Targeting the apoptosis pathway in hematologic malignancies

A randomized, placebo-controlled phase 2 study of ganitumab or conatumumab in combination with FOLFIRI for second-line treatment of mutant KRAS metastatic colorectal cancer†

(2013) A. L. Cohn et al.   ANNALS OF ONCOLOGY

Potent obatoclax cytotoxicity and activation of triple death mode killing across infant acute lymphoblastic leukemia

(2013) K. A. Urtishak et al.   BLOOD

XIAP antisense therapy with AEG 35156 in acute myeloid leukemia

(2013) Lakshmikanth Katragadda et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Safety and pharmacokinetics of the antisense oligonucleotide (ASO) LY2181308 as a single-agent or in combination with idarubicin and cytarabine in patients with refractory or relapsed acute myeloid leukemia (AML)

(2013) Harry P. Erba et al.   INVESTIGATIONAL NEW DRUGS

A Randomized Phase 2 Study of Paclitaxel and Carboplatin with or without Conatumumab for First-Line Treatment of Advanced Non–Small-Cell Lung Cancer

(2013) Luis Paz-Ares et al.   Journal of Thoracic Oncology

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

A randomized, placebo-controlled phase 2 study of ganitumab (AMG 479) or conatumumab (AMG 655) in combination with gemcitabine in patients with metastatic pancreatic cancer

(2012) H. L. Kindler et al.   ANNALS OF ONCOLOGY

Cotargeting signaling pathways driving survival and cell cycle circumvents resistance to Kit inhibitors in leukemia

(2012) D. Buet et al.   BLOOD

Experience with obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist in patients with relapsed or refractory classical Hodgkin lymphoma

(2012) Y. Oki et al.   BLOOD

AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer

(2012) Melissa K. Brunckhorst et al.   CANCER BIOLOGY & THERAPY

Survivin as a Prognostic/Predictive Marker and Molecular Target in Cancer Therapy

(2012) F. Rodel et al.   CURRENT MEDICINAL CHEMISTRY

First-line treatment of metastatic or locally advanced unresectable soft tissue sarcomas with conatumumab in combination with doxorubicin or doxorubicin alone: A Phase I/II open-label and double-blind study

(2012) George D. Demetri et al.   EUROPEAN JOURNAL OF CANCER

Targeting the Bcl-2 family for cancer therapy

(2012) Shibu Thomas et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Phase I Trial and Pharmacokinetic Study of Lexatumumab in Pediatric Patients With Solid Tumors

(2012) Melinda S. Merchant et al.   JOURNAL OF CLINICAL ONCOLOGY

Bax and Bak are required for apogossypolone, a BH3-mimetic, induced apoptosis in chronic lymphocytic leukemia cells

(2012) Kumudha Balakrishnan et al.   LEUKEMIA & LYMPHOMA

Development of Noxa-like BH3 Mimetics for Apoptosis-Based Therapeutic Strategy in Chronic Lymphocytic Leukemia

(2012) Christian Billard   MOLECULAR CANCER RESEARCH

Targeting IAP proteins for therapeutic intervention in cancer

(2012) Simone Fulda et al.   NATURE REVIEWS DRUG DISCOVERY

ABT-737 is highly effective against molecular subgroups of multiple myeloma

(2011) L. Bodet et al.   BLOOD

Evaluation of pharmacodynamic biomarkers in a Phase 1a trial of dulanermin (rhApo2L/TRAIL) in patients with advanced tumours

(2011) Y Pan et al.   BRITISH JOURNAL OF CANCER

Distinct cellular and therapeutic effects of obatoclax in rituximab-sensitive and -resistant lymphomas

(2011) Elizabeth A. Brem et al.   BRITISH JOURNAL OF HAEMATOLOGY

A phase II study of the survivin suppressant YM155 in patients with refractory diffuse large B-cell lymphoma

(2011) Bruce D. Cheson et al.   CANCER

Tipping the Noxa/Mcl-1 Balance Overcomes ABT-737 Resistance in Chronic Lymphocytic Leukemia

(2011) J. M. Tromp et al.   CLINICAL CANCER RESEARCH

Addition of AEG35156 XIAP Antisense Oligonucleotide in Reinduction Chemotherapy Does Not Improve Remission Rates in Patients With Primary Refractory Acute Myeloid Leukemia in a Randomized Phase II Study

(2011) Aaron D. Schimmer et al.   Clinical Lymphoma Myeloma & Leukemia

Randomized Phase II Study of Dulanermin in Combination With Paclitaxel, Carboplatin, and Bevacizumab in Advanced Non–Small-Cell Lung Cancer

(2011) Jean-Charles Soria et al.   JOURNAL OF CLINICAL ONCOLOGY

Substantial Susceptibility of Chronic Lymphocytic Leukemia to BCL2 Inhibition: Results of a Phase I Study of Navitoclax in Patients With Relapsed or Refractory Disease

