nodules in group 3 was 4 ± 2. The PGRS score was found significantly lower in Group 3 than other groups (p: 0.03). Lymphocytic response rate was found higher in the Group 3. Conclusions: It has been found that nivolumab significantly better than DTIC on peritoneal metastases of malign melanoma in mouse models. Nivolumab treatment gives promising results with pathological evidence in the treatment of metastatic disease of malignant melanoma.
Descritores: Neoplasias Peritoneais/tratamento farmacológico
Peritônio/patologia
Melanoma/tratamento farmacológico
Anticorpos Monoclonais/farmacologia
Antineoplásicos/farmacologia
-Neoplasias Peritoneais/cirurgia
Neoplasias Peritoneais/patologia
Neoplasias Peritoneais/secundário
Peritônio/efeitos dos fármacos
Distribuição Aleatória
Análise de Regressão
Dacarbazina/uso terapêutico
Modelos Animais de Doenças
Avaliação Pré-Clínica de Medicamentos
Gradação de Tumores
Nivolumabe
Hipertermia Induzida
Melanoma/secundário
Anticorpos Monoclonais/uso terapêutico
Antineoplásicos/uso terapêutico
Limites: Animais
Masculino
Ratos
Responsável: BR1.1 - BIREME


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Id: lil-582740
Autor: Cortez, Afonso José Pereira; Dulley, Frederico Luiz; Saboya, Rosaura; Mendrone Júnior, Alfredo; Amigo Filho, Ulisses; Coracin, Fabio Luiz; Buccheri, Valéria; Linardi, Camila da Cruz Gouveia; Ruiz, Milton Artur; Chamone, Dalton de Alencar Fischer.
Título: Autologous hematopoietic stem cell transplantation in classical Hodgkin's lymphoma
Fonte: Rev. bras. hematol. hemoter;33(1):10-14, Feb. 2011. graf, tab.
Idioma: en.
Resumo: BACKGROUND: Hodgkin's lymphoma has high rates of cure, but in 15 percent to 20 percent of general patients and between 35 percent and 40 percent of those in advanced stages, the disease will progress or will relapse after initial treatment. For this group, hematopoietic stem cell transplantation is considered one option of salvage therapy. OBJECTIVES: To evaluate a group of 106 patients with Hodgkin's lymphoma, who suffered relapse or who were refractory to treatment, submitted to autologous hematopoietic stem cell transplantation in a single transplant center. METHODS: A retrospective study was performed with data collected from patient charts. The analysis involved 106 classical Hodgkin's lymphoma patients who were consecutively submitted to high-dose chemotherapy followed by autologous transplants in a single institution from April 1993 to December 2006. RESULTS: The overall survival rates of this population at five and ten years were 86 percent and 70 percent, respectively. The disease-free survival was approximately 60 percent at five years. Four patients died of procedure-related causes but relapse of classical Hodgkin's lymphoma after transplant was the most frequent cause of death. Univariate analysis shows that sensitivity to pre-transplant treatment and hemoglobin < 10 g/dL at diagnosis had an impact on patient survival. Unlike other studies, B-type symptoms did not seem to affect overall survival. Lactic dehydrogenase and serum albumin concentrations analyzed at diagnosis did not influence patient survival either. CONCLUSION: Autologous hematopoietic stem cell transplantation is an effective treatment strategy for early and late relapse in classical Hodgkin's lymphoma for cases that were responsive to pre-transplant chemotherapy. Refractory to treatment is a sign of worse prognosis. Additionally, a hemoglobin concentration below 10 g/dL at diagnosis of Hodgkin's lymphoma has a negative impact on the survival of patients after transplant. As far as we know this relationship has not been previously reported.
Descritores: Transplante Autólogo
Vimblastina
Bleomicina
Doença de Hodgkin
Doxorrubicina
Estudos Retrospectivos
Transplante de Células-Tronco Hematopoéticas
Dacarbazina
Limites: Humanos
Masculino
Feminino
Responsável: BR408.1 - Biblioteca da Faculdade de Medicina - BFM


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Id: biblio-898956
Autor: Jaime-Pérez, José Carlos; Gamboa-Alonso, Carmen Magdalena; Padilla-Medina, José Ramón; Jiménez-Castillo, Raúl Alberto; Olguín-Ramírez, Leticia Alejandra; Gutiérrez-Aguirre, César Homero; Cantú-Rodríguez, Olga Graciela; Gómez-Almaguer, David.
Título: High frequency of primary refractory disease and low progression-free survival rate of Hodgkin's lymphoma: a decade of experience in a Latin American center
Fonte: Rev. bras. hematol. hemoter;39(4):325-330, Oct.-Dec. 2017. tab.
Idioma: en.
Resumo: Abstract Background: Reports dealing with clinical outcomes of classical Hodgkin's lymphoma in low- to middle-income countries are scarce and response to therapy is poorly documented. This report describes the characteristics and clinical outcomes of patients with classical Hodgkin's lymphoma from a single institution in Latin America. Method: A retrospective study was conducted over ten years of patients with classical Hodgkin's lymphoma treated at a referral center. Progression-free and overall survival rates were estimated by Kaplan-Meier analysis. The univariate Cox regression model was used to estimate associations between important variables and clinical outcomes. Main results: One hundred and twenty-eight patients were analyzed. The mean age was 28.5 years. The five-year progression-free and overall survival were 37.3% and 78.9%, respectively. Of the whole group, 55 (43%) were primary refractory cases. Only 39/83 (47%) patients with advanced disease vs. 34/45 (75.6%) in early stages (p-value = 0.002) achieved complete remission. Those with advanced disease had a five-year overall survival of 68.7% vs. 91.8% for early disease (p-value = 0.132). Thirty-one patients relapsed (24.2%) and 20 (64.5%) received a transplant. The hazard ratio for progression with bone marrow infiltration was 2.628 (p-value = 0.037). For death, an International Prognostic Score ≥4 had a hazard ratio of 3.355 (p-value = 0.050) in univariate analysis. Two-thirds of classical Hodgkin's lymphoma patients diagnosed at advanced stages had a low progression-free survival but an overall survival similar to high-income countries. Conclusion: Patients diagnosed with classical Hodgkin's lymphoma in Northeastern Mexico had a significantly low progression-free survival rate and presented with advanced disease, underscoring the need for earlier diagnosis and improved contemporary therapeutic strategies in these mainly young productive-age Hodgkin's lymphoma patients.
Descritores: Vincristina
Bleomicina
Doença de Hodgkin
Doxorrubicina
Taxa de Sobrevida
Dacarbazina
América Latina
Responsável: BR408.1 - Biblioteca da Faculdade de Medicina - BFM


