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https://www.readbyqxmd.com/read/27911119/phase-ii-study-of-dasatinib-in-previously-treated-patients-with-advanced-non-small-cell-lung-cancer
#1
Michael J Kelley, Gautam Jha, Debra Shoemaker, James E Herndon, Lin Gu, William T Barry, Jeffrey Crawford, Neal Ready
The Src pathway in activated in about one-third of non-small cell lung cancer (NSCLC) tumors. Dasatinib has Src-inhibitor activity. We examined the activity of dasatinib in 37 patients with advanced, previously treated NSCLC. Among the 29 patients who underwent pre-treatment biopsy for RNA biomarker analysis, 25 were treated with dasatinib 70 mg twice daily. There were no responses. Five patients discontinued treatment due to toxicity. Three patients had minor biopsy-related pneumothoraces. Given the lack of responses, no biomarkers were analyzed...
December 2, 2016: Cancer Investigation
https://www.readbyqxmd.com/read/27908221/dasatinib-prevent-hepatic-fibrosis-induced-by-carbon-tetrachloride-ccl4-via-anti-inflammatory-and-antioxidant-mechanism
#2
Adel Mohammadalipour, Jamshid Karimi, Iraj Khodadadi, Ghasem Solgi, Mohammad Hashemnia, Nasrin Sheikh, Majid Bahabadi
OBJECTIVES: Dasatinib, a potent and broad-spectrum tyrosine kinase inhibitor, is approved for the treatment of imatinib-resistant chronic myelogenous leukemia. The aim of this study was to evaluate the anti-fibrotic, anti-inflammatory and antioxidant effects of this agent against CCl4-induced hepatic fibrosis and oxidative status. MATERIALS AND METHODS: Experimental fibrosis was induced in Wistar male rats by 12 weeks of CCl4 administration (i.p.). During the last 8 weeks of injection, rats were gavaged daily with Dasatinib (10 mg/kg)...
December 1, 2016: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/27904083/novel-sulfonamide-derivatives-carrying-a-biologically-active-3-4-dimethoxyphenyl-moiety-as-vegfr-2-inhibitors
#3
Mostafa Mohammed Ghorab, Mansour Sulaiman Alsaid, Yassin Mohammed Nissan, Abdelkader Elbadawy Ashour, Abdullah Abdulalrahman Al-Mishari, Ashok Kumar, Sheikh Fayaz Ahmed
Novel sulfonamides 3-19 with a biologically active 3,4-dimethoxyphenyl moiety were designed and synthesized. The structures of the synthesized compounds were established using elemental analyses, IR, (1)H-NMR, (13)C-NMR spectral data and mass spectroscopy. All the synthesized compounds were evaluated for their in vitro anticancer activity against four cancer cell lines, namely human hepatocellular carcinoma (HepG2), human medulloblastoma (Daoy), human cervical cancer (HeLa), and human colon cancer (HT-29), by using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and dasatinib as the reference drug...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27901368/second-line-small-molecule-therapy-options-for-treating-chronic-myeloid-leukemia
#4
Matteo Molica, Fulvio Massaro, Massimo Breccia
Approximately 33% of chronic myeloid leukemia (CML) patients discontinue treatment with imatinib in the long-term due to resistance and/or intolerance. Second-generation tyrosine kinase inhibitors (TKIs) (dasatinib, nilotinib, bosutinib) and third-generation (ponatinib) have added complexity to the treatment paradigm for this disease. Areas covered: Second generation TKIs, approved as second-line treatment in all phases of the disease, are highly effective in patients resistant to and/or intolerant to imatinib and are extremely active against all the resistant BCR-ABL1 mutations, with the exception of T3151...