(2011) Andrew W. Roberts et al.   JOURNAL OF CLINICAL ONCOLOGY

A Potent and Orally Active Antagonist (SM-406/AT-406) of Multiple Inhibitor of Apoptosis Proteins (IAPs) in Clinical Development for Cancer Treatment

(2011) Qian Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of CD44, a receptor for extracellular matrix components, protects chronic lymphocytic leukemia cells from spontaneous and drug induced apoptosis through MCL-1

(2011) Yair Herishanu et al.   LEUKEMIA & LYMPHOMA

Initial testing (stage 1) of LCL161, a SMAC mimetic, by the pediatric preclinical testing program

(2011) Peter J. Houghton et al.   PEDIATRIC BLOOD & CANCER

XIAP antisense oligonucleotide (AEG35156) achieves target knockdown and induces apoptosis preferentially in CD34+38− cells in a phase 1/2 study of patients with relapsed/refractory AML

(2010) Bing Z. Carter et al.   APOPTOSIS

Inflammation and survival pathways: Chronic lymphocytic leukemia as a model system

(2010) Lisa S. Chen et al.   BIOCHEMICAL PHARMACOLOGY

Combination immunotherapy using adoptive T-cell transfer and tumor antigen vaccination on the basis of hTERT and survivin after ASCT for myeloma

(2010) A. P. Rapoport et al.   BLOOD

A Phase 1b/2 trial of mapatumumab in patients with relapsed/refractory non-Hodgkin's lymphoma

(2010) A Younes et al.   BRITISH JOURNAL OF CANCER

Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo

(2010) Yuan Sun et al.   CANCER BIOLOGY & THERAPY

Conatumumab, a fully human agonist antibody to death receptor 5, induces apoptosis via caspase activation in multiple tumor types

(2010) Paula J. Kaplan-Lefko et al.   CANCER BIOLOGY & THERAPY

Phase I Trial of Weekly Tigatuzumab, an Agonistic Humanized Monoclonal Antibody Targeting Death Receptor 5 (DR5)

(2010) Andres Forero-Torres et al.   CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS

Phase I study of LY2181308, an antisense oligonucleotide against survivin, in patients with advanced solid tumors

(2010) M. Tanioka et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Discovery and Canine Preclinical Assessment of a Nontoxic Procaspase-3-Activating Compound

(2010) Q. P. Peterson et al.   CANCER RESEARCH

A Phase I Safety and Pharmacokinetic Study of the Death Receptor 5 Agonistic Antibody PRO95780 in Patients with Advanced Malignancies

(2010) D. R. Camidge et al.   CLINICAL CANCER RESEARCH

A First-in-Human Study of Conatumumab in Adult Patients with Advanced Solid Tumors

(2010) R. S. Herbst et al.   CLINICAL CANCER RESEARCH

Tumor Survivin Is Downregulated by the Antisense Oligonucleotide LY2181308: A Proof-of-Concept, First-in-Human Dose Study

(2010) D. C. Talbot et al.   CLINICAL CANCER RESEARCH

Phase II Study of Obatoclax Mesylate (GX15-070), a Small-Molecule BCL-2 Family Antagonist, for Patients With Myelofibrosis

(2010) Sameer A. Parikh et al.   Clinical Lymphoma Myeloma & Leukemia

Expression and prognostic significance of the inhibitor of apoptosis protein (IAP) family and its antagonists in chronic lymphocytic leukaemia

(2010) Olga Grzybowska-Izydorczyk et al.   EUROPEAN JOURNAL OF CANCER

Induction of autophagy-dependent necroptosis is required for childhood acute lymphoblastic leukemia cells to overcome glucocorticoid resistance

(2010) Laura Bonapace et al.   JOURNAL OF CLINICAL INVESTIGATION

Phase 1b Study of Dulanermin (recombinant human Apo2L/TRAIL) in Combination With Paclitaxel, Carboplatin, and Bevacizumab in Patients With Advanced Non-Squamous Non–Small-Cell Lung Cancer

(2010) Jean-Charles Soria et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Dose-Escalation Study of Recombinant Human Apo2L/TRAIL, a Dual Proapoptotic Receptor Agonist, in Patients With Advanced Cancer

(2010) Roy S. Herbst et al.   JOURNAL OF CLINICAL ONCOLOGY

BI-97C1, an Optically Pure Apogossypol Derivative as Pan-Active Inhibitor of Antiapoptotic B-Cell Lymphoma/Leukemia-2 (Bcl-2) Family Proteins

(2010) Jun Wei et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prognostic significance of XIAP expression in DLBCL and effect of its inhibition on AKT signalling

(2010) Azhar R Hussain et al.   JOURNAL OF PATHOLOGY

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity

(2010) Wyndham H Wilson et al.   LANCET ONCOLOGY

Smac mimetics: implications for enhancement of targeted therapies in leukemia

(2010) E Weisberg et al.   LEUKEMIA

Influence of high expression of Smac/DIABLO protein on the clinical outcome in acute myeloid leukemia patients

