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https://www.readbyqxmd.com/read/29643994/grape-seed-procyanidin-extract-against-lung-cancer-the-role-of-microrna-106b-bioavailability-and-bioactivity
#1
Bingye Xue, Qing-Yi Lu, Larry Massie, Clifford Qualls, Jenny T Mao
MiR-106b is an oncomir and a potential target for anti-cancer therapy. We hypothesize that grape seed procyanidin extract (GSE) exerts antineoplastic effects on lung cancer through modulations of miR-106b and its downstream target. We found that GSE significantly down-regulated miR-106b in a variety of lung neoplastic cells and increased cyclin-dependent kinase inhibitor 1A ( CDKN1A ) mRNA and protein (p21) levels. Transfection of miR-106b mimics reversed the up-regulations of CDKN1A mRNA and p21, abrogated the GSE induced anti-proliferative and anti-invasive properties in lung cancer cells...
March 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29568368/trifluridine-tipiracil-overcomes-the-resistance-of-human-gastric-5-fluorouracil-refractory-cells-with-high-thymidylate-synthase-expression
#2
Kazuaki Matsuoka, Fumio Nakagawa, Takashi Kobunai, Teiji Takechi
Trifluridine/tipiracil (FTD/TPI or TFTD, also known as TAS-102) is a combination of the antineoplastic thymidine analog, FTD, and thymidine phosphorylase inhibitor, TPI (molar ratio 1:0.5). FTD/TPI was approved in Japan, the United States, and the European Union for the treatment of unresectable advanced or recurrent colorectal cancer. We evaluated the in vitro and in vivo efficacy and mechanisms of action of FTD and FTD/TPI against 5-fluorouracil (5-FU)-resistant MKN45/5FU, MKN74/5FU, and KATOIII/5FU human gastric cancer cells overexpressing thymidylate synthase (TS) and their respective parent cell lines...
March 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29561706/potential-of-bcl2-as-a-target-for-chronic-lymphocytic-leukemia-treatment
#3
Riccardo Moia, Fary Diop, Chiara Favini, Ahad Ahmed Kodipad, Gianluca Gaidano
Chronic lymphocytic leukemia (CLL) is a highly heterogeneous disease. Deregulation of apoptosis is a major pathogenetic feature, and represents a therapeutic target. TP53 disrupted patients are categorized as high risk patients and are treated with novel target therapies. Among these new drugs, venetoclax, an orally bioavailable BCL2 inhibitor, has shown high efficacy also in relapsed/refractory CLL with TP53 disruption. Venetoclax has also been tested in combination with other drugs without compromising venetoclax dose and with a good safety profile...
March 21, 2018: Expert Review of Hematology
https://www.readbyqxmd.com/read/29558225/bioactivity-and-pharmacological-properties-of-%C3%AE-mangostin-from-the-mangosteen-fruit-a-review
#4
Guoqing Chen, Yong Li, Wei Wang, Liping Deng
Introduction Mangosteen as a rare and precious fruit looks like a queen crown, known as "Queen of Fruit". α-Mangostin (α-MG) is the most representative xanthone isolated from the pericarp of mangosteen, possessing extensive biological activities and pharmacological properties, which can be considered as an antineoplastic agent, antioxidant, anti-proliferation and induces apoptosis in various types of human cancer cells, and has protective effect on induced apoptotic damage. Areas covered The bioactivity and pharmacological Properties of α-MG are being actively investigated by various industrial and academic institutions...
March 20, 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29550915/effect-of-the-active-ingredient-of-kaempferia-parviflora-5-7-dimethoxyflavone-on-the-pharmacokinetics-of-midazolam
#5
Wataru Ochiai, Hiroko Kobayashi, Satoshi Kitaoka, Mayumi Kashiwada, Yuya Koyama, Saho Nakaishi, Tomomi Nagai, Masaki Aburada, Kiyoshi Sugiyama
5,7-Dimethoxyflavone (5,7-DMF), one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. On the other hand, in vitro studies have reported that it directly inhibits the drug metabolizing enzyme family cytochrome P450 (CYP) 3As. In this study, its safety was evaluated from a pharmacokinetic point of view, based on daily ingestion of 5,7-DMF. Midazolam, a substrate of CYP3As, was orally administered to mice treated with 5,7-DMF for 10 days, and its pharmacokinetic properties were investigated...
