Scientific Presentations and Publications

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Title
Meeting/Journal
Date 
Phase 1 study of the HSP90 inhibitor MPC-3100 in subjects with refractory or recurrent cancer pdf-icon-small AACR-NCI-EORTC International Conference
Nov-2011
Pharmacokinetics, anti-tumor activity and therapeutic index of Nampt inhibitor MPC-8640 in mice pdf-icon-small AACR-NCI-EORTC International Conference
Nov-2011
Phase II study of verubulin (MPC-6827) for the treatment of subjects with recurrent glioblastoma naïve to treatment with bevacizumab. pdf-icon-small American Society of Clinical Oncology Jun-2011
Activity of the cancer metabolism inhibitor MPC-9528 in xenograft models: Comparison of different dosing schedules. pdf-icon-small American Society of Clinical Oncology Jun-2011
MPI-0485520, a Small Molecule Inhibitor of IKKε/TBK1 is Active In aMouse Collagen-Induced Arthritis Model pdf-icon-small EULAR Annual European Congress of Rheumatology May-2011
Coadministration of nicotinic acid with the Nampt inhibitor MPC-9528 enhances anti-tumor activity in Naprt deficient cancer cells in culture and in xenografts pdf-icon-small AACR 102nd Annual Meeting Apr-2011
The Nampt inhibitor MPC-9528 synergizes with DNA damaging agents pdf-icon-small AACR 102nd Annual Meeting Apr-2011
Basal NAD levels and Nampt expression correlate with in vitro and in vivo sensitivity of tumor cell lines to the Nampt inhibitor MPC-9528 pdf-icon-small AACR 102nd Annual Meeting Apr-2011
Administration of Nicotinic Acid Reduces or Prevents Adverse Effects of MPC-9528, A Potent and Selective Nampt Inhibitor pdf-icon-small AACR 102nd Annual Meeting Apr-2011
The cancer metabolism inhibitor MPC-9528 induces tumor regression in xenograft models with multiple dosing schedules by causing rapid and sustained reduction in tumor NAD pdf-icon-small AACR 102nd Annual Meeting Apr-2011
Evaluation of the Pharmacokinetics and Efficacy of a Novel Pro-Drug of the HSP90 Inhibitor,MPC-3100, Designed with Improved Solubility pdf-icon-small AACR 102nd Annual Meeting Apr-2011
MPC-3100, a synthetic Hsp90 inhibitor, induces biomarker changes in vitro and in vivo pdf-icon-small AACR 102nd Annual Meeting Apr-2011
Anti-tumor Activity of MPC-3100, a Synthetic Hsp90 Inhibitor, in Combination with Erlotinib and Sorafenib pdf-icon-small AACR 102nd Annual Meeting Apr-2011
Comparative In Vitro and In Vivo Metabolism of MPC-3100, an Oral HSP90 Inhibitor, in Rat, Dog, Monkey and Human pdf-icon-small  AACR 102nd Annual Meeting  Apr-2011
Verubulin hydrochloride
view abstract
Drugs of the Future Dec-2010
Phase I clinical trial of MPC-6827 (Azixa), a microtubule destabilizing agent, in patients with advanced cancer view abstract Molecular Cancer Therapeutics 
Dec-2010
Phase 2 study of Azixa (verubulin or MPC-6827) for the treatment of glioblastoma after bevacizumab failure pdf-icon-small 2010 Society for Neuro-Oncology Scientific Meeting Nov-2010
The Nampt inhibitor MPC-9528 and the PARP inhibitor olaparib synergize in killing a BRCA--deficient cancer cell line pdf-icon-small 22nd EORTC-NCI-AACR Symposium Nov-2010
Anti-Tumor Activity of MPC-9528, GMX1778, and APO866: Nampt Inhibitors of Three Structural Classes pdf-icon-small 22nd EORTC-NCI-AACR Symposium Nov-2010
Inhibition of Cytosolic Nucleic Acid Receptor Pathways Using the Small Molecule IKKepsilon/TBK1 Kinase Inhibitor pdf-icon-small 74th ACR/ARHP Annual Meeting Nov-2010
MPC-9528, a cancer metabolism inhibitor, demonstrates greater therapeutic index in a Naprt1 deficient cancer xenograft model with co-administration of nicotinic acid pdf-icon-small Cancer and Metabolism: Pathways to the Future Symposium  Sep-2010
Chemical Proteomics Identifies Nampt as the Target of CB30865, An Orphan Cytotoxic Compound
view abstract
Chemistry and Biology Jun-2010
A clinical study investigating MPC-6827 with carboplatin in the treatment of patients with relapsed glioblastoma multiforme pdf-icon-small ASCO Jun-2010
Final report: MPC-6827 is safely combined with temozolomide for the treatment of patients with metastatic melanoma pdf-icon-small ASCO Jun-2010
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring
 
view abstract
Bioorg Med Chem Lett. Apr- 2010
Anti-tumor Activity of MPC-3100, a Synthetic, Orally Bioavailable Hsp90 Inhibitor, in Animal Models. pdf-icon-small AACR Apr-2010
Cellular and In Vivo Properties of MPI-0485520, a Novel and Potent Small Molecule Inhibitor of IKKe pdf-icon-small FASEB Apr-2010
TTK Kinase Inhibitor Development through Chemical Proteomics pdf-icon-small FASEB Apr-2010
Identifying the target of an orphan compound: CB30865 is a Nampt inhibitor pdf-icon-small AACR Apr-2010