(2010) Agnieszka Pluta et al.   LEUKEMIA RESEARCH

VSV Oncolysis in Combination With the BCL-2 Inhibitor Obatoclax Overcomes Apoptosis Resistance in Chronic Lymphocytic Leukemia

(2010) Sara Samuel et al.   MOLECULAR THERAPY

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

(2010) Michelle L Stewart et al.   Nature Chemical Biology

XIAP expression is post-transcriptionally upregulated in childhood ALL and is associated with glucocorticoid response in T-cell ALL

(2010) Patrick Hundsdoerfer et al.   PEDIATRIC BLOOD & CANCER

Phase I and pharmacokinetic study of lexatumumab (HGS-ETR2) given every 2 weeks in patients with advanced solid tumors

(2009) H. A. Wakelee et al.   ANNALS OF ONCOLOGY

Identification of proapoptotic Bim as a tumor suppressor in neoplastic mast cells: role of KIT D816V and effects of various targeted drugs

(2009) K. J. Aichberger et al.   BLOOD

Different forms of cell death induced by putative BCL2 inhibitors

(2009) M Vogler et al.   CELL DEATH AND DIFFERENTIATION

Targeting apoptosis: preclinical and early clinical experience with mapatumumab, an agonist monoclonal antibody targeting TRAIL-R1

(2009) Patricia Moretto et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

5-Year Survival in Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia in a Randomized, Phase III Trial of Fludarabine Plus Cyclophosphamide With or Without Oblimersen

(2009) Susan O'Brien et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I/II Trial of AEG35156 X-Linked Inhibitor of Apoptosis Protein Antisense Oligonucleotide Combined With Idarubicin and Cytarabine in Patients With Relapsed or Primary Refractory Acute Myeloid Leukemia

(2009) Aaron D. Schimmer et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Trial of AEG35156 Administered as a 7-Day and 3-Day Continuous Intravenous Infusion in Patients With Advanced Refractory Cancer

(2009) Emma Dean et al.   JOURNAL OF CLINICAL ONCOLOGY

Overexpression of X-linked Inhibitor of Apoptosis Protein (XIAP) is an Independent Unfavorable Prognostic Factor in Childhood de Novo Acute Myeloid Leukemia

(2009) Ki Woong Sung et al.   JOURNAL OF KOREAN MEDICAL SCIENCE

PAC-1 Activates Procaspase-3 in Vitro through Relief of Zinc-Mediated Inhibition

(2009) Quinn P. Peterson et al.   JOURNAL OF MOLECULAR BIOLOGY

Phase III randomised study of dexamethasone with or without oblimersen sodium for patients with advanced multiple myeloma

(2009) Asher A. Chanan-Khan et al.   LEUKEMIA & LYMPHOMA

Small-Molecule Activators of a Proenzyme

(2009) D. W. Wolan et al.   SCIENCE

Design of Small-Molecule Peptidic and Nonpeptidic Smac Mimetics

(2008) Haiying Sun et al.   ACCOUNTS OF CHEMICAL RESEARCH

Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048)

(2008) S. Kitada et al.   BLOOD

Gossypol, a BH3 mimetic, induces apoptosis in chronic lymphocytic leukemia cells

(2008) K. Balakrishnan et al.   BLOOD

Bcl-2-family proteins and hematologic malignancies: history and future prospects

(2008) J. C. Reed   BLOOD

Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia

(2008) S. M. O'Brien et al.   BLOOD

AT-101 induces apoptosis in CLL B cells and overcomes stromal cell-mediated Mcl-1 induction and drug resistance

(2008) K. Balakrishnan et al.   BLOOD

Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax)

(2008) M. Konopleva et al.   CANCER RESEARCH

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

Structural and functional analysis of the interaction between the agonistic monoclonal antibody Apomab and the proapoptotic receptor DR5

(2008) C Adams et al.   CELL DEATH AND DIFFERENTIATION

A Phase I Study of the Pan Bcl-2 Family Inhibitor Obatoclax Mesylate in Patients with Advanced Hematologic Malignancies

(2008) A. D. Schimmer et al.   CLINICAL CANCER RESEARCH

A novel BH3 ligand that selectively targets Mcl-1 reveals that apoptosis can proceed without Mcl-1 degradation

(2008) Erinna F. Lee et al.   JOURNAL OF CELL BIOLOGY

Phase I and Pharmacokinetic Study of YM155, a Small-Molecule Inhibitor of Survivin

(2008) Anthony W. Tolcher et al.   JOURNAL OF CLINICAL ONCOLOGY

BCL-2 family antagonists for cancer therapy

(2008) Guillaume Lessene et al.   NATURE REVIEWS DRUG DISCOVERY

Directing cancer cells to self-destruct with pro-apoptotic receptor agonists

(2008) Avi Ashkenazi   NATURE REVIEWS DRUG DISCOVERY