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Imbruvica

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https://www.readbyqxmd.com/read/27854034/efficient-preparation-of-s-n-boc-3-hydroxylpiperidine-through-bioreduction-by-a-thermostable-aldo-ketoreductase
#1
Mengyan He, Shuo Zhou, Maolin Cui, Xiaolu Jin, Dunyue Lai, Shuangling Zhang, Zhiguo Wang, Zhenming Chen
(S)-N-Boc-3-hydroxypiperidine ((S)-NBHP) is a key pharmaceutical intermediate and the chiral source in synthesizing Imbruvica, which is a newly approved drug in lymphoma therapy by targeting Bruton's tyrosine kinase (BTK). Current chemical synthesis of (S)-NBHP suffered from the need of noble metal catalyst and low yield. The single reported bioconversion of (S)-NBHP was achieved by using recombinant ketoreductase, but enzyme sequence was kept confidential and the catalytic process suffered from the thermodeactivation and substrate inhibition...
November 16, 2016: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/27668052/imbruvica-ibrutinib-first-drug-approved-for-the-treatment-of-patients-with-waldenstr%C3%A3-m-s-macroglobulinemia
#2
Lisa A Raedler
No abstract text is available yet for this article.
March 2016: American Health & Drug Benefits
https://www.readbyqxmd.com/read/27231694/spontaneous-iliopsoas-muscle-hemorrhage-secondary-to-ibrutinib-imbruvica-pharmacyclics-brief-report
#3
Anna Sarcon, Gregory P Botta, Nikunj Patel, Alan Saven
Ibrutinib (Imbruvica; Pharmacyclics) is the first Food and Drug Administration-approved inhibitor of Burton's tyrosine kinase (BTK). Attenuation of BTK signaling ultimately leads to inhibition of B-cell proliferation and apoptosis. After a series of clinical trials, the Food and Drug Administration approved ibrutinib in patients with relapsed chronic lymphocytic leukemia in 2014 and Waldenström's macroglobulinemia in 2015. Those trials included rare grade 3+ hemorrhagic events associated with ibrutinib. Herein, we report a unique presentation of back pain due to iliopsoas muscle hemorrhage in a patient with Waldenström's macroglobulinemia after initiation of ibrutinib...
April 2016: Journal of Investigative Medicine High Impact Case Reports
https://www.readbyqxmd.com/read/27183765/ibrutinib-imbruvica-relapsed-chronic-lymphocytic-leukaemia-and-mantle-cell-lymphoma-uncertain-impact-on-survival
#4
REVIEW
January
codynamic interactions are also likely in view of its adverse effect profile. There is no consensus on the treatment of patients with refractory or relapsed mantle cell lymphoma, or for patients with relapsed or possibly refractory chronic lymphocytic leukaemia. Ibrutinib inhibits an enzyme involved in regulating B lymphocyte activity. It has been authorised in the European Union for these conditions. Clinical evaluation of ibrutinib in mantle cell lymphoma is based on a single non-comparative trial in 111 patients, in which the median overall survival time was 22...
April 2016: Prescrire International
https://www.readbyqxmd.com/read/26629268/imbruvica-ibrutinib-first-in-class-bruton-s-tyrosine-kinase-inhibitor-receives-expanded-indications-for-patients-with-relapsed-chronic-lymphocytic-leukemia
#5
Lisa A Raedler
No abstract text is available yet for this article.
March 2015: American Health & Drug Benefits
https://www.readbyqxmd.com/read/26275952/fda-approval-ibrutinib-for-patients-with-previously-treated-mantle-cell-lymphoma-and-previously-treated-chronic-lymphocytic-leukemia
#6
MULTICENTER STUDY
R Angelo de Claro, Karen M McGinn, Nicole Verdun, Shwu-Luan Lee, Haw-Jyh Chiu, Haleh Saber, Margaret E Brower, C J George Chang, Elimika Pfuma, Bahru Habtemariam, Julie Bullock, Yun Wang, Lei Nie, Xiao-Hong Chen, Donghao Robert Lu, Ali Al-Hakim, Robert C Kane, Edvardas Kaminskas, Robert Justice, Ann T Farrell, Richard Pazdur
On November 13, 2013, the FDA granted accelerated approval to ibrutinib (IMBRUVICA capsules; Pharmacyclics, Inc.) for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy. On February 12, 2014, the FDA granted accelerated approval for the treatment of patients with chronic lymphocytic leukemia (CLL) who have received at least one prior therapy. Ibrutinib is a first-in-class Bruton's tyrosine kinase (BTK) inhibitor that received all four expedited programs of the FDA: Fast-Track designation, Breakthrough Therapy designation, Priority Review, and Accelerated Approval...