March 17, 2018: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29536134/conflicting-meal-recommendations-for-oral-oncology-drugs-pose-risks-to-patient-care
#6
Guo Yu, Dan-Na Wu, Yan Gong, Guo-Fu Li, Hong-Hao Zhou
PURPOSE: The labeling information, authorized by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA), is expected to guide the method of drug administration with reference to meal intake, aiming at ensuring favorable safety profile and achieving optimal drug exposure. However, interactions between meals and a specific oral anticancer medication are complicated in that could be strongly affected by inter-individual variability in pharmacokinetics, meal compositions, and the timing of drug administration with respect to meal intake, which could lead to conflicting meal recommendations between regulatory authorities...
March 13, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29533791/supragingival-and-subgingival-microbiota-from-patients-with-poor-oral-hygiene-submitted-to-radiotherapy-for-head-and-neck-cancer-treatment
#7
Elerson Gaetti-Jardim, Ellen Cristina Gaetti Jardim, Christiane Marie Schweitzer, Júlio Cesar Leite da Silva, Murilo Moura Oliveira, Danilo Chizzolini Masocatto, Cauê Monteiro Dos Santos
OBJECTIVE: This case-control study aimed to evaluate the effects of conventional radiotherapy (RT) on the prevalence and populations of oral microorganisms in head and neck cancer patients who did not receive adequate preventive dental care. It was hypothesized that side effects of radiotherapy could be associated with radiation dose, microbiological aspects, and socioeconomic conditions of the patients. DESIGN: Twenty-eight dentate patients with head and neck cancer submitted to RT were included in the study...
January 8, 2018: Archives of Oral Biology
https://www.readbyqxmd.com/read/29517103/lenvatinib-exhibits-antineoplastic-activity-in-anaplastic-thyroid-cancer-in-vitro-and-in-vivo
#8
Silvia Martina Ferrari, Guido Bocci, Teresa Di Desidero, Giusy Elia, Ilaria Ruffilli, Francesca Ragusa, Paola Orlandi, Sabrina Rosaria Paparo, Armando Patrizio, Simona Piaggi, Concettina La Motta, Salvatore Ulisse, Enke Baldini, Gabriele Materazzi, Paolo Miccoli, Alessandro Antonelli, Poupak Fallahi
Lenvatinib is an oral, multitargeted tyrosine kinase inhibitor (TKI) of VEGFR1-VEGFR3, FGFR1-FGFR4, PDGFRα, RET and v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT) signaling networks involved in tumor angiogenesis. We have evaluated the antitumor activity of lenvatinib in primary anaplastic thyroid cancer (ATC) cells, in the human cell line 8305C (undifferentiated thyroid cancer) and in an ATC-cell line (AF). The AF cell line was obtained from the primary ATC cultures and was the one that grew over 50 passages...
March 8, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29503551/developments-in-the-treatment-of-carcinoid-syndrome-impact-of-telotristat
#9
REVIEW
David L Chan, Simron Singh
Carcinoid syndrome occurs in 20% of patients with neuroendocrine tumors, and serotonin is usually the main causative hormonal peptide. Carcinoid syndrome, and particularly diarrhea, can significantly impact patients' quality of life. Somatostatin analogs (SSAs) are the mainstay of treatment, but are unable to ameliorate symptoms in all patients due to dose-limiting side effects and tachyphylaxis. Telotristat is a novel oral inhibitor of tryptophan hydroxylase, which is the rate-limiting enzyme in serotonin synthesis...
