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Carfilzomib

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https://www.readbyqxmd.com/read/28927064/bortezomib-carfilzomib-and-ixazomib-do-not-mediate-relevant-transporter-based-drug-drug-interactions
#1
Jannick Clemens, Lukas Welti, Julia Schäfer, Anja Seckinger, Jürgen Burhenne, Dirk Theile, Johanna Weiss
In order to optimize the clinical application of an increasing number of proteasome inhibitors, investigations into the differences between their respective pharmacodynamic and pharmacokinetic profiles, including their ability to act as a perpetrator in drug-drug interactions, are warranted. Therefore, in the present in vitro study, it was investigated whether bortezomib, carfilzomib and ixazomib are able to alter the expression, and/or the activity, of specific drug transporters generally relevant for pharmacokinetic drug-drug interactions...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28918995/cutaneous-adverse-events-of-targeted-therapies-for-hematolymphoid-malignancies
#2
REVIEW
Julia D Ransohoff, Bernice Y Kwong
The identification of oncogenic drivers of liquid tumors has led to the rapid development of targeted agents with distinct cutaneous adverse event (AE) profiles. The diagnosis and management of these skin toxicities has motivated a novel partnership between dermatologists and oncologists in developing supportive oncodermatology clinics. In this article we review the current state of knowledge of clinical presentation, mechanisms, and management of the most common and significant cutaneous AEs observed during treatment with targeted therapies for hematologic and lymphoid malignancies...
July 14, 2017: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/28918323/quantitative-determination-of-carfilzomib-in-mouse-plasma-by-liquid-chromatography-tandem-mass-spectrometry-and-its-application-to-a-pharmacokinetic-study
#3
Jee Sun Min, Jiseon Kim, Jung Ho Kim, Doyun Kim, Yu Fen Zheng, Ji Eun Park, Wooin Lee, Soo Kyung Bae
A highly sensitive and rapid LC-MS/MS method was developed and validated to determine the levels of carfilzomib in mice plasma by using chlorpropamide as an internal standard. Carfilzomib and chlorpropamide were extracted from 5 μL of plasma after protein precipitation with acetonitrile. Chromatographic separation was performed on Phenomenex Luna C18 column (50×2.0mm id, 3μm). The mobile phase consisted of 0.1% formic acid in acetonitrile -0.1% formic acid in water (1:1v/v) and the flow rate was 0.3mL/min...
September 1, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28914153/cardiotoxicity-with-carfilzomib-at-doses-greater-than-27%C3%A2-mg-m-2-a-case-series
#4
Gee Youn Kim, Tania Ahuja, John Papadopoulos, Frank Cirrone
Carfilzomib is a second-generation proteasome inhibitor that irreversibly inhibits chymotrypsin-like (CT-L) activities of the proteasome, and is indicated for relapsed or refractory multiple myeloma. Cardiotoxicity is a well-established adverse effect of carfilzomib. The extent of cardiac toxicity in the literature spans anywhere from palpitations to cardiac arrest, with the most commonly reported manifestation being new-onset or worsening heart failure. A pre-clinical study of the pharmacokinetics and pharmacodynamics of carfilzomib given via intravenous bolus or 30-minute infusion in rats showed that carfilzomib can strongly induce apoptosis and potently damage cardiac myocytes at clinically relevant concentrations...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28911826/immunoproteasome-selective-and-non-selective-inhibitors-a-promising-approach-for-the-treatment-of-multiple-myeloma
#5
REVIEW
Roberta Ettari, Maria Zappalà, Silvana Grasso, Caterina Musolino, Vanessa Innao, Alessandro Allegra
The ubiquitin-proteasome system (UPS) is the major non-lysosomal proteolytic system for the degradation of abnormal or damaged proteins no longer required. The proteasome is involved in degradation of numerous proteins which regulate the cell cycle, indicating a role in controlling cell proliferation and maintaining cell survival. Defects in the UPS can lead to anarchic cell proliferation and to tumor development. For these reasons UPS inhibition has become a significant new strategy for drug development in cancer treatment...
