Journal ArticleDOI
Cyclin-Dependent Kinase 4/6 Inhibitors for the Treatment of Breast Cancer: A Review of Preclinical and Clinical Data
Neelima Vidula,Hope S. Rugo +1 more
TLDR
The mechanism of action of CDK 4/6 inhibitors, preclinical studies on their efficacy, ongoing clinical trials in breast cancer, and toxicity profiles are reviewed.About:
This article is published in Clinical Breast Cancer.The article was published on 2016-02-01. It has received 81 citations till now. The article focuses on the topics: Palbociclib & Breast cancer.read more
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Cardiovascular Disease and Breast Cancer: Where These Entities Intersect: A Scientific Statement From the American Heart Association.
Laxmi S. Mehta,Karol E. Watson,Ana Barac,Theresa M. Beckie,Vera Bittner,Salvador Cruz-Flores,Susan Dent,Lavanya Kondapalli,Bonnie Ky,Tochukwu M. Okwuosa,Ileana L. Piña,Annabelle Santos Volgman +11 more
TL;DR: This document will provide a comprehensive overview of the prevalence of these diseases, shared risk factors, the cardiotoxic effects of therapy, and the prevention and treatment of CVD in breast cancer patients.
Journal ArticleDOI
MONARCH 1, A Phase II Study of Abemaciclib, a CDK4 and CDK6 Inhibitor, as a Single Agent, in Patients with Refractory HR+/HER2− Metastatic Breast Cancer
Maura N. Dickler,Sara M. Tolaney,Hope S. Rugo,Javier Cortes,Véronique Diéras,Debra A. Patt,Debra A. Patt,Hans Wildiers,Clifford A. Hudis,Joyce O'Shaughnessy,Esther Zamora,Denise A. Yardley,Martin Frenzel,Andrew Koustenis,José Baselga +14 more
TL;DR: In this poor-prognosis, heavily pretreated population with refractory HR+/HER2− metastatic breast cancer, continuous dosing of single-agent abemaciciclib was well tolerated and exhibited promising clinical activity.
Journal ArticleDOI
Endocrine Therapy for Hormone Receptor–Positive Metastatic Breast Cancer: American Society of Clinical Oncology Guideline
Hope S. Rugo,R. Bryan Rumble,Erin Macrae,Debra L. Barton,Hannah Klein Connolly,Maura N. Dickler,Lesley Fallowfield,Barbara Fowble,James N. Ingle,Mohammad Jahanzeb,Stephen R. D. Johnston,Larissa A. Korde,James Khatcheressian,Rita S. Mehta,Hyman B. Muss,Harold J. Burstein +15 more
TL;DR: This guideline puts forth recommendations for endocrine therapy as treatment for women with HR-positive MBC, and aromatase inhibitors (AIs) are the preferred first-line endocrine Therapy, with or without the cyclin-dependent kinase inhibitor palbociclib.
Journal ArticleDOI
Spectrum and Degree of CDK Drug Interactions Predicts Clinical Performance
Ping Chen,Nathan V. Lee,Wenyue Hu,Meirong Xu,Rose Ann Ferre,Hieu Lam,Simon Bergqvist,James Solowiej,Wade Diehl,You-Ai He,Xiu Yu,Asako Nagata,Todd VanArsdale,Brion W. Murray +13 more
TL;DR: Therapeutically targeting aberrant intracellular kinase signaling is attractive from a biological perspective but drug development is often hindered by toxicities and inadequate efficacy, so understanding the molecular components of potency and selectivity facilitates rational design of future generations of kinase-directed drugs.
Journal ArticleDOI
Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs.
TL;DR: Owing to their role in cell proliferation, CDKs represent natural targets for anticancer therapies and one of their most common toxicities is myelosuppression with decreased neutrophil production.
References
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Journal ArticleDOI
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
Richard S. Finn,John Crown,István Láng,Katalin Boér,Igor Bondarenko,Sergey O. Kulyk,Johannes Ettl,Ravindranath Patel,Tamás Pintér,Marcus Schmidt,Yaroslav Shparyk,Anu Thummala,Nataliya L. Voytko,Camilla Fowst,Xin Huang,Sindy T. Kim,Sophia Randolph,Dennis J. Slamon +17 more
TL;DR: Palbociclib (PD-0332991) is an oral, small-molecule inhibitor of cyclin-dependent kinases (CDKs) 4 and 6 with preclinical evidence of growth-inhibitory activity in oestrogen receptor-positive breast cancer cells and synergy with anti-oestrogens as mentioned in this paper.
Journal ArticleDOI
PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro
Richard S. Finn,Judy Dering,Dylan Conklin,Ondrej Kalous,David Cohen,Amrita J. Desai,Charles Ginther,Mohammad Atefi,Isan Chen,Camilla Fowst,Gerret Los,Dennis J. Slamon +11 more
TL;DR: A role for CDK4/6 inhibition in some breast cancers is suggested and criteria for patient selection in clinical studies of PD 0332991 is identified.
Journal Article
Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts
David W. Fry,Patricia J. Harvey,Paul R. Keller,William Elliott,Maryanne Meade,Erin Trachet,Mudher Albassam,Xianxian Zheng,Wilbur R. Leopold,Nancy Pryer,Peter L. Toogood +10 more
TL;DR: Results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors.
Journal ArticleDOI
Palbociclib in Hormone-Receptor–Positive Advanced Breast Cancer
Nicholas C. Turner,Jungsil Ro,Fabrice Andre,Sherene Loi,Sunil Verma,Hiroji Iwata,Nadia Harbeck,Sibylle Loibl,Cynthia Huang Bartlett,Ke Zhang,Carla Giorgetti,Sophia Randolph,Maria Koehler,Massimo Cristofanilli,Massimo Cristofanilli +14 more
TL;DR: Among patients with hormone-receptor-positive metastatic breast cancer who had progression of disease during prior endocrine therapy, palbociclib combined with fulvestrant resulted in longer progression-free survival than fulvestrants alone.
Journal ArticleDOI
Estrogen-induced activation of Cdk4 and Cdk2 during G1-S phase progression is accompanied by increased cyclin D1 expression and decreased cyclin-dependent kinase inhibitor association with cyclin E-Cdk2.
Owen W. J. Prall,Boris Sarcevic,Elizabeth A. Musgrove,Colin K. W. Watts,Robert L. Sutherland +4 more
TL;DR: The treatment of MCF-7 breast cancer cells with the pure estrogen antagonist ICI 182780 is treated to inhibit estrogen-induced gene expression and induce G1 phase arrest to provide an explanation for the early activation of both cyclin D1-Cdk4 and cyclin E-C DK2 complexes that accompany G1-S phase progression in response to estradiol.