August 15, 2015: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/26118882/-ibrutinib-a-new-drug-of-b-cell-malignancies
#7
REVIEW
Catherine Thieblemont
Ibrutinib (Imbruvica®) is a first-in-class, orally administered once-daily, that inhibits B-cell antigen receptor signaling downstream of Bruton's tyrosine kinase (BTK). Ibrutinib has been approved in USA in February 2014 and in France in October 2014 for the treatment of patients with relapsed/refractory mantle cell lymphoma (MCL) or chronic lymphocytic leukaemia (CLL) and for the treatment of patients with CLL and a chromosome 17 deletion (del 17p) or TP53 mutation. In clinical studies, ibrutinib induced an impressive overall response rate (68%) in patients with relapsed/refractory MCL (phase II study)...
June 2015: Bulletin du Cancer
https://www.readbyqxmd.com/read/26111359/targets-for-ibrutinib-beyond-b-cell-malignancies
#8
REVIEW
A Berglöf, A Hamasy, S Meinke, M Palma, A Krstic, R Månsson, E Kimby, A Österborg, C I E Smith
Ibrutinib (Imbruvica™) is an irreversible, potent inhibitor of Bruton's tyrosine kinase (BTK). Over the last few years, ibrutinib has developed from a promising drug candidate to being approved by FDA for the treatment of three B cell malignancies, a truly remarkable feat. Few, if any medicines are monospecific and ibrutinib is no exception; already during ibrutinib's initial characterization, it was found that it could bind also to other kinases. In this review, we discuss the implications of such interactions, which go beyond the selective effect on BTK in B cell malignancies...
September 2015: Scandinavian Journal of Immunology
https://www.readbyqxmd.com/read/25802231/ibrutinib-a-review-of-its-use-in-patients-with-mantle-cell-lymphoma-or-chronic-lymphocytic-leukaemia
#9
REVIEW
Esther S Kim, Sohita Dhillon
Ibrutinib (Imbruvica®) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK. Oral ibrutinib is indicated for the treatment of patients with relapsed/refractory mantle cell lymphoma (MCL) or chronic lymphocytic leukaemia (CLL) and for the treatment of patients with CLL and a chromosome 17 deletion (del 17p) or TP53 mutation. This article summarizes pharmacological, efficacy and tolerability data relevant to the use of ibrutinib in these indications...
May 2015: Drugs
https://www.readbyqxmd.com/read/25589346/bruton-tyrosine-kinase-is-a-therapeutic-target-in-stem-like-cells-from-multiple-myeloma
#10
Ye Yang, Jumei Shi, Zhimin Gu, Mohamed E Salama, Satyabrata Das, Erik Wendlandt, Hongwei Xu, Junwei Huang, Yi Tao, Mu Hao, Reinaldo Franqui, Dana Levasseur, Siegfried Janz, Guido Tricot, Fenghuang Zhan
Ibrutinib (Imbruvica), a small-drug inhibitor of Bruton tyrosine kinase (BTK), is currently undergoing clinical testing in patients with multiple myeloma, yet important questions on the role of BTK in myeloma biology and treatment are outstanding. Using flow-sorted side population cells from human myeloma cell lines and multiple myeloma primary samples as surrogate for the elusive multiple myeloma stem cell, we found that elevated expression of BTK in myeloma cells leads to AKT/WNT/β-catenin-dependent upregulation of key stemness genes (OCT4, SOX2, NANOG, and MYC) and enhanced self-renewal...
February 1, 2015: Cancer Research
https://www.readbyqxmd.com/read/25477591/decimal-commas-are-a-problem-actiq-is-not-for-sore-throats-dosing-error-with-tasigna-repackaging-of-imbruvica-is-approved
#11
Michael R Cohen, Judy L Smetzer
These medication errors have occurred in health care facilities at least once. They will happen again-perhaps where you work. Through education and alertness of personnel and procedural safeguards, they can be avoided. You should consider publishing accounts of errors in your newsletters and/or presenting them at your inservice training programs. Your assistance is required to continue this feature. The reports described here were received through the Institute for Safe Medication Practices (ISMP) Medication Errors Reporting Program...
