Palbociclib: A Novel Cyclin-Dependent Kinase Inhibitor for Hormone Receptor-Positive Advanced Breast Cancer

The Annals of Pharmacotherapy
Neha S ManginiMichael J Berger

Abstract

To review palbociclib, a novel small-molecule inhibitor of cyclin-dependent kinases 4 and 6, and its current place in therapy for the treatment of hormone receptor (HMR)-positive, human epidermal growth factor receptor 2 (Her2)-negative advanced breast cancer. Four phase I trials, 2 phase II trials, and 1 phase III trial were identified from May 2004 to May 2015 using PubMed, American Society of Clinical Oncology (ASCO) abstracts, and European Society of Medical Oncology (ESMO) abstracts. In the first-line setting, the phase II PALbociclib: Ongoing trials in the Management of breast cAncer (PALOMA)-1 trial randomized patients to receive letrozole alone or letrozole plus palbociclib 125 mg daily for 3 weeks, followed by 1 week off, as initial therapy for advanced breast cancer. The investigator-assessed median progression-free survival (PFS) was 20. 2 months for the combination versus 10.2 months for letrozole alone (hazard ratio [HR] = 0.488; 95% CI = 0.319-0.748; 1-sided P = 0.0004). The ensuing Food and Drug Administration approval of palbociclib was given a "breakthrough therapy" designation, where preliminary evidence suggests substantial improvement over existing therapies for a serious or life-threatening disease. A confi...Continue Reading

References

Nov 15, 2000·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·J M NabholtzM von Euler
Jun 13, 2001·Seminars in Oncology·A U Buzdar
Apr 11, 2006·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Geoffrey I Shapiro
Aug 26, 2009·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·John F R RobertsonMatthew J Ellis
Jun 26, 2010·The Journal of Clinical Investigation·Søren M JohnsonNorman E Sharpless
Jun 29, 2011·Annals of Oncology : Official Journal of the European Society for Medical Oncology·A GoldhirschUNKNOWN Panel members
Jul 8, 2011·Nature Reviews. Cancer·Elizabeth A MusgroveRobert L Sutherland
Nov 18, 2011·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Keith T FlahertyGary K Schwartz
Dec 14, 2011·The New England Journal of Medicine·José BaselgaGabriel N Hortobagyi
Feb 4, 2012·Journal of the National Cancer Institute·Patrick J RobertsNorman E Sharpless
Aug 3, 2012·The New England Journal of Medicine·Rita S MehtaGabriel N Hortobagyi
May 6, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Mark A Dickson
Nov 25, 2014·Pediatric Blood & Cancer·Kris Ann P SchultzDavid J Vaughn
Dec 17, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Angela DeMichelePeter O'Dwyer
Jan 28, 2015·Critical Reviews in Oncology/hematology·Palma FedeleSaverio Cinieri
Jun 2, 2015·The New England Journal of Medicine·Nicholas C TurnerUNKNOWN PALOMA3 Study Group

❮ Previous
Next ❯

Citations

Apr 20, 2017·Journal of Medicinal Chemistry·Andrew C FlickChristopher J O'Donnell
Mar 23, 2017·Critical Reviews in Oncology/hematology·Silvia Paola CoronaDaniele Generali
Apr 30, 2016·American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists·Jill Stein, Janelle Mann
Aug 2, 2019·American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists·Robert J Cersosimo
Nov 28, 2020·Journal of Advanced Nursing·Ann M Mazzella EbsteinMark Robson
Feb 4, 2016·Cancer Research·Christina Y YimMichael J Spinella

❮ Previous
Next ❯

Methods Mentioned

BETA
xenografts
contraception
biopsy

Clinical Trials Mentioned

NCT00721409
NCT01740427
NCT02297438
NCT02028507
NCT01864746
NCT02296801

Related Concepts

Related Feeds

Blood Brain Barrier

The blood brain barrier is a border that separates blood from cerebrospinal fluid. Discover the latest search on this highly selective semipermeable membrane here.

Cell Checkpoints & Regulators

Cell cycle checkpoints are a series of complex checkpoint mechanisms that detect DNA abnormalities and ensure that DNA replication and repair are complete before cell division. They are primarily regulated by cyclins, cyclin-dependent kinases, and the anaphase-promoting complex/cyclosome. Here is the latest research.

B-Cell Lymphoma

B-cell lymphomas include lymphomas that affect B cells. This subtype of cancer accounts for over 80% of non-Hodgkin lymphomas in the US. Here is the latest research.

Blood Brain Barrier Regulation in Health & Disease

The blood brain barrier is essential in regulating the movement of molecules and substances in and out of the brain. Disruption to the blood brain barrier and changes in permeability allow pathogens and inflammatory molecules to cross the barrier and may play a part in the pathogenesis of neurodegenerative disorders. Here is the latest research in this field.

Blood And Marrow Transplantation

The use of hematopoietic stem cell transplantation or blood and marrow transplantation (bmt) is on the increase worldwide. BMT is used to replace damaged or destroyed bone marrow with healthy bone marrow stem cells. Here is the latest research on bone and marrow transplantation.

Breast Invasive Carcinoma (Keystone)

Invasive breast cancers indicate a spread into breast tissues and lymph nodes. Here are the latest discoveries pertaining to breast invasive carcinomas.

Cancer Stem Cells in Glioblastoma

Glioblastoma is the most common and aggressive type of brain tumor. It contains a population of tumor initiating stem cell-like cells known as cancer stem cells. Investigations are ongoing into these cancer stem cells found in these solid tumors which are highly resistance to treatment. Here is the latest research on cancer stem cells in glioblastoma.

Breast Invasive Carcinoma

Invasive breast cancers indicate a spread into breast tissues and lymph nodes. Here are the latest discoveries pertaining to breast invasive carcinomas.

Anemia

Anemia develops when your blood lacks enough healthy red blood cells. Anemia of inflammation (AI, also called anemia of chronic disease) is a common, typically normocytic, normochromic anemia that is caused by an underlying inflammatory disease. Here is the latest research on anemia.

Blood Brain Barrier Chips

The blood brain barrier (BBB) is comprised of endothelial cells that regulate the influx and outflux of plasma concentrations. Lab-on-a-chip devices allow scientists to model diseases and mechanisms such as the passage of therapeutic antibodies across the BBB. Discover the latest research on BBB chips here.