September 11, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28888912/chemotherapy-induces-secretion-of-exosomes-loaded-with-heparanase-that-degrades-extracellular-matrix-and-impacts-tumor-and-host-cell-behavior
#6
Shyam K Bandari, Anurag Purushothaman, Vishnu C Ramani, Garrett J Brinkley, Darshan S Chandrashekar, Sooryanarayana Varambally, James A Mobley, Yi Zhang, Elizabeth E Brown, Israel Vlodavsky, Ralph D Sanderson
The heparan sulfate-degrading enzyme heparanase promotes the progression of many cancers by driving tumor cell proliferation, metastasis and angiogenesis. Heparanase accomplishes this via multiple mechanisms including its recently described effect on enhancing biogenesis of tumor exosomes. Because we recently discovered that heparanase expression is upregulated in myeloma cells that survive chemotherapy, we were prompted to investigate the impact of anti-myeloma drugs on exosome biogenesis. When myeloma cells were exposed to the commonly utilized anti-myeloma drugs bortezomib, carfilzomib or melphalan, exosome secretion by the cells was dramatically enhanced...
September 6, 2017: Matrix Biology: Journal of the International Society for Matrix Biology
https://www.readbyqxmd.com/read/28887129/disulfiram-is-a-slow-binding-partial-noncompetitive-inhibitor-of-20s-proteasome-activity
#7
Brian B Hasinoff, Daywin Patel
The alcohol abuse drug disulfiram has also been shown to exhibit potent cell growth inhibitory and anticancer activity. While a number of cellular and animal studies have suggested that disulfiram exhibits its anticancer activity through interaction with the proteasome, direct evidence for inhibition of proteasome activity is lacking. In this study we show that disulfiram potently inhibits the chymotrypsin-like activity of purified human 20S proteasome at low micromolar pharmacological concentrations. The enzyme progress curves displayed characteristics of a slow-binding reaction, similar to that observed for the FDA-approved proteasomal-targeted anticancer drugs bortezomib and carfilzomib...
September 5, 2017: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28883286/proteasome-inhibitors-in-first-line-treatment-of-transplant-ineligible-multiple-myeloma-patients
#8
Junya Kuroda, Yuji Shimura
Since the turn of the century, many agents against multiple myeloma (MM) have been introduced into daily clinical practice. The development of further agents is ongoing and some of these will reach the point of use in clinical practice in the near future. As various treatment options become available, the selection of an appropriate treatment strategy for an individual patient becomes more important. Treatment selection and decision making are based on the following two apparently opposite factors: 1) generalized findings and evidence from clinical trials, and 2) disease risks and background of individuals, which are diverse among patients...
2017: [Rinshō Ketsueki] the Japanese Journal of Clinical Hematology
https://www.readbyqxmd.com/read/28883264/treatment-algorithms-for-multiple-myeloma-in-japan
#9
Shuji Ozaki
Recent progress in the development of novel therapeutic agents has remarkably improved the treatment outcome for multiple myeloma (MM). Proteasome inhibitors such as bortezomib, carfilzomib, and ixazomib; immunomodulatory drugs (IMiDs) such as thalidomide, lenalidomide, and pomalidomide; the histone deacetylase (HDAC) inhibitor panobinostat; and the monoclonal antibody, elotuzumab, have all been approved in Japan, although only bortezomib and lenalidomide have been approved for initial therapy. Accordingly, the Japanese Society of Hematology has released updated treatment guidelines for MM...
2017: [Rinshō Ketsueki] the Japanese Journal of Clinical Hematology
https://www.readbyqxmd.com/read/28843768/carfilzomib-or-bortezomib-in-relapsed-or-refractory-multiple-myeloma-endeavor-an-interim-overall-survival-analysis-of-an-open-label-randomised-phase-3-trial
#10
Meletios A Dimopoulos, Hartmut Goldschmidt, Ruben Niesvizky, Douglas Joshua, Wee-Joo Chng, Albert Oriol, Robert Z Orlowski, Heinz Ludwig, Thierry Facon, Roman Hajek, Katja Weisel, Vania Hungria, Leonard Minuk, Shibao Feng, Anita Zahlten-Kumeli, Amy S Kimball, Philippe Moreau
BACKGROUND: The phase 3 ENDEAVOR trial was a head-to-head comparison of two proteasome inhibitors in patients with relapsed or refractory multiple myeloma. Progression-free survival was previously reported to be significantly longer with carfilzomib administered in combination with dexamethasone than with bortezomib and dexamethasone in an interim analysis. The aim of this second interim analysis was to compare overall survival between the two treatment groups. METHODS: ENDEAVOR was a phase 3, open-label, randomised controlled trial in patients with relapsed or refractory multiple myeloma...
