2017年7月1日 · Here, we describe the mechanism of action of ribociclib and review preclinical and clinical data from phase I, II, and III trials of ribociclib across different tumor types, within the context of other selective CDK4/6 inhibitors.

2017年3月13日 · 对LEQ803的Cmax和AUC (一种显著的代谢物LEE011，占母体暴露的低于10%)分别减低96%和98%。 一种中度的CYP3A4抑制剂(红霉素[erythromycin]) 被预计增加ribociclib的Cmax和AUC分别1.3-倍和1.9-倍。

2017年7月2日 · Three selective CDK4/6 inhibitors are in late-stage clinical development: ribociclib (LEE011; Novartis), palbociclib (Ibrance; PD-0332991; Pfizer), and abemaciclib (LY-2835219; Eli Lilly). Palbociclib combined with letrozole or fulvestrant has demonstrated efficacy in patients with HR + advanced breast cancer (ABC; Table 1 ; refs.

placebo-controlled study of LEE011 (ribociclib) or placebo in combination with tamoxifen and goserelin or a non-steroidal aromatase inhibitor (NSAI) and goserelin for the treatment of premenopausal women with hormone receptor positive, HER2-negative, advanced breast cancer.

2016年11月3日 · Ribociclib (LEE011) is an orally bioavailable, selective, small-molecule inhibitor of CDK4/6 that blocks the phosphorylation of retinoblastoma protein, thereby preventing cell-cycle...

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC 50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Ribociclib is a selective, orally bioavailable inhibitor of CDK4 and CDK6, which was granted priority review by the US Food and Drug Administration in November 2016, and is set to enter the treatment landscape alongside other CDK4/6 inhibitors, including palbociclib and abemaciclib.

2016年8月3日 · LEE011 is a selective cyclin dependent kinase (CDK4/6) inhibitor. The Breakthrough Therapy designation is based primarily on positive results of the Phase III MONALEESA-2 trial of LEE011 in combination with letrozole in postmenopausal women who had received no prior therapy for their advanced disease[1].

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC 50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

2017年5月15日 · Purpose: The cyclin-dependent kinase (CDK) 4/6 inhibitor, ribociclib (LEE011), displayed preclinical activity in neuroblastoma and malignant rhabdoid tumor (MRT) models. In this phase I study, the maximum tolerated dose (MTD) and recommended phase II dose (RP2D), safety, pharmacokinetics (PK), and preliminary activity of single-agent ribociclib ...