Treating cancer with selective CDK4/6 inhibitors

Ph IB study of LEE011 and BYL719 in combination with letrozole in ER+, HER2- breast cancer.

(2017) Pamela N. Munster et al.   JOURNAL OF CLINICAL ONCOLOGY

Treatment Rationale and Study Design for the JUNIPER Study: A Randomized Phase III Study of Abemaciclib With Best Supportive Care Versus Erlotinib With Best Supportive Care in Patients With Stage IV Non–Small-Cell Lung Cancer With a Detectable KRAS Mutation Whose Disease Has Progressed After Platinum-Based Chemotherapy

(2016) Jonathan W. Goldman et al.   Clinical Lung Cancer

86O * PI3 kinase/mTOR inhibition increases sensitivity of ER positive breast cancers to CDK4/6 inhibition by blocking cell cycle re-entry driven by cyclinD1 and inducing apoptosis

(2015) M. T. Herrera-Abreu et al.   ANNALS OF ONCOLOGY

Abstract P5-10-06: Risk of recurrence estimates with IHC4 are tolerant of variations in staining and scoring

(2015) Andrew Dodson et al.   CANCER RESEARCH

Abstract P5-19-13: Clinical activity of abemaciclib, an oral cell cycle inhibitor, in metastatic breast cancer

(2015) Sara M Tolaney et al.   CANCER RESEARCH

Abstract OT1-1-07: A phase III study of abemaciclib (LY2835219) combined with fulvestrant in women with hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) breast cancer (MONARCH 2)

(2015) Antonio Llombart et al.   CANCER RESEARCH

Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy That Cotargets MEK and CDK4/6

(2015) E. K. Ziemke et al.   CLINICAL CANCER RESEARCH

CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma

(2015) M. E. Olanich et al.   CLINICAL CANCER RESEARCH

Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer

(2015) S. E. Wardell et al.   CLINICAL CANCER RESEARCH

Treatment Selection and Outcomes in Early-Stage Classical Hodgkin Lymphoma: Analysis of the National Cancer Data Base

(2015) Adam J. Olszewski et al.   JOURNAL OF CLINICAL ONCOLOGY

The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study

(2015) Richard S Finn et al.   LANCET ONCOLOGY

Phase 1/2 study of cyclin-dependent kinase (CDK)4/6 inhibitor palbociclib (PD-0332991) with bortezomib and dexamethasone in relapsed/refractory multiple myeloma

(2015) Ruben Niesvizky et al.   LEUKEMIA & LYMPHOMA

The history and future of targeting cyclin-dependent kinases in cancer therapy

(2015) Uzma Asghar et al.   NATURE REVIEWS DRUG DISCOVERY

Palbociclib in Hormone-Receptor–Positive Advanced Breast Cancer

(2015) Nicholas C. Turner et al.   NEW ENGLAND JOURNAL OF MEDICINE

Abstract CT232: Clinical activity of LY2835219, a novel cell cycle inhibitor selective for CDK4 and CDK6, in patients with metastatic breast cancer

(2015) Amita Patnaik et al.   CANCER RESEARCH

Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors

(2014) David J. Vaughn et al.   CANCER

CDK 4/6 Inhibitors Sensitize PIK3CA Mutant Breast Cancer to PI3K Inhibitors

(2014) Sadhna R. Vora et al.   CANCER CELL

CDK4/6 and IGF1 Receptor Inhibitors Synergize to Suppress the Growth of p16INK4A-Deficient Pancreatic Cancers

(2014) A. M. Heilmann et al.   CANCER RESEARCH

LINE-1 Hypomethylation, DNA Copy Number Alterations, andCDK6Amplification in Esophageal Squamous Cell Carcinoma

(2014) Yoshifumi Baba et al.   CLINICAL CANCER RESEARCH

CDK 4/6 Inhibitor Palbociclib (PD0332991) in Rb+ Advanced Breast Cancer: Phase II Activity, Safety, and Predictive Biomarker Assessment

