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Tirosine kinase inhibitor

Daniele Santini, Matteo Santoni, Alessandro Conti, Giuseppe Procopio, Elena Verzoni, Luca Galli, Giuseppe di Lorenzo, Ugo De Giorgi, Delia De Lisi, Maurizio Nicodemo, Marco Maruzzo, Francesco Massari, Sebastiano Buti, Emanuela Altobelli, Elisa Biasco, Riccardo Ricotta, Camillo Porta, Bruno Vincenzi, Rocco Papalia, Paolo Marchetti, Luciano Burattini, Rossana Berardi, Giovanni Muto, Rodolfo Montironi, Stefano Cascinu, Giuseppe Tonini
PURPOSE: We retrospectively analyzed the risk of recurrence and conditional Disease-Free Survival (cDFS) in 63 patients with complete remission during treatment with tirosin kinase inhibitor (TKI), alone or with local treatment in metastatic renal cell carcinoma. RESULTS: 37% patients achieve CR with TKI alone, while 63% with additional loco-regional treatments. 49% patients recurred after CR, with a median Disease free survival of 28.2 months. Patients treated with multimodal approaches present lower rate of recurrence (40% vs 61%) and longer Disease free survival compared to patient treated with TKI alone (16...
May 31, 2016: Oncotarget
Dafne Moreno-Lorenzana, Sócrates Avilés-Vazquez, Miguel Angel Sandoval Esquivel, Antonio Alvarado-Moreno, Vianney Ortiz-Navarrete, Héctor Torres-Martínez, Manuel Ayala-Sánchez, Héctor Mayani, Antonieta Chavez-Gonzalez
Chronic Myeloid Leukemia (CML) is sustained by a small population of cells with stem cell characteristics known as Leukemic Stem Cells that are positive to BCR-ABL fusion protein, involved with several abnormalities in cell proliferation, expansion, apoptosis and cell cycle regulation. Current treatment options for CML involve the use of Tirosine Kinase Inhibitor (Imatinib, Nilotinib and Dasatinib), that efficiently reduce proliferation proliferative cells but do not kill non proliferating CML primitive cells that remain and contributes to the persistence of the disease...
May 2, 2016: Cell Cycle
Federica Biello, Giovanni Burrafato, Erika Rijavec, Carlo Genova, Giulia Barletta, Anna Truini, Simona Coco, Maria Giovanna Dal Bello, Angela Alama, Francesco Boccardo, Francesco Grossi
Lung cancer is still the leading cause of cancer related death worldwide. Fibroblast growth factor receptor (FGFR) is a tirosine-kinase receptor that is seen to be amplified or mutated in non-small cell lung cancer (NSCLC) and it plays a crucial role in tumour development and maintenance. The authors analyzed the state of the art of FGFR by reviewing the current literature. Fibroblast growth factor (FGF)-FGFR pathway and their aberrations are described, with the evaluation of their possible prognostic role in NSCLC and in particular in squamous cell carcinomas, in which FGFR is more often amplified...
2016: Anti-cancer Agents in Medicinal Chemistry
S A Protsenko, A V Rudakova
Therapy for advanced non-small cell lung cancer (NSCLC) is very complex clinical problem. The optimal choice of therapy demands not only the analysis of data on clinical effectiveness, but also an assessment of cost-effectiveness of the applied drugs. The current options for first- or second/third-line of lung cancer treatment are tirosine kinase inhibitors (TKI)--gefitinib, erlotinib and afatinib. According to the received results TKI first-line therapy for NSCLC in patients with EGFR mutations is not only clinically effective but also is economically acceptable from a position of the Russian budgetary health care...
2015: Voprosy Onkologii
Bárbara Parente, Joana Gomes, Carla Nogueira, Diva Ferreira, Sofia Neves, Ana Barroso, Sara Conde, José Carlos Machado
Early studies with tirosine kinase inhibitors (TKI), namely Erlotinib and Gefitinib, in patients with non small cell lung cancer (NSCLC), showed that although most patients did not respond radiologically, a small percentage of those patients (about 10%) had an excellent response to treatment, with radiological regression and clinical response duration. Four patient populations are known as having better response to TKI as opposed to other patients: adenocarcinoma patients, non-smokers, women and asians. Nevertheless, a good general status remains a predictive factor for treatment response...
