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Triple negative breast cancer (TNBC) lacks specific drug targets and remains challenging. Palbociclib, a cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor is approved for metastatic estrogen receptor (ER)-positive and human epithermal growth factor 2 (HER2)-negative breast cancer. The nature of cell cycle inhibition by palbociclib suggests its potential in TNBC cells. Retinoblastoma (RB, a known substrate of CDK4/6) pathway deregulation is a frequent occurrence in TNBC and studies have revealed that pharmacological CDK4/6 inhibition induces a cooperative cytostatic effect with doxorubicin in RB-proficient TNBC models. In addition, recent studies reported that anti-androgen therapy shows preclinical efficacy in androgen-receptor (AR)-positive TNBC cells. Here we examined the effect of palbociclib in combination with an anti-androgen enzalutamide in TNBC cells.
This article was published in the following journal.
Name: PloS one
Palbociclib administered with endocrine therapy was tolerable when the overall incidence of toxicities was assessed separately for three PALOMA studies. This study analyzed pooled, longer-term PALOMA ...
Palbociclib is a cyclin-dependent kinase (CDK) 4 and 6 inhibitor that was conditionally approved in the United States (February 2015) and Canada (March 2016) with letrozole as initial endocrine-based ...
Palbociclib is an oral cyclin-dependent kinase 4/6 inhibitor, which is efficacious in treating breast cancer. Currently, there are numerous active clinical trials testing palbociclib alone or in combi...
Enzalutamide is a fast crystallizing, hydrophobic compound that has solubility limited absorption in vivo. Given the low aqueous solubility of this compound, it was of interest to evaluate amorphous f...
Outcome data on hormone receptor positive (HR), human epidermal growth factor receptor 2 (HER2) nonamplified (HER2) metastatic breast cancer (MBC) treated with palbociclib after treatment with everoli...
This is a multicenter, open label, Phase 1b study in patients with MBC. This study will have a dose escalation to identify the maximum tolerated dose (MTD) of the combination of gedatolisi...
This study is to evaluate preliminary efficacy of Ra-223 in combination with Enzalutamide in progressive CRPC patients with bone metastasis
The purpose of this trial is to test if the combination of enzalutamide and metformin in patients with castration resistant prostate cancer progressing on androgen deprivation therapy is m...
Since the amount of palbociclib eliminated in urine is 6.9%, renal impairment is not expected to have much impact on palbociclib. However, the Federal Drug Administration (FDA) Guidance r...
Primary Objectives: Dose Escalation: Part A (SAR439859 monotherapy); Part C (combination of SAR439859 with palbociclib) - To determine the maximum tolerated dose (MTD) and recom...
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Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...