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Id: lil-746680
Autor: Homedes, Núria; Ugalde, Antonio.
Título: El ciclo de los medicamentos: su impacto en el acceso y el uso adecuado / The medication cycle: its impact on access to and adequate use of drugs
Fonte: Salud colect;11(1):5-8, ene.-mar. 2015.
Idioma: es.
Descritores: Antineoplásicos/uso terapêutico
Proteínas de Neoplasias/antagonistas & inibidores
Neoplasias/tratamento farmacológico
Poli(ADP-Ribose) Polimerases/antagonistas & inibidores
-Antineoplásicos/farmacologia
Ensaios Clínicos como Assunto
Reparo do DNA/efeitos dos fármacos
DNA de Neoplasias/efeitos dos fármacos
DNA de Neoplasias/metabolismo
Sistemas de Liberação de Medicamentos
Desenho de Fármacos
Resistencia a Medicamentos Antineoplásicos
Ensaios de Seleção de Medicamentos Antitumorais
Sinergismo Farmacológico
Dacarbazina/administração & dosagem
Dacarbazina/análogos & derivados
Dacarbazina/farmacologia
Camundongos Knockout
Proteínas de Neoplasias/fisiologia
Neoplasias/enzimologia
Poli(ADP-Ribose) Polimerases/química
Poli(ADP-Ribose) Polimerases/deficiência
Poli(ADP-Ribose) Polimerases/genética
Poli(ADP-Ribose) Polimerases/fisiologia
Tolerância a Radiação/efeitos dos fármacos
Limites: Animais
Humanos
Camundongos
Tipo de Publ: Research Support, Non-U.S. Gov't
Revisão
Responsável: BR1.1 - BIREME


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Id: lil-744479
Autor: Sifontes-Rodríguez, Sergio; Monzote-Fidalgo, Lianet; Castañedo-Cancio, Nilo; Montalvo-Álvarez, Ana Margarita; López-Hernández, Yamilé; Diogo, Niurka Mollineda; Infante-Bourzac, Juan Francisco; Pérez-Martín, Oliver; Meneses-Marcel, Alfredo; García-Trevijano, José Antonio Escario; Cabrera-Pérez, Miguel Ángel.
Título: The efficacy of 2-nitrovinylfuran derivatives against Leishmania in vitro and in vivo
Fonte: Mem. Inst. Oswaldo Cruz;110(2):166-173, 04/2015. tab, graf.
Idioma: en.
Resumo: Despite recent advances in the treatment of some forms of leishmaniasis, the available drugs are still far from ideal due to inefficacy, parasite resistance, toxicity and cost. The wide-spectrum antimicrobial activity of 2-nitrovinylfuran compounds has been described, as has their activity against Trichomonas vaginalis and other protozoa. Thus, the aim of this study was to test the antileishmanial activities of six 2-nitrovinylfurans in vitro and in a murine model of leishmaniasis. Minimum parasiticide concentration (MPC) and 50% inhibitory concentration (IC50) values for these compounds against the promastigotes of Leishmania amazonensis, Leishmania infantum and Leishmania braziliensis were determined, as were the efficacies of two selected compounds in an experimental model of cutaneous leishmaniasis (CL) caused by L. amazonensis in BALB/c mice. All of the compounds were active against the promastigotes of the three Leishmania species tested. IC50 and MPC values were in the ranges of 0.8-4.7 µM and 1.7-32 µM, respectively. The compounds 2-bromo-5-(2-bromo-2-nitrovinyl)-furan (furvina) and 2-bromo-5-(2-methyl-2-nitrovinyl)-furan (UC245) also reduced lesion growth in vivo at a magnitude comparable to or higher than that achieved by amphotericin B treatment. The results demonstrate the potential of this class of compounds as antileishmanial agents and support the clinical testing of Dermofural(r) (a furvina-containing antifungal ointment) for the treatment of CL.
Descritores: Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico
Doença de Hodgkin/tratamento farmacológico
Doença de Hodgkin/patologia
-Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos
Bleomicina/efeitos adversos
Bleomicina/uso terapêutico
Terapia Combinada
Tomada de Decisões
Dacarbazina/efeitos adversos
Dacarbazina/uso terapêutico
Doxorrubicina/efeitos adversos
Doxorrubicina/uso terapêutico
Doença de Hodgkin/mortalidade
Estadiamento de Neoplasias
Guias de Prática Clínica como Assunto
Medição de Risco
Resultado do Tratamento
Vimblastina/efeitos adversos
Vimblastina/uso terapêutico
Limites: Humanos
Tipo de Publ: Revisão
Responsável: BR1.1 - BIREME



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