September 2014: Hospital Pharmacy
https://www.readbyqxmd.com/read/25407369/small-molecule-inhibitors-of-spleen-tyrosine-kinase-as-therapeutic-agents-for-immune-disorders-will-promise-meet-expectations
#12
REVIEW
Matthew C Lucas, Seng-Lai Tan
Following on the heels of the US FDA approval of tofacitinib (Xeljanz, Pfizer, USA), an inhibitor of the JAK family members, and ibrutinib (Imbruvica, Janssen, Belgium), an inhibitor of BTK, for the treatment of rheumatoid arthritis and chronic lymphocytic leukemia, respectively, there is now renewed interest in the biopharmaceutical industry in the development of orally active small-molecule agents targeting key protein kinases implicated in immune regulation. One such 'immunokinase' target is SYK, a non-receptor tyrosine protein kinase critical for transducing intracellular signaling cascades for various immune recognition receptors, such as the B-cell receptor and the Fc receptor...
2014: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/25101331/spotlight-on-chronic-lymphocytic-leukemia-a-pharma-matters-report
#13
REVIEW
P D'Souza, G Walker
A paradigm shift in the treatment of chronic lymphocytic leukemia (CLL) has taken place over the past decade, as therapies have progressed from providing palliative relief to inducing complete remission, eradicating minimal disease and improving survival. The development of Rituxan® (rituximab) and its use in immunochemotherapy regimens has transformed the treatment of CLL and is the current gold standard in physically fit individuals aged < 65 years. Despite this therapeutic development, Rituxan-based immunochemotherapy is limited in the two CLL groups that form the majority of CLL cases-the elderly and patients with comorbidities and high risk factors...
July 2014: Drugs of Today
https://www.readbyqxmd.com/read/25083126/ibrutinib-imbruvica-a-novel-targeted-therapy-for-chronic-lymphocytic-leukemia
#14
Sapna Parmar, Khilna Patel, Javier Pinilla-Ibarz
Ibrutinib (Imbruvica): a novel targeted therapy for chronic lymphocytic leukemia.
July 2014: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/25081321/ibrutinib-imbruvicatm-potently-inhibits-erbb-receptor-phosphorylation-and-cell-viability-of-erbb2-positive-breast-cancer-cells
#15
Nicole Grabinski, Florian Ewald
Ibrutinib (formerly PCI-32765) is a specific, irreversible, and potent inhibitor of Burton's tyrosine kinase (BTK) developed for the treatment of several forms of blood cancer. It is now an FDA-approved drug marketed under the name Imbruvica(TM) (Pharmacyclics, Inc.) and successfully used as an orally administered second-line drug in the treatment of mantle cell lymphoma. Since BTK is predominantly expressed in hematopoietic cells, the sensitivity of solid tumor cells to Ibrutinib has not been analyzed. In this study, we determined the effect of Ibrutinib on breast cancer cells...
December 2014: Investigational New Drugs
https://www.readbyqxmd.com/read/24757362/pharmaceutical-approval-update
#16
Marvin M Goldenberg
Ibrutinib (Imbruvica) for chronic lymphocytic leukemia, tasimelteon (Hetlioz) for non-24-hour sleep-wake disorder, and anti-inhibitor coagulant complex (Feiba) to prevent or reduce bleeding in hemophilia A or B.
April 2014: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/24749490/breaking-good-the-inexorable-rise-of-btk-inhibitors-in-the-treatment-of-chronic-lymphocytic-leukaemia
#17
REVIEW
Claire V Hutchinson, Martin J S Dyer
Although expressed in several haematological lineages and involved in multiple different signalling pathways, Bruton tyrosine kinase (BTK) plays an indispensible role in B cells in signalling from the B cell receptor (BCR) for antigen. Many B cell malignancies remain dependent on constitutive BCR signalling, making BTK a functional therapeutic target. Several BTK inhibitors (BTKi) with different kinomes and modes of action are being assessed clinically. This review documents the efficacy and toxicity of BTKi in chronic lymphocytic leukaemia (CLL)...
July 2014: British Journal of Haematology
https://www.readbyqxmd.com/read/24736247/ibrutinib-imbruvica-for-chronic-lymphocytic-leukemia
#18
REVIEW
(no author information available yet)
No abstract text is available yet for this article.
April 14, 2014: Medical Letter on Drugs and Therapeutics
https://www.readbyqxmd.com/read/24672212/pharmaceutical-approval-update
#19
Marvin M Goldenberg
Obinutuzumab (Gazyva) for chronic lymphocytic leukemia; ibrutinib (Imbruvica) for mantle-cell lymphoma; and sofosbuvir (Sovaldi) for chronic hepatitis C infection.
January 2014: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/24509736/imbruvica-next-big-drug-in-b-cell-cancer-approved-by-fda
#20
Malini Guha
No abstract text is available yet for this article.
February 2014: Nature Biotechnology
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