November 30, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27900042/antitumor-activity-of-7rh-a-discoidin-domain-receptor-1-inhibitor-alone-or-in-combination-with-dasatinib-exhibits-antitumor-effects-in-nasopharyngeal-carcinoma-cells
#5
Qiu-Ping Lu, Wen-Dan Chen, Jie-Ren Peng, Yao-Dong Xu, Qian Cai, Gong-Kan Feng, Ke Ding, Xiao-Feng Zhu, Zhong Guan
Dysregulation of the discoidin domain receptors (DDRs) has been implicated in the development of numerous types of tumors, including head and neck cancer, and nasopharyngeal, breast, ovarian and esophageal carcinomas. Furthermore, agents that inhibit DDR1 activity are hypothesized to be useful for the treatment of nasopharyngeal carcinoma (NPC). The aim of the present study was to evaluate the effect of the DDR1 inhibitory (3-(2-(pyrazolo(1,5-a)pyrimidin-6-yl)-ethynyl)benzamide compound, 7RH, in NPC cells both in vitro and in vivo, and its effect when used in combination with dasatinib, a SRC family kinase (SFK) inhibitor...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27895735/crk-like-adapter-protein-is-overexpressed-in-cervical-carcinoma-facilitates-proliferation-invasion-and-chemoresistance-and-regulates-src-and-akt-signaling
#6
Hong Ji, Bo Li, Shitai Zhang, Zheng He, Yang Zhou, Ling Ouyang
Overexpression of Crk-like (CrkL) adapter protein has been implicated in a number of types of human cancer. However, its involvement in human cervical carcinoma remains unclear. The present study aimed to explore the clinical significance and biological characteristics of CrkL in human cervical carcinoma. CrkL protein expression was examined in tissue samples from 92 cases of cervical carcinoma using immunohistochemistry, and was found to be overexpressed in 48.9% (45/92 cases). CrkL was transfected into HeLa and CaSki cervical carcinoma cell lines and its effects on biological behavior were examined...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27875633/design-synthesis-and-evaluation-of-dasatinib-amino-acid-and-dasatinib-fatty-acid-conjugates-as-protein-tyrosine-kinase-inhibitors
#7
Rakesh K Tiwari, Alex Brown, Amir Nasrolahi Shirazi, Jared Bolton, Amanda Tse, Gennady Verkhivker, Keykavous Parang, Gongqin Sun
Derivatives of dasatinib were synthesized via esterification with 25 carboxylic acids including amino acids and fatty acids by extending the inhibitor to interact with more diverse sites and to improve specificity. Dasatinib-L-arginine derivative (Das-R, 7) was the most potent of the inhibitors tested with IC50 values of 4.4 nM, <0.25 nM, and <0.45 nM against Csk, Src, and Abl kinases, respectively. The highest selectivity ratio obtained in our study, 91.4 Csk/Src belonged to compound 18 (Das-C10) with an IC50 of 3...
November 22, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27864292/clinical-efficacy-of-fecal-occult-blood-test-and-colonoscopy-for-dasatinib-induced-hemorrhagic-colitis-in-cml-patients
#8
Satoshi Nishiwaki, Matsuyoshi Maeda, Masahiro Yamada, Shingo Okuno, Yasuhiko Harada, Kotaro Suzuki, Shingo Kurahashi, Fumihiro Urano, Shozo Okamura, Isamu Sugiura
A positive fecal occult blood test (FOBT) is occasionally observed in some chronic myeloid leukemia (CML) patients treated with a tyrosine kinase inhibitor (TKI), and hemorrhagic colitis in patients treated with dasatinib has been reported. To clarify the frequency of TKI-induced hemorrhagic colitis and the screening efficacy of an FOBT followed by a colonoscopy, we prospectively enrolled CML patients treated with a TKI. FOBTs were performed in all patients and colonoscopy was performed in patients with positive FOBTs...
November 18, 2016: Blood
https://www.readbyqxmd.com/read/27861317/development-and-validation-of-a-simultaneous-quantification-method-of-fourteen-tyrosine-kinase-inhibitors-in-human-plasma-using-lc-ms-ms
#9
Huu-Hien Huynh, Claire Pressiat, Hélène Sauvageon, Isabelle Madelaine, Patricia Maslanka, Céleste Lebbé, Catherine Thieblemont, Lauriane Goldwirt, Samia Mourah
BACKGROUND: A sensitive LC-MS/MS method for the analysis in a small volume of plasma of 14 tyrosine kinase inhibitors (TKIs) currently used (imatinib, dasatinib, ibrutinib, ponatinib, trametinib, sunitinib, cobimetinib, dabrafenib, erlotinib, lapatinib, nilotinib, bosutinib, sorafenib, and vemurafenib) has been developed and validated. This multi-analyte LC-MS/MS assay is of interest for anticancer drug combination therapy. METHODS: After a simple protein precipitation of plasma samples, the chromatographic separation was performed using a UPLC system coupled with MS/MS in a positive ionization mode...
