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https://www.readbyqxmd.com/read/28103612/a-phase-iii-randomised-controlled-trial-of-erlotinib-vs-gefitinib-in-advanced-non-small-cell-lung-cancer-with-egfr-mutations
#1
J J Yang, Q Zhou, H H Yan, X C Zhang, H J Chen, H Y Tu, Z Wang, C R Xu, J Su, B C Wang, B Y Jiang, X Y Bai, W Z Zhong, X N Yang, Y L Wu
BACKGROUND: A phase III trial was conducted to compare the safety and efficacy of erlotinib with that of gefitinib in advanced non-small cell lung cancer harbouring epidermal growth factor receptor mutations in exon 19 or 21. METHODS: Eligible patients were randomised to receive erlotinib (150 mg per day) or gefitinib (250 mg per day) orally until disease progression or unacceptable toxicity. We aimed to determine whether erlotinib is superior to gefitinib in efficacy...
January 19, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28103611/phase-ii-randomised-discontinuation-trial-of-the-met-vegf-receptor-inhibitor-cabozantinib-in-metastatic-melanoma
#2
Adil Daud, Harriet M Kluger, Razelle Kurzrock, Frauke Schimmoller, Aaron L Weitzman, Thomas A Samuel, Ali H Moussa, Michael S Gordon, Geoffrey I Shapiro
BACKGROUND: A phase II randomised discontinuation trial assessed cabozantinib (XL184), an orally bioavailable inhibitor of tyrosine kinases including VEGF receptors, MET, and AXL, in a cohort of patients with metastatic melanoma. METHODS: Patients received cabozantinib 100 mg daily during a 12-week lead-in. Patients with stable disease (SD) per Response Evaluation Criteria in Solid Tumours (RECIST) at week 12 were randomised to cabozantinib or placebo. Primary endpoints were objective response rate (ORR) at week 12 and postrandomisation progression-free survival (PFS)...
January 19, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28103302/crude-extracts-flavokawain-b-and-alpinetin-compounds-from-the-rhizome-of-alpinia-mutica-induce-cell-death-via-uck2-enzyme-inhibition-and-in-turn-reduce-18s-rrna-biosynthesis-in-ht-29-cells
#3
Ibrahim Malami, Ahmad Bustamam Abdul, Rasedee Abdullah, Nur Kartinee Bt Kassim, Rozita Rosli, Swee Keong Yeap, Peter Waziri, Imaobong Christopher Etti, Muhammad Bashir Bello
Uridine-cytidine kinase 2 is an enzyme that is overexpressed in abnormal cell growth and its implication is considered a hallmark of cancer. Due to the selective expression of UCK2 in cancer cells, a selective inhibition of this key enzyme necessitates the discovery of its potential inhibitors for cancer chemotherapy. The present study was carried out to demonstrate the potentials of natural phytochemicals from the rhizome of Alpinia mutica to inhibit UCK2 useful for colorectal cancer. Here, we employed the used of in vitro to investigate the effectiveness of natural UCK2 inhibitors to cause HT-29 cell death...
2017: PloS One
https://www.readbyqxmd.com/read/28103177/hbxip-a-binding-protein-of-hbx-regulates-maintenance-of-the-g2-m-phase-checkpoint-induced-by-dna-damage-and-enhances-sensitivity-to-doxorubicin-induced-cytotoxicity
#4
Hong-Rong Fei, Yun-Sheng Zhou, Ruo-Tong Li, Ming-Feng Yang, Jian Ma, Feng-Ze Wang
To maintain the integrity of the genome, cells need to detect and repair DNA damage before they complete cell division. Hepatitis B x-interacting protein (HBXIP), a binding protein of HBx (Hepatitis B virus x protein), is aberrantly overexpressed in human cancer cells and show to promote cell proliferation and inhibit apoptosis. The present study is designed to investigate the role of HBXIP on the DNA damage response. Our results show that HBXIP acts as an important regulator of G2/M checkpoint in response to DNA damage...
January 19, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28102887/clinical-trial-of-nintedanib-in-patients-with-recurrent-or-metastatic-salivary-gland-cancer-of-the-head-and-neck-a-multicenter-phase-2-study-korean-cancer-study-group-hn14-01
#5
Youjin Kim, Su Jin Lee, Ji Yun Lee, Se-Hoon Lee, Jong-Mu Sun, Keunchil Park, Ho Jung An, Jae Yong Cho, Eun Joo Kang, Ha-Young Lee, Jinsoo Kim, Bhumsuk Keam, Hye Ryun Kim, Kyoung Eun Lee, Moon Young Choi, Ki Hyeong Lee, Myung-Ju Ahn
BACKGROUND: Salivary gland cancers (SGCs) are uncommon and account for less than 5% of all head and neck cancers, but they are histologically heterogeneous. No specific therapy, including targeted agents, has consistently improved clinical outcomes in recurrent/metastatic SGC. Recent studies suggest that vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) play important roles in SGC. Nintedanib is a potent small-molecule, triple-receptor tyrosine kinase inhibitor (VEGFR1, VEGFR2, and VEGFR3; fibroblast growth factor receptor 1 [FGFR1], FGFR2, and FGFR3; and PDGFRα and PDGFRß)...