August 23, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28843767/carfilzomib-versus-bortezomib-no-longer-an-endeavor
#11
Niels Wcj van de Donk
No abstract text is available yet for this article.
August 23, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28841232/inhibiting-heat-shock-protein-90-and-the-ubiquitin-proteasome-pathway-impairs-metabolic-homeostasis-and-leads-to-cell-death-in-human-pancreatic-cancer-cells
#12
Astrid Belalcazar, Walid L Shaib, Matthew R Farren, Chao Zhang, Zhengjia Chen, Lily Yang, Gregory B Lesinski, Bassel F El-Rayes, Ganji Purnachandra Nagaraju
BACKGROUND: Heat shock protein 90 (HSP90) and the ubiquitin-proteasome pathway play crucial roles in the homeostasis of pancreatic cancer cells. This study combined for the first time the HSP90 inhibitor ganetespib (Gan) and the proteasome inhibitor carfilzomib (Carf) to target key mechanisms of homeostasis in pancreatic cancer. It was hypothesized that Gan plus Carf would elicit potent antitumor activity by modulating complementary homeostatic processes. METHODS: In vitro and in vivo effects of this combination on mechanisms of cell growth and viability were evaluated with human pancreatic cancer cell lines (MIA PaCa-2 and HPAC)...
August 25, 2017: Cancer
https://www.readbyqxmd.com/read/28828905/the-activity-and-safety-of-novel-proteasome-inhibitors-strategies-single-doublet-and-triplet-for-relapsed-refractory-multiple-myeloma
#13
Huanwen Ma, Zheng Su, Fengqiang Sun, Ningning Zhao
PURPOSE: We sought to evaluate the activity and safety of these novel proteasome inhibitors (PIs) (carfilzomib, ixazomib, oprozomib and marizomib) containing regimens (single, doublet and triplet) for relapsed/refractory multiple myeloma (R/RMM). METHODS: We searched published reports including these novel PIs containing regimens for R/RMM. RESULTS: Finally, we identified 28 prospective studies that evaluated 4123 patients. Pooled analysis showed that novel PIs doublet combinations attained an impressive overall response rate (ORR) of 67%, which was higher than that of 22% from novel PIs single-agent (p < ...
August 22, 2017: Acta Oncologica
https://www.readbyqxmd.com/read/28819709/use-of-direct-oral-anticoagulants-in-patients-on-immunomodulatory-agents
#14
L Man, A Morris, J Brown, S Palkimas, K Davidson
Immunomodulatory agents (IMiDs) are used to treat multiple hematologic malignancies. Their use is also associated with increased risk of venous thromboembolism (VTE). Direct oral anticoagulants (DOACs) have been increasingly utilized but due to their relative novelty, their role in malignancy has only been recently investigated. The objective of this study was to assess the safety and efficacy of DOACs in patients receiving IMiDs. This was a retrospective study of patients at our institution treated with an IMiD and concomitant warfarin or DOAC between January 1, 2010 and December 31, 2015...
August 17, 2017: Journal of Thrombosis and Thrombolysis
https://www.readbyqxmd.com/read/28781837/carfilzomib-and-dexamethasone-for-extramedullary-myeloma-with-pleuropericardial-involvement
#15
Ignacio Español, Marta Romera, María Dolores Gutiérrez-Meca, Maria Del Carmen García, Aurelia Tejedor, Antonio Martínez, Jerónima Ibáñez, Felipe De Arriba, Alfredo Minguela, Teodoro Iturbe, Maria Dolores López
The dismal outcome of pleuropericardial extramedullary multiple myeloma (EMM) reflects both the selection of resistant disease and absence of useful drugs. Carfilzomib and dexamethasone should be explored in advanced EMM patients, even for bortezomib-resistant patients, as may provide much longer overall survival than previously reported treatments.