(2014) A. DeMichele et al.   CLINICAL CANCER RESEARCH

Semi-Mechanistic Pharmacokinetic/Pharmacodynamic Modeling of the Antitumor Activity of LY2835219, a New Cyclin-Dependent Kinase 4/6 Inhibitor, in Mice Bearing Human Tumor Xenografts

(2014) S. C. Tate et al.   CLINICAL CANCER RESEARCH

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine

(2014) Lawrence M. Gelbert et al.   INVESTIGATIONAL NEW DRUGS

Phase I Dose-Escalation Study of LCL161, an Oral Inhibitor of Apoptosis Proteins Inhibitor, in Patients With Advanced Solid Tumors

(2014) Jeffrey R. Infante et al.   JOURNAL OF CLINICAL ONCOLOGY

Solidifying Liquid Biopsies: Can Circulating Tumor Cell Monitoring Guide Treatment Selection in Breast Cancer?

(2014) Aditya Bardia et al.   JOURNAL OF CLINICAL ONCOLOGY

Abstract C81: BBB efflux pump activity limits brain penetration of palbociclib (PD0332991) in glioblastoma.

(2014) K. E. Parrish et al.   MOLECULAR CANCER THERAPEUTICS

Abstract PR02: LEE011: An orally bioavailable, selective small molecule inhibitor of CDK4/6- Reactivating Rb in cancer.

(2014) S. Kim et al.   MOLECULAR CANCER THERAPEUTICS

AMG 925 Is a Dual FLT3/CDK4 Inhibitor with the Potential to Overcome FLT3 Inhibitor Resistance in Acute Myeloid Leukemia

(2014) C. Li et al.   MOLECULAR CANCER THERAPEUTICS

The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation

(2014) V. Yadav et al.   MOLECULAR CANCER THERAPEUTICS

Antiproliferative Effects of CDK4/6 Inhibition in CDK4-Amplified Human Liposarcoma In Vitro and In Vivo

(2014) Y.-X. Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Synthetic Lethal Therapy for KRAS Mutant Non-small-cell Lung Carcinoma with Nanoparticle-mediated CDK4 siRNA Delivery

(2014) Cheng-Qiong Mao et al.   MOLECULAR THERAPY

Cyclin-Dependent Kinase Inhibitors as Marketed Anticancer Drugs: Where Are We Now? A Short Survey

(2014) Gaëlle Mariaule et al.   MOLECULES

PD0332991 (Palbociclib) for treatment of pediatric intracranial growing teratoma syndrome

(2014) Kris Ann P. Schultz et al.   PEDIATRIC BLOOD & CANCER

Loss ofCDKN2Aexpression is a frequent event in primary invasive melanoma and correlates with sensitivity to the CDK4/6 inhibitor PD0332991 in melanoma cell lines

(2014) Richard J. Young et al.   Pigment Cell & Melanoma Research

Cell-Cycle Reprogramming for PI3K Inhibition Overrides a Relapse-Specific C481S BTK Mutation Revealed by Longitudinal Functional Genomics in Mantle Cell Lymphoma

(2014) D. Chiron et al.   Cancer Discovery

Translocation t(2;7)(p11;q21) associated with the CDK6/IGK rearrangement is a rare but recurrent abnormality in B-cell lymphoproliferative malignancies

(2014) Nathalie Douet-Guilbert et al.   Cancer Genetics

The Proliferation-Quiescence Decision Is Controlled by a Bifurcation in CDK2 Activity at Mitotic Exit

(2013) Sabrina L. Spencer et al.   CELL

The Somatic Genomic Landscape of Glioblastoma

(2013) Cameron W. Brennan et al.   CELL

Induction of prolonged early G1arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3Kδ inhibition through PIK3IP1

(2013) David Chiron et al.   CELL CYCLE

Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma

(2013) J. Rader et al.   CLINICAL CANCER RESEARCH

Oncogene abnormalities in a series of primary melanomas of the sinonasal tract: NRAS mutations and cyclin D1 amplification are more frequent than KIT or BRAF mutations