January 19, 2017: Cancer
https://www.readbyqxmd.com/read/28102676/novel-antitumor-platinum-ii-conjugates-containing-the-nonsteroidal-anti-inflammatory-agent-diclofenac-synthesis-and-dual-mechanisms-of-antiproliferative-effects
#6
Francesco Paolo Intini, Juraj Zajac, Vojtech Novohradsky, Teresa Saltarella, Concetta Pacifico, Viktor Brabec, Giovanni Natile, Jana Kasparkova
One concept how to improve anticancer effects of conventional metallodrugs consists in conjugation of these compounds with other biologically (antitumor) active agents, acting by a different mechanism. Here, we present synthesis, biological effects, and mechanisms of action of new Pt(II) derivatives containing one or two nonsteroidal anti-inflammatory diclofenac (DCF) ligands also known for their antitumor effects. The antiproliferative properties of these metallic conjugates show that these compounds are potent and cancer cell selective cytotoxic agents exhibiting activity in cisplatin resistant and the COX-2 positive tumor cell lines...
January 19, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28102464/a-phase-i-and-pharmacokinetic-study-of-afilbercept-with-folfiri-comparison-of-chinese-and-caucasian-populations
#7
Jianming Xu, Yingxin Li, Xing Sun, Dongsheng Zhang, Rongrui Liu, Samira Ziti-Ljajic, Dongmei Shi, Fengying Xue, Nathalie Le Bail, Ruihua Xu
Background This study assessed the preliminary safety, pharmacokinetics (PK) and anti-tumor effects of aflibercept in combination with 5-fluorouracil, leucovorin and irinotecan (FOLFIRI) in Chinese patients with previously-treated advanced solid malignancies. Patients and Methods This open-label single-arm Phase I study conducted at two centers in China included adult (≥18 years) patients with metastatic or unresectable solid malignancies who had received ≥1 prior treatment. Patients received aflibercept 4 mg/kg IV on Day 1 followed by FOLFIRI over Days 1 and 2 every 2 weeks, and were assessed for safety, tumor response, PK parameters and immunogenicity...
January 19, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28102324/antiproliferative-and-apoptosis-inducing-effect-of-exo-protoporphyrin-ix-based-sonodynamic-therapy-on-human-oral-squamous-cell-carcinoma
#8
Yanhong Lv, Jinhua Zheng, Qi Zhou, Limin Jia, Chunying Wang, Nian Liu, Hong Zhao, Hang Ji, Baoxin Li, Wenwu Cao
Sonodynamic therapy (SDT) is an innovative modality for cancer treatment. But the biological effect of SDT on oral squamous cell carcinoma has not been studied. Our previous study has shown that endo-Protoporphyrin IX based SDT (ALA-SDT) could induce apoptosis in human tongue squamous carcinoma SAS cells through mitochondrial pathway. Herein, we investigated the effect of exo- Protoporphyrin based SDT (PpIX-SDT) on SAS cells in vitro and in vivo. We demonstrated that PpIX-SDT increased the ratio of cells in the G2/M phase and induced 3-4 times more cell apoptosis compared to sonocation alone...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28101887/abiraterone-or-enzalutamide-in-advanced-castration-resistant-prostate-cancer-an-indirect-comparison
#9
Akhil Chopra, Mina Georgieva, Gilberto Lopes, Chong Ming Yeo, Benjamin Haaland
BACKGROUND: To perform a comparative effectiveness analyses between enzalutamide and abiraterone acetate in both the pre-docetaxel and post-docetaxel settings based on published phase III randomized trials. METHODS: The primary measure of efficacy was the posterior probability that enzalutamide outperforms abiraterone acetate (AA) with prednisone in terms of overall survival (OS) on average. Indirect meta-estimates were generated from four randomized studies in the context of a Bayesian hierarchical model with study-specific efficacy estimates meta-analyzed on the log scale...