October 2008: Revista Portuguesa de Pneumologia
Silvia Stacchiotti, Flavio Crippa, Antonella Messina, Silvana Pilotti, Alessandro Gronchi, Jean Y Blay, Paolo G Casali
BACKGROUND: Pigmented villonodular synovitis (PVNS) is a rare locally aggressive tumor. PVNS is characterized in most cases by a specific t(1;2) translocation, which fuses the colony stimulating factor-1 (CSF1) gene to the collagen type VIa3 (COL6A3) promoter thus leading through a paracrine effect to the attraction of non-neoplastic inflammatory cells expressing CSF1-receptor. Imatinib is a tirosin-kinase inhibitors (TKI) active against CSF1-receptor whose activity in naïve PVNS was already described...
2013: Clinical Sarcoma Research
Silvia Stacchiotti, Gian Paolo Dagrada, Carlo Morosi, Tiziana Negri, Antonella Romanini, Silvana Pilotti, Alessandro Gronchi, Paolo G Casali
UNLABELLED: HASH(0x39ab7e8) BACKGROUND: Extraskeletal myxoid chondrosarcoma (EMCS) is a rare soft tissue sarcoma of uncertain differentiation, characterized in most cases by a translocation that results in the fusion protein EWSR1-CHN (the latter even called NR4A3 or TEC). EMCS is marked by >40% incidence of metastases in spite of its indolent behaviour. It is generally resistant to conventional chemotherapy, and, to the best of our knowledge, no data have been reported to date about the activity of tirosin-kinase inhibitor (TKI) in this tumor...
2012: Clinical Sarcoma Research
Jacopo Olivieri, Sabrina Coluzzi, Imma Attolico, Attilio Olivieri
Chronic Graft Versus Host Disease (cGVHD) is a major complication of allogeneic stem-cell transplantation (SCT). In many inflammatory fibrotic diseases, such as Systemic Scleroderma (SSc) and cGVHD with fibrotic features, an abnormal activation of transforming growth factor (TGFβ) and platelet-derived growth factor receptor (PDGF-R) pathways have been observed. Tyrosin Kinase Inhibitors (TKIs), which are currently used for treatment of patients with Chronic Myeloid Leukemia (CML), share potent antifibrotic and antiinflammatory properties, being powerful dual inhibitors of both PDGF-R and TGFβ pathways...
2011: TheScientificWorldJournal
Alberto Zambelli, Matteo Giovanni Della Porta, Ermanno Eleuteri, Luciana De Giuli, Oronzo Catalano, Carlo Tondini, Alberto Riccardi
Treatment of breast cancer (BC) has changed over the last decade with the advent of targeted therapies. Whereas traditional chemotherapy was directed toward all rapidly dividing cells (cancerous or not), several new anti-cancer drugs are mainly tailored to specific genetic pathways of cancer cells. Ideally, the goal of these new therapies is to improve the management of cancer with a specific targeting of the malignant cell and fewer side effects than traditional chemotherapy. Due to the initial success of this approach, an increasing number of targeted drugs entered into clinical development...
April 2011: Breast: Official Journal of the European Society of Mastology
António Almeida, Isabel Castro, Jorge Coutinho, Lurdes Guerra, Herlander Marques, Ana Marques Pereira
Chronic Myeloid Leukemia (CML) is a clonal stem cell disease characterized by the expression of the fusion protein bcr-abl1, which has deregulated tirosine-kinase activity. Tyrosine kinase inhibitors (TKIs), and in particular imatinib, introduced fundamental changes in the treatment of CML, becoming, in most cases, the first-line treatment of choice in the chronic phase of this disease. Compared to other available therapies imatinib results in a marked increase in overall survival, tolerability and quality of life...
September 2009: Acta Médica Portuguesa
M Gutiérrez, A I Fernández, M P Revuelta, B Cantabrana, A Hidalgo
1. The effects of 17 alpha-estradiol on KCl (60 mM), CaCl2 (30 microM to 10 mM) and vanadate (0.3 mM)-induced contractions in rat uterus have been assayed. Furthermore, the effect of 17 alpha-estradiol on calmodulin-stimulated cAMP-phosphodiesterase activity was also studied. 2. 17 alpha-estradiol relaxed the tonic contraction induced by KCl (60 mM) in a concentration-dependent way (IC50, 8.3 +/- 0.7 microM), and CaCl2 (0.1 to 10 mM) counteracted it. 3. CaCl2 (30 microM to 10 mM) produced concentration-dependent contraction of rat uterus in a calcium-free medium supplemented with 60 mM of KCl (EC50: 0...
January 1998: General Pharmacology
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