November 16, 2016: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/27858461/how-could-patient-reported-outcomes-improve-patient-management-in-chronic-myeloid-leukemia
#10
Federico De Marchi, Marta Medeot, Renato Fanin, Mario Tiribelli
Patients reported outcome (PRO) are still under-used in patients with chronic myeloid leukemia (CML) treated with tyrosine kinase inhibitors (TKIs), though data on the correlation between quality of life (QoL) and therapeutic efficacy are increasingly known. Chronic low-grade toxicities can reduce patient's QoL and negatively impact on adherence. Areas covered: This review will focus on the role of QoL questionnaires in patients with CML, receiving imatinib or newer TKIs (dasatinib, nilotinib, bosutinib, ponatinib)...
November 30, 2016: Expert Review of Hematology
https://www.readbyqxmd.com/read/27852118/risk-of-arterial-and-venous-occlusive-events-in-chronic-myeloid-leukemia-patients-treated-with-new-generation-bcr-abl-tyrosine-kinase-inhibitors-a-systematic-review-and-meta-analysis
#11
Hélène Haguet, Jonathan Douxfils, François Mullier, Christian Chatelain, Carlos Graux, Jean-Michel Dogné
BACKGROUND: A previous meta-analysis demonstrated that 3 of the new-generation BCR-ABL tyrosine kinase inhibitors (TKIs) (dasatinib, nilotinib and ponatinib) are associated with an increased risk of vascular occlusive events in patients with Ph+ chronic myeloid leukemia compared with imatinib. This meta-analysis of randomized controlled trials aims at assessing these risks separately. METHODS: The literature search was performed by two independent reviewers following the previous protocol (PROSPERO 2014:CRD42014014147)...
November 17, 2016: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/27848186/dasatinib-induces-autophagy-in-mice-with-bcr-abl-positive-leukemia
#12
Makiko Morita, Yoko Nishinaka, Itaru Kato, Satoshi Saida, Hidefumi Hiramatsu, Yasuhiko Kamikubo, Toshio Heike, Tatsutoshi Nakahata, Souichi Adachi
Dasatinib, a second-generation tyrosine kinase inhibitor, is a highly effective treatment for Bcr-Abl-positive leukemia. However, the mechanism by which dasatinib induces cell death is unclear, particularly in vivo. Autophagy is a lysosomal degradation mechanism essential for cell survival and differentiation. Autophagy also protects cells from the effects of drugs, including those used to treat leukemia. Here, we report that dasatinib induces autophagy in Bcr-Abl-positive leukemia cell lines and further show the induction of autophagy in an immunodeficient mouse model of human Bcr-Abl-positive leukemia with central nervous system (CNS) infiltration...
November 15, 2016: International Journal of Hematology
https://www.readbyqxmd.com/read/27847941/atomic-force-microscopy-and-graph-analysis-to-study-the-p-cadherin-sfk-mechanotransduction-signalling-in-breast-cancer-cells
#13
A S Ribeiro, F A Carvalho, J Figueiredo, R Carvalho, T Mestre, J Monteiro, A F Guedes, M Fonseca, J Sanches, R Seruca, N C Santos, J Paredes
Physical forces mediated by cell-cell adhesion molecules, as cadherins, play a crucial role in preserving normal tissue architecture. Accordingly, altered cadherins' expression has been documented as a common event during cancer progression. However, in most studies, no data exist linking pro-tumorigenic signaling and variations in the mechanical balance mediated by adhesive forces. In breast cancer, P-cadherin overexpression increases in vivo tumorigenic ability, as well as in vitro cell invasion, by activating Src family kinase (SFK) signalling...
November 16, 2016: Nanoscale
https://www.readbyqxmd.com/read/27842767/drug-hepatotoxicity-newer-agents
#14
REVIEW
Chalermrat Bunchorntavakul, K Rajender Reddy
Idiosyncratic hepatotoxicity is one of the most common reasons for an approved drug being restricted. This article focuses on hepatotoxicity of selected and recently introduced agents, such as, tyrosine kinase inhibitors, monoclonal antibodies, novel oral anticoagulants, newer antiplatelets, antibiotics, anti-diabetics, anti-epileptics, anti-depressants, anti-psychotics and anti-retrovirals. Overall, the incidence of clinically relevant hepatotoxicity from newer agents seems to be lower than that of the older agents...
February 2017: Clinics in Liver Disease
https://www.readbyqxmd.com/read/27825730/nodular-histiocytic-hiperplasia-is-this-a-cause-of-dasatinib-pleural-effusion
#15
Satoshi Hamada, Eiichi Hayashi, Mitsuhiro Tsukino
No abstract text is available yet for this article.
