New Proteasome Inhibitors in Myeloma

An open-label, single-arm, phase 2 (PX-171-004) study of single-agent carfilzomib in bortezomib-naive patients with relapsed and/or refractory multiple myeloma

(2012) R. Vij et al.   BLOOD

The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects

(2012) M A Hurchla et al.   LEUKEMIA

Discovery and Development of Second-Generation Proteasome Inhibitors

(2012) Christopher J. Kirk   SEMINARS IN HEMATOLOGY

The Immunoproteasome as a Target in Hematologic Malignancies

(2012) Deborah J. Kuhn et al.   SEMINARS IN HEMATOLOGY

Antitumor Activity of the Investigational Proteasome Inhibitor MLN9708 in Mouse Models of B-cell and Plasma Cell Malignancies

(2011) E. C. Lee et al.   CLINICAL CANCER RESEARCH

In Vitro and In Vivo Selective Antitumor Activity of a Novel Orally Bioavailable Proteasome Inhibitor MLN9708 against Multiple Myeloma Cells

(2011) Dharminder Chauhan et al.   CLINICAL CANCER RESEARCH

Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events

(2011) S. Arastu-Kapur et al.   CLINICAL CANCER RESEARCH

Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials

(2011) B. C. Potts et al.   CURRENT CANCER DRUG TARGETS

Pharmacokinetics, Pharmacodynamics, Metabolism, Distribution, and Excretion of Carfilzomib in Rats

(2011) J. Yang et al.   DRUG METABOLISM AND DISPOSITION

Carfilzomib Interacts Synergistically with Histone Deacetylase Inhibitors in Mantle Cell Lymphoma Cells In Vitro and In Vivo

(2011) G. Dasmahapatra et al.   MOLECULAR CANCER THERAPEUTICS

A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma

(2010) D. Chauhan et al.   BLOOD

Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia

(2010) A. M. Roccaro et al.   BLOOD

Efficacy and safety of once-weekly bortezomib in multiple myeloma patients

(2010) S. Bringhen et al.   BLOOD

Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI-0052 (marizomib) in a human plasmacytoma xenograft murine model

(2010) Ajita V. Singh et al.   BRITISH JOURNAL OF HAEMATOLOGY

Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

(2010) E. Kupperman et al.   CANCER RESEARCH

Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy

(2010) Lawrence R. Dick et al.   DRUG DISCOVERY TODAY

Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma

(2009) D. Chauhan et al.   BLOOD

The proteasome inhibitor CEP-18770 enhances the anti-myeloma activity of bortezomib and melphalan

(2009) Eric Sanchez et al.   BRITISH JOURNAL OF HAEMATOLOGY

A Phase 1 Dose Escalation Study of the Safety and Pharmacokinetics of the Novel Proteasome Inhibitor Carfilzomib (PR-171) in Patients with Hematologic Malignancies

(2009) O. A. O'Connor et al.   CLINICAL CANCER RESEARCH

Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047)

(2009) Han-Jie Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

The use of novel agents in the treatment of relapsed and refractory multiple myeloma

(2009) J P Laubach et al.   LEUKEMIA

Emerging Treatments for Multiple Myeloma: Beyond Immunomodulatory Drugs and Bortezomib

(2009) Constantine S. Mitsiades et al.   SEMINARS IN HEMATOLOGY

Targeted inhibition of the immunoproteasome is a potent strategy against models of multiple myeloma that overcomes resistance to conventional drugs and nonspecific proteasome inhibitors

(2008) Deborah J. Kuhn et al.   BLOOD