Profile of palbociclib in the treatment of metastatic breast cancer

Moataz Ehab,1 Mohamad Elbaz2,31Department of Pharmacy Practice, 2Department of Pharmacology, Pharmacy School, Helwan University, Egypt; 3Department of Pathology, The Comprehensive Cancer Center, The Ohio State University Wexner Medical Center, Columbus, OH, USAAbstract: Breast cancer is the...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Ehab M, Elbaz M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Cyclin Dependent kinases cell cycle metastatic breast cancer PD0332991 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/0a6c90fb114d48eaa1ea6c231d4e5709
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:0a6c90fb114d48eaa1ea6c231d4e5709
record_format	dspace
spelling	oai:doaj.org-article:0a6c90fb114d48eaa1ea6c231d4e57092021-12-02T06:15:23ZProfile of palbociclib in the treatment of metastatic breast cancer1179-1314https://doaj.org/article/0a6c90fb114d48eaa1ea6c231d4e57092016-05-01T00:00:00Zhttps://www.dovepress.com/profile-of-palbociclib-in-the-treatment-of-metastatic-breast-cancer-peer-reviewed-article-BCTThttps://doaj.org/toc/1179-1314Moataz Ehab,1 Mohamad Elbaz2,31Department of Pharmacy Practice, 2Department of Pharmacology, Pharmacy School, Helwan University, Egypt; 3Department of Pathology, The Comprehensive Cancer Center, The Ohio State University Wexner Medical Center, Columbus, OH, USAAbstract: Breast cancer is the most common cancer diagnosed in women. Each year, thousands die either because of disease progression or failure of treatment. Breast cancer is classified into different subtypes based on the molecular expression of estrogen receptor (ER), progesterone receptor, and/or human epidermal growth factor receptor 2 (HER2). These receptors represent important therapeutic targets either through monoclonal antibodies or through small-molecule inhibitors directed toward them. However, up to 40% of patients develop either a primary or a secondary resistance to the current treatments. Therefore, there is an urgent need for investigating new targets in order to overcome the resistance and/or enhance the current therapies. Cell cycle is altered in many human cancers, especially in breast cancer. Cyclin-dependent kinases (CDKs), especially CDK4 and CDK6, play a pivotal role in cell cycle progression that makes them potential targets for new promising therapies. CDK inhibition has shown strong antitumor activities, ranging from cytostatic antiproliferative effects to synergistic effects in combination with other antitumor drugs. In order to overcome the drawbacks of the first-generation CDK inhibitors, recently, new CDK inhibitors have emerged that are more selective to CDK4 and CDK6 such as palbociclib, which is the most advanced CDK4/6 inhibitor in trials. In preclinical studies, palbociclib has shown a very promising antitumor activity, especially against ERα+ breast cancer subtype. Palbociclib has gained world attention, and US the Food and Drug Administration has accelerated its approval for first-line treatment in combination with letrozole for the first-line systematic treatment of postmenopausal women with ERα+/HER2− locally advanced or metastatic breast cancer. In this review, we discuss the potential role of CDK inhibition in breast cancer treatment, and focus on palbociclib progress from preclinical studies to clinical trials with mentioning the most recent ongoing as well as planned Phase II and Phase III trials of palbociclib in advanced breast cancer.Keywords: cyclin-dependent kinases, cell cycle, metastatic breast cancer, PD0332991Ehab MElbaz MDove Medical PressarticleCyclin Dependent kinasescell cyclemetastatic breast cancerPD0332991Neoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENBreast Cancer: Targets and Therapy, Vol 2016, Iss Issue 1, Pp 83-91 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Cyclin Dependent kinases cell cycle metastatic breast cancer PD0332991 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	Cyclin Dependent kinases cell cycle metastatic breast cancer PD0332991 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Ehab M Elbaz M Profile of palbociclib in the treatment of metastatic breast cancer
description	Moataz Ehab,1 Mohamad Elbaz2,31Department of Pharmacy Practice, 2Department of Pharmacology, Pharmacy School, Helwan University, Egypt; 3Department of Pathology, The Comprehensive Cancer Center, The Ohio State University Wexner Medical Center, Columbus, OH, USAAbstract: Breast cancer is the most common cancer diagnosed in women. Each year, thousands die either because of disease progression or failure of treatment. Breast cancer is classified into different subtypes based on the molecular expression of estrogen receptor (ER), progesterone receptor, and/or human epidermal growth factor receptor 2 (HER2). These receptors represent important therapeutic targets either through monoclonal antibodies or through small-molecule inhibitors directed toward them. However, up to 40% of patients develop either a primary or a secondary resistance to the current treatments. Therefore, there is an urgent need for investigating new targets in order to overcome the resistance and/or enhance the current therapies. Cell cycle is altered in many human cancers, especially in breast cancer. Cyclin-dependent kinases (CDKs), especially CDK4 and CDK6, play a pivotal role in cell cycle progression that makes them potential targets for new promising therapies. CDK inhibition has shown strong antitumor activities, ranging from cytostatic antiproliferative effects to synergistic effects in combination with other antitumor drugs. In order to overcome the drawbacks of the first-generation CDK inhibitors, recently, new CDK inhibitors have emerged that are more selective to CDK4 and CDK6 such as palbociclib, which is the most advanced CDK4/6 inhibitor in trials. In preclinical studies, palbociclib has shown a very promising antitumor activity, especially against ERα+ breast cancer subtype. Palbociclib has gained world attention, and US the Food and Drug Administration has accelerated its approval for first-line treatment in combination with letrozole for the first-line systematic treatment of postmenopausal women with ERα+/HER2− locally advanced or metastatic breast cancer. In this review, we discuss the potential role of CDK inhibition in breast cancer treatment, and focus on palbociclib progress from preclinical studies to clinical trials with mentioning the most recent ongoing as well as planned Phase II and Phase III trials of palbociclib in advanced breast cancer.Keywords: cyclin-dependent kinases, cell cycle, metastatic breast cancer, PD0332991
format	article
author	Ehab M Elbaz M
author_facet	Ehab M Elbaz M
author_sort	Ehab M
title	Profile of palbociclib in the treatment of metastatic breast cancer
title_short	Profile of palbociclib in the treatment of metastatic breast cancer
title_full	Profile of palbociclib in the treatment of metastatic breast cancer
title_fullStr	Profile of palbociclib in the treatment of metastatic breast cancer
title_full_unstemmed	Profile of palbociclib in the treatment of metastatic breast cancer
title_sort	profile of palbociclib in the treatment of metastatic breast cancer
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/0a6c90fb114d48eaa1ea6c231d4e5709
work_keys_str_mv	AT ehabm profileofpalbociclibinthetreatmentofmetastaticbreastcancer AT elbazm profileofpalbociclibinthetreatmentofmetastaticbreastcancer
_version_	1718399975260422144

Profile of palbociclib in the treatment of metastatic breast cancer

Ejemplares similares