Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated.

2022年11月14日 · These data suggest that VIP152 is a highly selective inhibitor of CDK9 that represents an attractive new therapy for CLL. Chronic lymphocytic leukemia (CLL) is a genetically heterogeneous disease...

VIP152 induced cell death in CLL cell lines and primary patient samples. Transcriptome analysis revealed inhibition of RNA degradation through the AU-Rich Element (ARE) dysregulation. Mechanistically, VIP152 inhibits the assembly of P-TEFb onto the transcription machinery and disturbs binding partners.

2021年11月5日 · VIP152 is a highly specific inhibitor of CDK9 - considered the most important CDK kinase member for CLL clinical activity. VIP152 has favorable pharmacokinetic properties and has demonstrated durable, preliminary single-agent clinical activity in double-hit diffuse large B-cell lymphoma.

(+)-Enitociclib ( (+)-BAY-1251152) 是 BAY-1251152 的一个对映体，旋光性为 (+)。 (+)-Enitociclib 是一种有效的选择性 CDK9 抑制剂， IC50 为 3 nM。 (+)-Enitociclib 具有抗肿瘤活性。 * Please select Quantity before adding items. • Acta Pharm Sin B. 2023 May 26. • Oncotarget. 2023 Dec 20:14:997-1008. [Abstract]

2022年11月15日 · Enitociclib (VIP152/formerly BAY1251152) Is a Selective and Active CDK9 Inhibitor : Preliminary Safety and Early Signs of Efficacy in Patients with Non-Hodgkin Lymphoma (NHL) and Chronic Lymphocytic Leukemia (CLL)

These data suggest that VIP152 is a highly selective inhibitor of CDK9 that represents an attractive new therapy for CLL. Chronic lymphocytic leukemia (CLL) is a genetically heteroge-neous...

2021年5月28日 · VIP152 (formerly BAY 1251152), a potent and highly selective CDK9 inhibitor, has been evaluated in a Phase 1 dose-escalation study in patients with advanced cancer. The maximum tolerated dose was 30 mg once weekly administered in consecutive 21-day cycles, based on neutropenia as the dose-limiting toxicity (JCO 2018;36:2507; NCT02635672).

2015年12月17日 · 一项开放标签、多中心 I 期剂量递增研究，以表征 VIP152 (BAY 1251152) 的安全性、耐受性、初步抗肿瘤活性、药代动力学和最大耐受剂量作为晚期癌症受试者的单一疗法或联合疗法。 确定 VIP152 (BAY 1251152) 作为单一疗法或联合疗法在实体瘤和侵袭性非霍奇金淋巴瘤 (NHL) 患者中的安全性、耐受性、药代动力学、最大耐受剂量 (MTD) 和推荐的 2 期剂量 (RP2D)。 第 2 部分 VIP152 单一疗法（全球）。 第 3 部分 VIP152 与 pembrolizumab 联合用药的剂量 …

2021年11月5日 · VIP152 is a well-tolerated and clinically active CDK9 inhibitor leading to complete metabolic remissions in 2/7 HGBL patients treated with once weekly (QW) 30 mg intravenous administration (Lücking et al. J Med Chem …