2018: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/29497292/poly-lactic-co-glycolic-acid-loaded-nanoparticles-of-betulinic-acid-for-improved-treatment-of-hepatic-cancer-characterization-in-vitro-and-in-vivo-evaluations
#10
Pranesh Kumar, Ashok K Singh, Vinit Raj, Amit Rai, Amit K Keshari, Dinesh Kumar, Biswanath Maity, Anand Prakash, Sabyasachi Maiti, Sudipta Saha
Purpose: The application of betulinic acid (B), a potent antineoplastic agent, is limited due to poor bioavailability, short plasma half-life and inappropriate tissue distribution. Thus, we aimed to prepare novel 50:50 poly(lactic- co -glycolic acid) (PLGA)-loaded B nanoparticles (BNP) and to compare its anti-hepatocellular carcinoma (HCC) activity with parent B. Methods: BNP were synthesized and characterized using different methods such as scanning electron microscopy (SEM), fourier-transform infrared (FTIR) spectrometry and particle size analyses...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29468981/lenvatinib-in-the-therapy-of-aggressive-thyroid-cancer-state-of-the-art-and-new-perspectives-with-patents-recently-applied
#11
Silvia Martina Ferrari, Ilaria Ruffilli, Marco Centanni, Camilla Virili, Gabriele Materazzi, Magdalini Alexopoulou, Mario Miccoli, Alessandro Antonelli, Poupak Fallahi
BACKGROUND AND OBJECTIVE: Lenvatinib is an oral, multitargeted tyrosine kinase inhibitor (TKI) of vascular endothelial growth factor receptors (VEGFR1-VEGFR3), fibroblast growth factor receptors (FGFR1-FGFR4), platelet-derived growth factor receptor (PDGFR)α, rearranged during transfection (RET), and v-kit (KIT) signaling networks implicated in tumor angiogenesis. METHOD: Here we review the scientific literature about lenvatinib in the treatment of thyroid cancer...
February 19, 2018: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29430197/profile-of-buparlisib-and-its-potential-in-the-treatment-of-breast-cancer-evidence-to-date
#12
REVIEW
Carmen Criscitiello, Giulia Viale, Giuseppe Curigliano, Aron Goldhirsch
Alteration of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin signaling pathway is key for the growth and survival of several cancers, including breast cancer. In addition, dysregulation of PI3K signaling may contribute to resistance to several anticancer agents. PI3K inhibitors may, therefore, be effective as antineoplastic therapy. Buparlisib is a potent and highly specific oral inhibitor of the pan-class I PI3K family. Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase signaling pathway in an ATP-competitive manner, thus inhibiting the production of the secondary messenger phosphatidylinositol (3,4,5)-trisphosphate and activation of the PI3K signaling pathway...
2018: Breast Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/29389333/targeted-cancer-therapies-oral-health-care-implications
#13
Eleni Georgakopoulou, Justin Stebbing, Crispian Scully
BACKGROUND: Targeted treatments have been incorporated into oncology protocols, often with more traditional therapies, and are not totally free of adverse reactions, some of which affect the orofacial region. METHODS: The authors searched PubMed, the Cochrane Library, and the US Food and Drug Administration Approved Drug Products database to identify reported adverse effects of targeted agents in the orofacial region as well as other implications in oral health care...
February 2018: Journal of the American Dental Association
https://www.readbyqxmd.com/read/29375014/impact-of-a-formal-pharmacist-run-oral-antineoplastic-monitoring-program-a-pilot-study-in-an-adult-genitourinary-oncology-clinic
#14
Brette Conliffe, Lindsay Figg, Padmini Moffett, Leslie Lauterwasser, Laura Beth Parsons
Background In recent years, there has been a changing paradigm in the management of oncologic disease states from the use of intravenous therapies, requiring a visit to the infusion center or hospitalization, to new therapies that can be administered orally.1,2 Several publications have evaluated the role pharmacists may play in the initial prescribing of oral chemotherapy, however the impact of a formalized pharmacist follow-up program has not been well defined. This study evaluates the impact of a pilot pharmacist-run oral antineoplastic monitoring program...
January 1, 2018: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/29372342/determination-of-flutamide-and-two-major-metabolites-using-hplc-dad-and-hptlc-methods
#15
Nada S Abdelwahab, Heba A H Elshemy, Nehal F Farid
Flutamide is a potential antineoplastic drug classified as an anti-androgen. It is a therapy for men with advanced prostate cancer, administered orally after which it undergoes extensively first pass metabolism in the liver with the production of several metabolites. These metabolites are predominantly excreted in urine. One of the important metabolites in plasma is 4-nitro-3-(trifluoromethyl)phenylamine (Flu-1), while the main metabolite in urine is 2-amino-5-nitro-4-(trifluoromethyl)phenol (Flu-3). In this work the two metabolites, Flu-1 and Flu-3, have been synthesized, and then structural confirmation has been carried out by HNMR analysis...