(2013) Meriem Chraybi et al.   HUMAN PATHOLOGY

Bisphosphonate-Related Osteonecrosis of Jaw in the Adjuvant Breast Cancer Setting: Risks and Perspective

(2013) Charles L. Shapiro   JOURNAL OF CLINICAL ONCOLOGY

Phase II Trial of the CDK4 Inhibitor PD0332991 in Patients With Advanced CDK4-Amplified Well-Differentiated or Dedifferentiated Liposarcoma

(2013) Mark A. Dickson et al.   JOURNAL OF CLINICAL ONCOLOGY

Final Overall Survival: Fulvestrant 500 mg vs 250 mg in the Randomized CONFIRM Trial

(2013) A. D. Leo et al.   JNCI-Journal of the National Cancer Institute

ESR1 ligand-binding domain mutations in hormone-resistant breast cancer

(2013) Weiyi Toy et al.   NATURE GENETICS

Activating ESR1 mutations in hormone-resistant metastatic breast cancer

(2013) Dan R Robinson et al.   NATURE GENETICS

Targeting cell cycle and hormone receptor pathways in cancer

(2013) C E S Comstock et al.   ONCOGENE

PD-0332991, a CDK4/6 Inhibitor, Significantly Prolongs Survival in a Genetically Engineered Mouse Model of Brainstem Glioma

(2013) Kelly L. Barton et al.   PLoS One

Intratumor heterogeneity in human glioblastoma reflects cancer evolutionary dynamics

(2013) A. Sottoriva et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective CDK4/6 inhibition with tumor responses by PD0332991 in patients with mantle cell lymphoma

(2012) J. P. Leonard et al.   BLOOD

The Requirement for Cyclin D Function in Tumor Maintenance

(2012) Yoon Jong Choi et al.   CANCER CELL

Therapeutic Targeting of the Cyclin D3:CDK4/6 Complex in T Cell Leukemia

(2012) Catherine M. Sawai et al.   CANCER CELL

The Cyclin-Dependent Kinase Inhibitor Flavopiridol Potentiates Doxorubicin Efficacy in Advanced Sarcomas: Preclinical Investigations and Results of a Phase I Dose-Escalation Clinical Trial

(2012) J. J. Luke et al.   CLINICAL CANCER RESEARCH

Sequencing of t(2;7) Translocations Reveals a Consistent Breakpoint Linking CDK6 to the IGK Locus in Indolent B-Cell Neoplasia

(2012) Edward P.K. Parker et al.   JOURNAL OF MOLECULAR DIAGNOSTICS

Abstract B234: LY2835219, a potent oral inhibitor of the cyclin-dependent kinases 4 and 6 (CDK4/6) that crosses the blood-brain barrier and demonstrates in vivo activity against intracranial human brain tumor xenografts.

(2012) C. Sanchez-Martinez et al.   MOLECULAR CANCER THERAPEUTICS

Cdk4/6 Inhibition Induces Epithelial-Mesenchymal Transition and Enhances Invasiveness in Pancreatic Cancer Cells

(2012) F. Liu et al.   MOLECULAR CANCER THERAPEUTICS

Cyclin E2 Overexpression Is Associated with Endocrine Resistance but not Insensitivity to CDK2 Inhibition in Human Breast Cancer Cells

(2012) C. E. Caldon et al.   MOLECULAR CANCER THERAPEUTICS

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

Oncogenic NRAS signaling differentially regulates survival and proliferation in melanoma

(2012) Lawrence N Kwong et al.   NATURE MEDICINE

p16-Cdk4-Rb axis controls sensitivity to a cyclin-dependent kinase inhibitor PD0332991 in glioblastoma xenograft cells

(2012) L. Cen et al.   NEURO-ONCOLOGY

Phase I study of PD 0332991, a cyclin-dependent kinase inhibitor, administered in 3-week cycles (Schedule 2/1)

