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Romualdo Barroso-Sousa, Geoffrey I Shapiro, Sara M Tolaney
Clinical and preclinical data support a significant role for inhibitors of the cyclin-dependent kinases (CDKs) 4 and 6 in the treatment of patients with breast cancer. Recently, based on data showing improvement in progression-free survival, the use of palbociclib (Ibrance; Pfizer, Inc.) in combination with endocrine agents was approved to treat patients with hormone receptor-positive advanced disease. Importantly, 2 other CDK4/6 inhibitors, abemaciclib (LY2835219; Lilly) and ribociclib (LEE011; Novartis), are in the late stage of clinical development...
June 2016: Breast Care
Jessica L F Teh, Timothy J Purwin, Evan J Greenawalt, Inna Chervoneva, Allison Goldberg, Michael A Davies, Andrew E Aplin
Aberrant cell-cycle progression is a hallmark feature of cancer cells. Cyclin-dependent kinases 4 and 6 (CDK4/6) drive progression through the G1 stage of the cell cycle, at least in part, by inactivating the tumor suppressor, retinoblastoma. CDK4/6 are targetable and the selective CDK4/6 inhibitor, palbociclib, was recently FDA approved for the treatment of estrogen receptor-positive, HER2-negative advanced breast cancer. In cutaneous melanoma, driver mutations in NRAS and BRAF promote CDK4/6 activation, suggesting that inhibitors such as palbociclib are likely to provide therapeutic benefit in combination with BRAF inhibitors and/or MEK inhibitors that are FDA-approved...
September 15, 2016: Cancer Research
Amanda J Walker, Suparna Wedam, Laleh Amiri-Kordestani, Erik Bloomquist, Shengui Tang, Rajeshwari Sridhara, Wei Chen, Todd R Palmby, Jeanne Fourie Zirkelbach, Wentao Fu, Qi Liu, Amy Tilley, Geoffrey Kim, Paul G Kluetz, Amy E McKee, Richard Pazdur
On February 19, 2016, the FDA approved palbociclib (Ibrance, Pfizer) for use in combination with fulvestrant (Faslodex, AstraZeneca) for the treatment of women with hormone receptor (HR)-positive, HER2-negative advanced or metastatic breast cancer (MBC) with disease progression following endocrine therapy. The approval was based on the results of a randomized, double-blind, placebo-controlled trial conducted in 521 pre- and postmenopausal women with HR-positive, HER2-negative advanced or MBC. Patients were randomized (2:1) to receive palbociclib plus fulvestrant (n = 347) or placebo plus fulvestrant (n = 174)...
July 12, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Robert Roskoski
Cyclins and cyclin-dependent protein kinases (CDKs) are important regulatory components that are required for cell cycle progression. The levels of the cell cycle CDKs are generally constant and their activities are controlled by cyclins, proteins whose levels oscillate during each cell cycle. Additional CDK family members were subsequently discovered that play significant roles in a wide range of activities including the control of gene transcription, metabolism, and neuronal function. In response to mitogenic stimuli, cells in the G1 phase of the cell cycle produce cyclins of the D type that activate CDK4/6...
May 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Julia A Beaver, Laleh Amiri-Kordestani, Rosane Charlab, Wei Chen, Todd Palmby, Amy Tilley, Jeanne Fourie Zirkelbach, Jingyu Yu, Qi Liu, Liang Zhao, Joyce Crich, Xiao Hong Chen, Minerva Hughes, Erik Bloomquist, Shenghui Tang, Rajeshwari Sridhara, Paul G Kluetz, Geoffrey Kim, Amna Ibrahim, Richard Pazdur, Patricia Cortazar
On February 3, 2015, the FDA granted accelerated approval to palbociclib (IBRANCE, Pfizer Inc.), an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), for use in combination with letrozole for the treatment of postmenopausal women with estrogen receptor (ER)-positive, HER2-negative advanced breast cancer as initial endocrine-based therapy for their metastatic disease. The approval is based on a randomized, multicenter, open-label phase I/II trial (PALOMA-1) in 165 patients randomized to palbociclib (125 mg orally daily for 21 consecutive days, followed by 7 days off treatment) plus letrozole (2...
November 1, 2015: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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August 17, 2015: Medical Letter on Drugs and Therapeutics
Thomas J Raub, Graham N Wishart, Palaniappan Kulanthaivel, Brian A Staton, Rose T Ajamie, Geri A Sawada, Lawrence M Gelbert, Harlan E Shannon, Concepcion Sanchez-Martinez, Alfonso De Dios
Effective treatments for primary brain tumors and brain metastases represent a major unmet medical need. Targeting the CDK4/CDK6-cyclin D1-Rb-p16/ink4a pathway using a potent CDK4 and CDK6 kinase inhibitor has potential for treating primary central nervous system tumors such as glioblastoma and some peripheral tumors with high incidence of brain metastases. We compared central nervous system exposures of two orally bioavailable CDK4 and CDK6 inhibitors: abemaciclib, which is currently in advanced clinical development, and palbociclib (IBRANCE; Pfizer), which was recently approved by the U...
September 2015: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Todd VanArsdale, Chris Boshoff, Kim T Arndt, Robert T Abraham
Cancer cells bypass normal controls over mitotic cell-cycle progression to achieve a deregulated state of proliferation. The retinoblastoma tumor suppressor protein (pRb) governs a key cell-cycle checkpoint that normally prevents G1-phase cells from entering S-phase in the absence of appropriate mitogenic signals. Cancer cells frequently overcome pRb-dependent growth suppression via constitutive phosphorylation and inactivation of pRb function by cyclin-dependent kinase (CDK) 4 or CDK6 partnered with D-type cyclins...
July 1, 2015: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Kunj Gohil
Palbociclib (Ibrance) for breast cancer, secukinumab (Cosentyx) for plaque psoriasis, meningococcal group B vaccine (Bexsero) to help prevent meningitis, and lenvatinib (Lenvima) for differentiated thyroid cancer.
April 2015: P & T: a Peer-reviewed Journal for Formulary Management
Sohita Dhillon
Palbociclib (IbranceĀ®) is an oral, reversible, selective, small-molecule inhibitor of cyclin-dependent kinases (CDK) 4 and CDK6 developed by Pfizer for the treatment of cancer. CDKs are important modulators of cell cycle entry and progression in response to growth signals, and inhibition of these kinases with palbociclib could enhance the activity of other anticancer drugs in tolerable regimens. Palbociclib, in combination with letrozole, was recently approved in the US for the first-line treatment of advanced breast cancer...
April 2015: Drugs
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