Literature DB >> 25456369

Safety and tolerability of ixazomib, an oral proteasome inhibitor, in combination with lenalidomide and dexamethasone in patients with previously untreated multiple myeloma: an open-label phase 1/2 study.

Shaji K Kumar1, Jesus G Berdeja2, Ruben Niesvizky3, Sagar Lonial4, Jacob P Laubach5, Mehdi Hamadani6, A Keith Stewart7, Parameswaran Hari8, Vivek Roy9, Robert Vescio10, Jonathan L Kaufman4, Deborah Berg11, Eileen Liao11, Alessandra Di Bacco11, Jose Estevam11, Neeraj Gupta11, Ai-Min Hui11, Vincent Rajkumar12, Paul G Richardson5.   

Abstract

BACKGROUND: The combination of bortezomib, lenalidomide, and dexamethasone is a highly effective therapy for newly diagnosed multiple myeloma. Ixazomib is an investigational, oral, proteasome inhibitor with promising anti-myeloma effects and low rates of peripheral neuropathy. In a phase 1/2 trial we aimed to assess the safety, tolerability, and activity of ixazomib in combination with lenalidomide and dexamethasone in newly diagnosed multiple myeloma.
METHODS: We enrolled patients newly diagnosed with multiple myeloma aged 18 years or older with measurable disease, Eastern Cooperative Oncology Group performance status 0-2, and no grade 2 or higher peripheral neuropathy, and treated them with oral ixazomib (days 1, 8, 15) plus lenalidomide 25 mg (days 1-21) and dexamethasone 40 mg (days 1, 8, 15, 22) for up to 12 28-day cycles, followed by maintenance therapy with ixazomib alone. In phase 1, we gave patients escalating doses of ixazomib (1·68-3·95 mg/m(2)) to establish the recommended dose for phase 2. The primary endpoints were maximum tolerated dose for phase 1, and the rate of very good partial response or better for phase 2. Safety analyses were done in all patients who received at least one dose of study drug; efficacy analyses were done in all patients who received at least one dose of study drug at the phase 2 dose, had measurable disease at baseline, and had at least one post-baseline response assessment. This study is registered at ClinicalTrials.gov, number NCT01217957.
FINDINGS: Between Nov 22, 2010, and Feb 28, 2012, we enrolled 65 patients (15 to phase 1 and 50 to phase 2). Four dose-limiting toxic events were noted in phase 1: one at a dose of ixazomib of 2·97 mg/m(2) and three at 3·95 mg/m(2). The maximum tolerated dose of ixazomib was established as 2·97 mg/m(2) and the recommended phase 2 dose was 2·23 mg/m(2), which was converted to a 4·0 mg fixed dose based on population pharmacokinetic results. Grade 3 or higher adverse events related to any drug were reported in 41 (63%) patients, including skin and subcutaneous tissue disorders (11 patients, 17%), neutropenia (eight patients, 12%), and thrombocytopenia (five patients, 8%); drug-related peripheral neuropathy of grade 3 or higher occurred in four (6%) patients. Five patients discontinued because of adverse events. In 64 response-evaluable patients, 37 (58%, 95% CI 45-70) had a very good partial response or better.
INTERPRETATION: The all-oral combination of weekly ixazomib plus lenalidomide and dexamethasone was generally well tolerated and appeared active in newly diagnosed multiple myeloma. These results support the phase 3 trial development of this combination for multiple myeloma. FUNDING: Millennium Pharmaceuticals, a wholly owned subsidiary of Takeda Pharmaceutical International Company.
Copyright © 2014 Elsevier Ltd. All rights reserved.

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Year:  2014        PMID: 25456369     DOI: 10.1016/S1470-2045(14)71125-8

Source DB:  PubMed          Journal:  Lancet Oncol        ISSN: 1470-2045            Impact factor:   41.316


  98 in total

Review 1.  Nanotherapeutics for multiple myeloma.

Authors:  Alexander Zheleznyak; Monica Shokeen; Samuel Achilefu
Journal:  Wiley Interdiscip Rev Nanomed Nanobiotechnol       Date:  2018-04-26

Review 2.  Integration of Novel Agents into the Care of Patients with Multiple Myeloma.

Authors:  Robert Z Orlowski; Sagar Lonial
Journal:  Clin Cancer Res       Date:  2016-11-14       Impact factor: 12.531

3.  Progress and Paradigms in Multiple Myeloma.

Authors:  Kenneth C Anderson
Journal:  Clin Cancer Res       Date:  2016-11-15       Impact factor: 12.531

4.  Multiple myeloma: 2018 update on diagnosis, risk‐stratification, and management

Authors: 
Journal:  Am J Hematol       Date:  2018-08-16       Impact factor: 10.047

5.  CRISPR Genome-Wide Screening Identifies Dependence on the Proteasome Subunit PSMC6 for Bortezomib Sensitivity in Multiple Myeloma.

Authors:  Chang-Xin Shi; K Martin Kortüm; Yuan Xiao Zhu; Laura A Bruins; Patrick Jedlowski; Patrick G Votruba; Moulun Luo; Robert A Stewart; Jonathan Ahmann; Esteban Braggio; A Keith Stewart
Journal:  Mol Cancer Ther       Date:  2017-09-27       Impact factor: 6.261

6.  Promising therapies in multiple myeloma.

Authors:  Giada Bianchi; Paul G Richardson; Kenneth C Anderson
Journal:  Blood       Date:  2015-06-01       Impact factor: 22.113

Review 7.  The potential of ixazomib, a second-generation proteasome inhibitor, in the treatment of multiple myeloma.

Authors:  Jason Brayer; Rachid Baz
Journal:  Ther Adv Hematol       Date:  2017-06-28

8.  New drugs in myeloma: beware of phase I trial results, beware of cost and demand for new trials.

Authors:  P Moreau
Journal:  Leukemia       Date:  2017-06-30       Impact factor: 11.528

9.  Ixazomib-induced cutaneous necrotizing vasculitis.

Authors:  A Alloo; H Khosravi; S R Granter; S M Jadeja; P G Richardson; J J Castillo; N R LeBoeuf
Journal:  Support Care Cancer       Date:  2018-02-01       Impact factor: 3.603

10.  Ixazomib promotes CHOP-dependent DR5 induction and apoptosis in colorectal cancer cells.

Authors:  Dan Yue; Xun Sun
Journal:  Cancer Biol Ther       Date:  2018-10-25       Impact factor: 4.742

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