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Revision as of 21:55, 8 April 2013
In clinical trials.
General information
Class/mechanism: Second-generation proteasome inhibitor; interferes with degradation of ubiquitinated proteins. This disrupts normal homeostatic mechansims, leading to cell death. The tissue distribution profile of MLN9708 may be different than Bortezomib (Velcade) due to a shorter 20S proteasome dissociation half-life. Upon exposure to aqueous solutions, MLN9708 hydrolyzes to MLN2238, the active form.[1][2][3][4]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Clinical trials
- A Study of MLN9708 Administered in Combination With Lenalidomide and Low-Dose Dexamethasone in Patients With Newly Diagnosed Multiple Myeloma
- Phase 1 Study of Oral MLN9708 in Patients With Advanced Nonhematologic Malignancies or Lymphoma
- Proteasome Inhibitor MLN9708 in Treating Patients With Relapsed Multiple Myeloma That Is Not Refractory to Bortezomib
- A Study of MLN9708 in Adult Patients With Lymphoma
- Study of Oral MLN9708 in Adult Patients With Relapsed or Refractory Light Chain Amyloidosis
- Study Evaluating the Safety and Tolerability of Weekly Dosing of Oral MLN9708 in Adult Patients With Relapsed and Refractory Multiple Myeloma
Patient drug information
No information available.
References
- ↑ Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L, Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80. Epub 2010 Feb 16. PubMed
- ↑ Siegfried Janz, Brian G Van Ness, Vishala Neppalli, Ray Liu, Michael D Pickard, Jennifer Terkelsen, Daniel Bradley, Ling Hu, Erik Kupperman, Mark Manfredi, and Edmund Lee. The Novel Proteasome Inhibitor MLN9708 Demonstrates Efficacy in a Genetically-Engineered Mouse Model of De Novo Plasma Cell Malignancy. 2009 ASH Annual Meeting oral poster/abstract 3849.
- ↑ Aisha Masood, MD, Kasyapa Chitta, PhD, Kiersten M Miles, PhD, Nazmul H Khan, PhD, Remi Adelaiye, Drusilla Akhtar, Taimur Sher, MD, and Asher A. Chanan-Khan, MD. An Investigational Proteasome Inhibitor MLN9708 (MLN2238) Induces Apoptosis In Human Multiple Myeloma Cells In Vitro. 2010 ASH Annual Meeting oral poster/abstract 3066.
- ↑ Paul G. Richardson, MD, Rachid Baz, MD, Luhua Wang, MD, Andrzej J Jakubowiak, MD, PhD, Deborah Berg, RN, MSN, Guohui Liu, PhD, Neeraj Gupta, PhD, Alessandra Di Bacco, PhD, Ai-Min Hui, MD, and Sagar Lonial, MD. Investigational Agent MLN9708, An Oral Proteasome Inhibitor, in Patients (Pts) with Relapsed and/or Refractory Multiple Myeloma (MM): Results From the Expansion Cohorts of a Phase 1 Dose-Escalation Study. 2011 ASH Annual Meeting oral poster/abstract 301.