January 19, 2017: Prostate
https://www.readbyqxmd.com/read/28101350/tp53-mutation-is-associated-with-a-poor-clinical-outcome-for-non-small-cell-lung-cancer-evidence-from-a-meta-analysis
#10
Jincui Gu, Yanbin Zhou, Lixia Huang, Weijun Ou, Jian Wu, Shaoli Li, Junwen Xu, Jinlun Feng, Baomo Liu
A number of studies have examined the association between tumor protein 53 (TP53) mutations and the clinical outcome in patients with non-small-cell lung cancer (NSCLC), although these have yielded conflicting results. In the present study, electronic databases updated to September 2015 were searched to find relevant studies. A meta-analysis was performed on the eligible studies, which quantitatively evaluated the association between the TP53 mutations and the survival of patients with NSCLC. Subgroup and sensitivity analyses were performed...
December 2016: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28101220/antitumor-effect-of-forbesione-isolated-from-garcinia-hanburyi-on-cholangiocarcinoma-in-vitro-and-in-vivo
#11
Parichart Boueroy, Chariya Hahnvajanawong, Thidarut Boonmars, Sunitta Saensa-Ard, Natthinee Anantachoke, Kulthida Vaeteewoottacharn, Vichai Reutrakul
Cholangiocarcinoma (CCA) is a malignancy with no effective therapy and poor prognosis. Forbesione, a caged xanthone isolated from Garcinia hanburyi, has been reported to inhibit proliferation and to induce apoptosis in human CCA cell lines. The present study aimed to further explore the potential anticancer properties of forbesione by testing its effects against the hamster CCA cell line Ham-1 in vitro and in vivo. It was observed that forbesione inhibited the growth of Ham-1 cells in vitro and suppressed Ham-1 growth as allograft in hamsters by inducing cell cycle arrest at the S phase...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28101215/rottlerin-induced-autophagy-leads-to-apoptosis-in-bladder-cancer-cells
#12
Ping Qi, Zhenhua He, Lixiu Zhang, Yuan Fan, Zhiping Wang
It has been well-established that apoptosis contributes to cancer cell death; however, the role of autophagy in cancer cell death remains unclear. The aim of the present study was to investigate the effects of rottlerin, a traditional Indian medicine, on cell growth inhibition and autophagy in EJ human bladder carcinoma cells in vitro. Cell viability, measured by MTT assay, was found to be suppressed in a dose- and time-dependent manner. In addition, apoptosis was significantly increased in cells treated with rottlerin, as indicated by increased annexin V-fluorescein isothiocyanate/propidium iodide staining and changes in the cell cycle distribution that indicated blockage at G1 phase...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28100988/simultaneous-analyses-of-n-linked-and-o-linked-glycans-of-ovarian-cancer-cells-using-solid-phase-chemoenzymatic-method
#13
Shuang Yang, Naseruddin Höti, Weiming Yang, Yang Liu, Lijun Chen, Shuwei Li, Hui Zhang
BACKGROUND: Glycans play critical roles in a number of biological activities. Two common types of glycans, N-linked and O-linked, have been extensively analyzed in the last decades. N-glycans are typically released from glycoproteins by enzymes, while O-glycans are released from glycoproteins by chemical methods. It is important to identify and quantify both N- and O-linked glycans of glycoproteins to determine the changes of glycans. METHODS: The effort has been dedicated to study glycans from ovarian cancer cells treated with O-linked glycosylation inhibitor qualitatively and quantitatively...
2017: Clinical Proteomics
https://www.readbyqxmd.com/read/28100868/growth-inhibition-of-refractory-human-gallbladder-cancer-cells-by-retinol-and-its-mechanism-of-action
#14
Chuan Li, Masahiko Imai, Shinya Hasegawa, Masahiro Yamasaki, Noriko Takahashi
Among the constituents of the essential nutrient vitamin A, retinol is a potent suppressor of refractory cancer cell growth linked to tumor progression, showing greater efficacy than retinoic acid (RA). However, the mechanisms of retinol action on human refractory cancer are not known well. In the current study, we examined the actions of retinol on proliferation of human gallbladder cancer NOZ C-1 cells. Retinol and RA inhibited the proliferation of human NOZ C-1 cells in dose-dependent manner, while RA was less potent than retinol...
January 18, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28098885/carboxamide-analog-itr-284-evokes-apoptosis-and-inhibits-migration-ability-in-human-lung-adenocarcinoma-a549-cells
#15
Jai-Sing Yang, Chia-An Lin, Chi-Cheng Lu, Yen-Fang Wen, Fuu-Jen Tsai, Shih-Chang Tsai
Lung adenocarcinoma is the most common type of lung cancer and found in both smokers and non-smokers, but the treatment of lung cancer is limited. ITR-284 has been shown to be a potent carboxamide-derived anticancer agent and to induce apoptosis in leukemia and colon cancer cells. However, little is known whether ITR-284 has anticancer activity in human lung adenocarcinoma cells through induction of apoptosis and suppression of migration in vitro. We showed that ITR-284 inhibited human lung cancer A549 cells using the thiazolyl blue tetrazolium bromide (MTT) assay and evoked apoptosis via the cell cycle distribution at S phase arrest...