(2011) G K Schwartz et al.   BRITISH JOURNAL OF CANCER

Early G1 Cyclin-Dependent Kinases as Prognostic Markers and Potential Therapeutic Targets in Esophageal Adenocarcinoma

(2011) A. Ismail et al.   CLINICAL CANCER RESEARCH

Phase I, Dose-Escalation Trial of the Oral Cyclin-Dependent Kinase 4/6 Inhibitor PD 0332991, Administered Using a 21-Day Schedule in Patients with Advanced Cancer

(2011) K. T. Flaherty et al.   CLINICAL CANCER RESEARCH

Expression of p16 and Retinoblastoma Determines Response to CDK4/6 Inhibition in Ovarian Cancer

(2011) Gottfried E. Konecny et al.   CLINICAL CANCER RESEARCH

Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer

(2011) C. Thangavel et al.   ENDOCRINE-RELATED CANCER

ER -Dependent E2F Transcription Can Mediate Resistance to Estrogen Deprivation in Human Breast Cancer

(2011) T. W. Miller et al.   Cancer Discovery

Molecular characterization of a t(2;7) translocation linking CDK6 to the IGK locus in CD5− monoclonal B-cell lymphocytosis

(2011) Edward Parker et al.   Cancer Genetics

A Synthetic Lethal Interaction between K-Ras Oncogenes and Cdk4 Unveils a Therapeutic Strategy for Non-small Cell Lung Carcinoma

(2010) Marta Puyol et al.   CANCER CELL

Pharmacologic Inhibition of Cyclin-Dependent Kinases 4 and 6 Arrests the Growth of Glioblastoma Multiforme Intracranial Xenografts

(2010) K. Michaud et al.   CANCER RESEARCH

RB-pathway disruption in breast cancer

(2010) Adam Ertel et al.   CELL CYCLE

Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies

(2010) Christophe Le Tourneau et al.   EUROPEAN JOURNAL OF CANCER

Proliferative Suppression by CDK4/6 Inhibition: Complex Function of the Retinoblastoma Pathway in Liver Tissue and Hepatoma Cells

(2010) Dayana B. Rivadeneira et al.   GASTROENTEROLOGY

Subtype-specific genomic alterations define new targets for soft-tissue sarcoma therapy

(2010) Jordi Barretina et al.   NATURE GENETICS

Pattern of retinoblastoma pathway inactivation dictates response to CDK4/6 inhibition in GBM

(2010) W. R. Wiedemeyer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phase I Study of Flavopiridol with Oxaliplatin and Fluorouracil/Leucovorin in Advanced Solid Tumors

(2009) D. Rathkopf et al.   CLINICAL CANCER RESEARCH

Clinical and Biological Significance of CDK4 Amplification in Well-Differentiated and Dedifferentiated Liposarcomas

(2009) A. Italiano et al.   CLINICAL CANCER RESEARCH

Cell cycle kinases as therapeutic targets for cancer

(2009) Silvia Lapenna et al.   NATURE REVIEWS DRUG DISCOVERY

Treatment of Growing Teratoma Syndrome

(2009) David J. Vaughn et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Novel Therapeutic Combination Using PD 0332991 and Bortezomib: Study in the 5T33MM Myeloma Model

(2008) E. Menu et al.   CANCER RESEARCH

HMGA2 is the partner of MDM2 in well-differentiated and dedifferentiated liposarcomas whereas CDK4 belongs to a distinct inconsistent amplicon

(2008) Antoine Italiano et al.   INTERNATIONAL JOURNAL OF CANCER

Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas

(2008) K. S.M. Smalley et al.   MOLECULAR CANCER THERAPEUTICS

CDK8 is a colorectal cancer oncogene that regulates β-catenin activity

(2008) Ron Firestein et al.   NATURE

An Integrated Genomic Analysis of Human Glioblastoma Multiforme

(2008) D. W. Parsons et al.   SCIENCE