November 5, 2016: Archivos de Bronconeumología
https://www.readbyqxmd.com/read/27810077/chronic-myelogenous-leukemia-with-acquired-t-11-14-q13-q32-ccnd1-igh-a-case-report-and-literature-review
#16
M T Manda-Mapalo, P Khalili, D Quintana, I Rabinowitz, Q Y Zhang
Approximately 5-10% of chronic myeloid leukemia (CML) patients are found to have structural or numerical additional chromosomal abnormality (ACAs) in addition to the characteristic t(9;22)(q34;q11.2) BCR/ABL1 at the time of diagnosis. The prognostic significance of such additional chromosomal abnormalities has been controversial. Translocation t(11;14)(q13;q32) CCND1-IGH is typically associated with mantle cell lymphoma or a subset of plasma cell myeloma and is exceedingly rare in myeloid neoplasm. Here we report a unique case describing a patient found at diagnosis of chronic phase CML to have both the Philadelphia chromosome as well as t(11;14)-a rare cytogenetic combination...
October 2016: Cancer Genetics
https://www.readbyqxmd.com/read/27805766/determination-of-dasatinib-in-the-tablet-dosage-form-by-ultra-high-performance-liquid-chromatography-capillary-zone-electrophoresis-and-sequential-injection-analysis
#17
Aroa Garcia Gonzalez, Lukáš Taraba, Jakub Hraníček, Petr Kozlík, Pavel Coufal
Dasatinib is a novel oral prescription drug proposed for treating adult patients with chronic myeloid leukemia. Three analytical methods, namely ultra high performance liquid chromatography, capillary zone electrophoresis, and sequential injection analysis, were developed, validated and compared for determination of the drug in the tablet dosage form. The total analysis time of optimized ultra high performance liquid chromatography and capillary zone electrophoresis methods was 2.0 and 2.2 min, respectively...
November 2, 2016: Journal of Separation Science
https://www.readbyqxmd.com/read/27803756/dasatinib-induced-pleural-effusion-chylothorax-an-option-to-consider
#18
Lucía Ferreiro, Esther San-José, Juan Suárez-Antelo, Luis Valdés
Dasatinib is a drug for treatment of oncogene fusion protein BCR-ABL-positive chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant/intolerant to imatinib. Pleural effusion (PE) is a common adverse effect, and in this context, we present four cases seen due to this cause. One of them is a chylothorax. The PE grade is variable, and the physiopathology is not well established, although a block in T-lymphocyte function or inhibition of platelet-derived growth factor receptor-β is suggested being involved...
October 2016: Annals of Thoracic Medicine
https://www.readbyqxmd.com/read/27798955/inhibition-of-src-family-kinases-reduces-myeloid-derived-suppressor-cells-in-head-and-neck-cancer
#19
Liang Mao, Wei-Wei Deng, Guang-Tao Yu, Lin-Lin Bu, Jian-Feng Liu, Si-Rui Ma, Lei Wu, Ashok B Kulkarni, Wen-Feng Zhang, Zhi-Jun Sun
SRC family kinases (SFKs), a group of nonreceptor tyrosine kinases, modulate multiple cellular functions, such as cell proliferation, differentiation and metabolism. SFKs display aberrant activity in progressive stages of human cancers. However, the precise role of SFKs in the head and neck squamous cell carcinoma (HNSCC) signaling network is far from clear. In this study, we found that the inhibition of SFKs activity by dasatinib effectively reduced the tumor size and population of MDSCs in the HNSCC mouse model...
October 31, 2016: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/27798188/oxidation-of-kcnb1-potassium-channels-causes-neurotoxicity-and-cognitive-impairment-in-a-mouse-model-of-traumatic-brain-injury
#20
Wei Yu, Randika Parakramaweera, Shavonne Teng, Manasa Gowda, Yashsavi Sharad, Smita Thakker-Varia, Janet Alder, Federico Sesti
: The delayed rectifier potassium (K(+)) channel KCNB1 (Kv2.1), which conducts a major somatodendritic current in cortex and hippocampus, is known to undergo oxidation in the brain, but whether this can cause neurodegeneration and cognitive impairment is not known. Here, we used transgenic mice harboring human KCNB1 wild-type (Tg-WT) or a nonoxidable C73A mutant (Tg-C73A) in cortex and hippocampus to determine whether oxidized KCNB1 channels affect brain function. Animals were subjected to moderate traumatic brain injury (TBI), a condition characterized by extensive oxidative stress...
October 26, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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