January 16, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28098872/trim29-promotes-progression-of-thyroid-carcinoma-via-activating-p13k-akt-signaling-pathway
#16
Jinkai Xu, Zongyu Li, Qinghua Su, Jun Zhao, Jiancang Ma
Thyroid cancer (TC) is a common malignancy of the endocrine system. Abnormal expression of tripartite motif-containing 29 (TRIM29) has been reported to promote tumorigenesis and predict poor prognosis in several human malignancies. The aim of this study was to assess the involvement of TRIM29 in the significance and prognosis of TC. Fifty-six tumor samples and their clinicopathological para-meters were obtained from TC patients; the expression level of TRIM29 was detected by RT-qPCR and western blotting. TRIM29 expression was knocked down by small interfering RNA (siRNA) among TT, TPC-1, and K1 cells to investigate the biological role of TRIM29 in TC cells...
January 13, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28098860/chondroitin-sulfate-proteoglycan-protein-is-stimulated-by-interleukin%C3%A2-11-and-promotes-endometrial-epithelial-cancer-cell-proliferation-and-migration
#17
Amy Winship, Michelle Van Sinderen, Ariella Heffernan-Marks, Eva Dimitriadis
Endometrial cancer is the most common gynecological cancer. We identified interleukin 11 (IL11) as a critical mediator of endometrial tumourigenesis and demonstrated that IL11 regulates chondroitin sulfate proteoglycan (CSPG4) in human placental trophoblasts. CSPG4 is a cell membrane protein overexpressed in numerous human cancers, although its role in endometrial cancer has not been investigated. We examined CSPG4 expression and localization in primary human type I endometrioid grade (G) 1-3 tumours by qPCR and immunohistochemistry and determined whether IL11 stimulated CSPG4...
January 13, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28097641/natural-products-diversity-of-marine-ascidians-tunicates-ascidiacea-and-successful-drugs-in-clinical-development
#18
REVIEW
Satheesh Kumar Palanisamy, N M Rajendran, Angela Marino
This present study reviewed the chemical diversity of marine ascidians and their pharmacological applications, challenges and recent developments in marine drug discovery reported during 1994-2014, highlighting the structural activity of compounds produced by these specimens. Till date only 5% of living ascidian species were studied from <3000 species, this study represented from family didemnidae (32%), polyclinidae (22%), styelidae and polycitoridae (11-12%) exhibiting the highest number of promising MNPs...
January 17, 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/28097385/two-phase-1-dose-escalation-studies-exploring-multiple-regimens-of-litronesib-ly2523355-an-eg5-inhibitor-in-patients-with-advanced-cancer
#19
Jeffrey R Infante, Amita Patnaik, Claire F Verschraegen, Anthony J Olszanski, Montaser Shaheen, Howard A Burris, Anthony W Tolcher, Kyriakos P Papadopoulos, Muralidhar Beeram, Scott M Hynes, Jennifer Leohr, Aimee Bence Lin, Lily Q Li, Anna McGlothlin, Daphne L Farrington, Eric H Westin, Roger B Cohen
PURPOSE: This first-in-human report examined the recommended Phase 2 dose and schedule of litronesib, a selective allosteric kinesin Eg5 inhibitor. METHODS: Two concurrent dose-escalation studies investigated litronesib across the dose range of 0.125-16 mg/m(2)/day, evaluating the following schedules of administration on a 21-day cycle: Days 1, 2, 3; Days 1, 5, 9; Days 1, 8; Days 1, 5; or Days 1, 4, with or without pegfilgrastim. Best overall response was defined per Response Evaluation Criteria in Solid Tumors (RECIST Version 1...
January 17, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28096932/contemporary-agents-in-the-management-of-metastatic-castration-resistant-prostate-cancer
#20
REVIEW
Anil Kapoor, Christopher Wu, Bobby Shayegan, Adrian P Rybak
Docetaxel-based chemotherapy has been the standard of care for metastatic castration-resistant prostate cancer (mCRPC) since 2004. Over the past few years, there has been a significant paradigm shift in the treatment landscape of this disease. A deeper understanding of prostate cancer biology, along with the development of novel agents has created hope towards treating chemotherapy-naïve and resistant disease. Following the implementation of docetaxel as the first-line therapy for mCRPC, five novel therapies have demonstrated survival benefit in mCRPC...
November 2016: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
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