January 25, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29306306/use-of-oral-antineoplastic-in-special-situations-in-a-third-level-hospital-real-life-results
#16
Carmen Garcia-Muñoz, Pedro Pablo Rodriguez-Quesada, José Miguel Ferrari-Piquero
OBJECTIVE: To analyse the effectiveness and safety of oral antineoplastic drugs  (ANEOs) that are authorized in special situations in a third-level hospital and to  compare the results obtained with the clinical evidence used for this  authorization. METHOD: Descriptive observational and retrospective study. We included all  adult patients who started treatment with ANEO in special situations during the  year 2016. We collected demographic, treatment-related and clinical variables  (overall survival (OS), progression-free survival (PFS))...
January 1, 2018: Farmacia Hospitalaria
https://www.readbyqxmd.com/read/29298742/-multicentric-reticulohistiocytosis-is-a-rare-form-of-paraneoplasia
#17
Anna Maria Anderson, Tanja Todberg, Kristian Kofoed, Trine Zeeberg Iversen, Martin Andersen, Sofie Vetli Hjorth, Daniel El Fassi
A 59-year-old woman developed a rash and severe arthralgia, which primarily affected her fingers. She displayed digital arthritis and nodules on the hands, chest, face, and oral cavity. Blood samples were normal. Skin biopsies revealed histiocytic proliferation. The surface marker profile and clinical findings were consistent with multicentric reticulohistiocytosis, which may occur as a paraneoplastic phenomenon. On workup, she was diagnosed with an otherwise asymptomatic stage IVC fallopian tube cancer. She experienced little effect of prednisolone, but her condition improved on antineoplastic treatment...
January 1, 2018: Ugeskrift for Laeger
https://www.readbyqxmd.com/read/29284479/acacia-hydaspica-r-parker-prevents-doxorubicin-induced-cardiac-injury-by-attenuation-of-oxidative-stress-and-structural-cardiomyocyte-alterations-in-rats
#18
Tayyaba Afsar, Suhail Razak, Khalid Mujasam Batoo, Muhammad Rashid Khan
BACKGROUND: The use of doxorubicin (DOX) an anthracycline antineoplastic agent is withdrawn due to its cardio-toxic side effects. Oxidative stress has been recognized as the primary cause of DOX induced cardiotoxicity. We have investigated whether polyphenol rich ethyl acetate extract of Acacia hydaspica (AHE) can attenuate doxorubicin-induced cardiotoxicity via inhibition of oxidative stress. METHODS: AHE was administered orally to rats once daily for 6 weeks at doses of 200 and 400 mg/kg b...
December 29, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29197167/to-take-or-not-to-take-with-meals-unraveling-issues-related-to-food-effects-labeling-for-oral-antineoplastic-drugs
#19
Jiexin Deng, Satjit S Brar, Lawrence J Lesko
There has been controversy regarding whether bioavailability of certain oral oncology drugs should be maximized by taking these medications with food, irrespective of label instructions in the dosing and administration section. To provide insight into this controversy, we conducted an in-depth analysis for oral antineoplastic drugs approved by the Food and Drug Administration in 2000-2016 and identified important issues influencing food labeling decisions. Furthermore, a case study involving sonidegib, a drug approved for locally advanced basal cell carcinoma with a significant food effect on exposure, was used to demonstrate the consequences of failure to adhere to food label recommendations using drug-specific population pharmacokinetic and exposure-toxicity models...
December 2, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29176395/integrated-safety-summary-for-trifluridine-tipiracil-tas-102
#20
Alfredo Falcone, Atsushi Ohtsu, Eric Van Cutsem, Robert J Mayer, Michele Buscaglia, Johanna C Bendell, Scott Kopetz, Paul Bebeau, Takayuki Yoshino
Trifluridine/tipiracil, an oral treatment combining trifluridine (an antineoplastic thymidine-based nucleoside analog) and tipiracil hydrochloride (a thymidine phosphorylase inhibitor), led to significant improvement in overall survival in metastatic colorectal cancer (mCRC) patients refractory to standard therapy in the phase III RECOURSE trial. Here, we report an integrated summary of the safety of trifluridine/tipiracil. The main safety analysis includes integrated data from the RECOURSE and J003 studies (safety data group 2) of patients with refractory mCRC receiving trifluridine/tipiracil at the recommended starting dose: 35 mg/m twice daily for 5 days with 2 days' rest for 2 weeks, followed by a 14-day rest (one cycle)...
January 2018: Anti-cancer Drugs
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