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 …

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 …

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; …

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 …

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 …

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 …

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 …

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 …

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 …

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 …