MPI-0486348: A novel inhibitor of nicotinamide phosphoribosyltransferase induces tumor regression in a preclinical model pdf-icon-small AACR Apr-2010
Next Generation Orally Bioavailable HIV-1 Maturation Inhibitors pdf-icon-small ACS Mar-2010
MPC-4326 (bevirimat dimeglumine) Drug-Drug Interaction Profile pdf-icon-small CROI Feb-2010
Inhibition of TTK Activates the p53 Pathway pdf-icon-small AACR-NCI-EORTC Nov-2009
MPC-6827 is safely combined with temozolomide for the treatment of patients with metastatic melanoma pdf-icon-small AACR-NCI-EORTC Nov-2009
Pharmacokinetic and pharmacodynamic data for MPC-3100, a fully synthetic, orally bioavailable HSP90 inhibitor, in cancer patients pdf-icon-small AACR-NCI-EORTC Nov-2009
Inhibition of TTK Promotes Chromosome Segregation Defects in a Manner Distinct from Inhibitors of Aurora or PLK Mitotic Kinases pdf-icon-small AACR Frontiers in Basic Cancer Research Oct-2009
MPC-6827: anti-tumor activity in an orthotopic brain model and in combination with bevacizumab
view presentation pdf-icon-small
SNO Oct-2009
Efficacy, Safety and Pharmacokinetics of MPC-4326 (bevirimat dimeglumine) 200mg BID and 300mg BID Monotherapy Administered for 14 days in Subjects with HIV-1 Infection
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ICAAC Sep-2009
Pharmacokinetics and Safety of a Novel 100 mg Tablet Formulation of MPC-4326 in Subjects with HIV-1 Infection pdf-icon-small ICAAC Sep-2009
Impact of human immunodeficiency virus type 1 resistance to protease inhibitors on evolution of resistance to the maturation inhibitor bevirimat
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J. Virology May-2009
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration
 view abstract
J Med Chem Apr-2009
Azixa, a Microtubule Destabilizing Agent, in Solid Tumors: Results of a Phase 1 Trial pdf-icon-small AACR-NCI-EORTC Apr-2009
Characterization of an orally bioavailable homolog of MPC-6827 (MPI-443803) that maintains high brain penetration pdf-icon-small AACR Apr-2009
A Novel Small Molecule Inhibitor of the Mitotic Kinase TTK with Anti- Tumor Activity in Pre-Clinical Models pdf-icon-small AACR Apr-2009
Anti-viral Characterization in vitro of a Novel Maturation Inhibitor, MPC-9055 pdf-icon-small CROI Feb-2009
Phase 1, Single Ascending Oral Dose Study of the Safety, Tolerability, and Pharmacokinetics of a Novel HIV-1 Maturation Inhibitor in HIV Negative Healthy Subjects pdf-icon-small CROI Feb-2009
Susceptibility of Diverse HIV-1 Patient Isolates to the Maturation Inhibitor, Bevirimat (MPC-4326*), is Determined by Clade-Specific Polymorphisms in Gag CA-SP1 pdf-icon-small CROI Feb-2009
MPC-3100: A non-natural product Hsp90 inhibitor with anti-tumor activity in preclinical models. pdf-icon-small AACR-NCI-EORTC Oct-2008
HIV-1 Gag Polymorphisms Determine Treatment Response to Bevirimat (PA-457) pdf-icon-small XVII International HIV Drug Resistance Workshop Jun-2008
Role of Gag Polymorphisms in HIV-1 Sensitivity to the Maturation Inhibitor Bevirimat pdf-icon-small XVII International HIV Drug Resistance Workshop Jun-2008
MPC-6827: A Small-Molecule Inhibitor of Microtubule Formation That Is Not a Substrate for Multidrug Resistance Pumps pdf-icon-small Cancer Research Jun-2007
Two phase 1 studies of MPC-6827, a novel vascular disrupting agent (VDA), in patients with advanced solid tumors and CNS metastases pdf-icon-small ASCO Jun-2007
Vascular Disruption Effects of MPC-6827 pdf-icon-small AACR Jun-2007
The first in class maturation inhibitor, PA-457, is a potent inhibitor of HIV drug-resistant isolates and acts synergistically with approved HIV drugs in vitro pdf-icon-small CROI Feb-2006
Pharmacokinetic/Pharmacodynamic Effects of PA-457 In HIV-infected Patients Following A Single Oral Dose pdf-icon-small IAS Jul-2005
MPC-6827, A Small Molecule Inhibitor of Microtubule Formation with High Brain Penetration: Absorption, Distribution, Metabolism, Excretion, and Clinical Considerations pdf-icon-small AACR Apr-2005
MPC-6827, A Small Molecule Inhibitor of Microtubule Formation; Pharmacokinetics in Nu/+ Mice, Sprague Dawley Rats and Beagle Dogs Following Intravenous Administration. pdf-icon-small AACR Apr-2005
MPC-6827: A small molecule inhibitor of microtubule formation that is not a substrate for multi-drug resistance pumps pdf-icon-small AACR Apr-2005
Antitumor Activity of MPC-6827 in Human Breast, Colon, Pancreatic, Ovarian and Mouse Melanoma Tumor Xenografts in Athymic Nude Mice pdf-icon-small AACR Mar-2004
PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing
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PNAS Nov-2003
The Protein Network of HIV Budding
view abstract
Cell Sep-2003
Tsg101 and the Vacuolar Protein Sorting Pathway Are Essential for HIV-1 Budding
view abstract
Cell Oct-2001