August 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/28763310/elderly-patients-with-multiple-myeloma-towards-a-frailty-approach
#16
REVIEW
Sonja Zweegman, Monika Engelhardt, Alessandra Larocca
PURPOSE OF REVIEW: To describe how to better identify frail multiple myeloma patients and to treat them appropriately. RECENT FINDINGS: Proteasome inhibitors, such as bortezomib, carfilzomib, and ixazomib, and immunomodulatory agents (IMiDs), such as thalidomide, lenalidomide, and pomalidomide, have significantly improved the outcome of multiple myeloma patients in the last decade. However, both in clinical trials and in daily clinical practice, elderly multiple myeloma patients have shown lesser benefit...
September 2017: Current Opinion in Oncology
https://www.readbyqxmd.com/read/28760601/a-functional-drug-re-purposing-screening-identifies-carfilzomib-as-a-drug-preventing-17%C3%AE-estradiol-er%C3%AE-signaling-and-cell-proliferation-in-breast-cancer-cells
#17
Claudia Busonero, Stefano Leone, Cinzia Klemm, Filippo Acconcia
Most cases of breast cancer (BC) are estrogen receptor α-positive (ERα+) at diagnosis. The presence of ERα drives the therapeutic approach for this disease, which often consists of endocrine therapy (ET). 4OH-Tamoxifen and faslodex (i.e., fulvestrant - ICI182,780) are two ETs that render tumor cells insensitive to 17β-estradiol (E2)-dependent proliferative stimuli and prevent BC progression. However, ET has limitations and serious failures in different tissues and organs. Thus, there is an urgent need to identify novel drugs to fight BC in the clinic...
July 29, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28747580/emerging-drugs-and-combinations-to-treat-multiple-myeloma
#18
REVIEW
Alessandra Larocca, Roberto Mina, Francesca Gay, Sara Bringhen, Mario Boccadoro
In the past few years, multiple targeted therapies and immunotherapies including second generation immunomodulatory drugs (pomalidomide) and proteasome inhibitors (carfilzomib, ixazomib), monoclonal antibodies and checkpoint inhibitors were approved for the treatment of myeloma or entered advanced phases of clinical testing. These agents showed significant activity in advanced myeloma and increased the available treatment strategies.Pomalidomide is well-tolerated and effective in patients with relapsed/refractory multiple myeloma who have exhausted any possible treatment with lenalidomide and bortezomib...
July 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28747306/how-i-treat-new-agents-in-myeloma
#19
Philippe Moreau
At present, multiple classes of agents with distinct mechanisms of action are available for the treatment of patients with multiple myeloma (MM), including alkylators, steroids, immunomodulatory agents (IMiDs), proteasome inhibitors (PIs), histone deacetylase inhibitors (DACIs) and monoclonal antibodies (mAbs). Over the last 5 years, several new agents, such as the third-generation IMiD pomalidomide, the second generation PIs carfilzomib and ixazomib, the DACI panobinostat and two monoclonal antibodies, elotuzumab and daratumumab, have been approved, incorporated into clinical guidelines and have transformed our approach to the treatment of patients...
July 26, 2017: Blood
https://www.readbyqxmd.com/read/28723635/meta-analysis-of-the-efficacy-of-treatments-for-newly-diagnosed-and-relapsed-refractory-multiple-myeloma-with-del-17p
#20
Jinghua Liu, Hui Yang, Xiaochan Liang, Yuxin Wang, Jian Hou, Yanqin Liu, Jigang Wang, Fan Zhou
We analyzed the treatment of newly diagnosed and relapsed/refractory multiple myeloma (NDMM/RRMM) patients with del(17p). Thirteen prospective studies that evaluated 3,187 MM patients, including 685with del(17p), were included in our meta-analysis. The incidence of del(17p) in NDMM and RRMM patients was similar (13% vs. 14%, respectively, P = 0.64, I2 = 94%). The overall response rate (ORR) to new agents was 40.5% and 67.1%, respectively, in RRMM patients with or without del(17p) (P = 0.1, I2 = 63.9%). NDMM patients with del(17p) treated with PAD (bortezomib, adriamycin, and dexamethasone) induction therapy followed by bortezomib maintenance therapy had higher progression-free survival (PFS) (25...
June 27, 2017: Oncotarget
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