2023年3月1日 · XL102 is a potent, orally bioavailable, highly selective covalent CDK7 inhibitor. QUARTZ-101 is a first-in-human, open-label trial (NCT04726332) evaluating the safety, tolerability, and optimal dose of XL102 as a single agent and in combination regimens in patients with solid tumors, with expansion in subsequent tumor cohorts of advanced HR+ BC ...

2022年6月2日 · In the dose-escalation stage (modified interval 3+3 design), a maximum tolerated dose and/or recommended dose (MTD/RD) of XL102 will be established (primary endpoint) for use alone (solid tumors) and then for use in combination with standard dose fulvestrant (HR+BC) or abiraterone/prednisone (mCRPC); dose escalation will require ̃36 pts for ...

2023年7月29日 · • XL102 is a novel, highly specific, orally bioavailable covalent inhibitor of CDK7 • CDK7 inhibition induces cell cycle arrest and apoptosis via CDK7/c-Myc/p53 axis in AML • XL102 synergizes with Venetoclax in AML

2023年7月29日 · The data suggests XL102 induces apoptosis in AML cells via CDK7/c-Myc/p53 axis. RNA-sequencing from paired Venetoclax-sensitive and Venetoclax-resistant cells treated with XL102 showed downregulation of genes involved in proliferation and apoptosis.

2022年2月15日 · XL102 induced cell death in a number of cancer cell lines and caused tumor regression in murine xenograft models of multiple tumor types including HR+ BC and TNBC. Here, we present the study design of an ongoing phase 1 trial in solid tumors which includes cohorts with advanced HR+ BC, TNBC, epithelial ovarian cancer (EOC), and metastatic ...

Background: XL102 is an orally bioavailable, selective, and covalent small-molecule inhibitor of cyclin-dependent kinase 7 (CDK7). CDK7 is a serine/threonine kinase that is overexpressed in multiple tumor types. CDK7 controls cell cycle progression via the phosphorylation of CDKs (1, 2, 4, and 6) and regu-

2021年10月26日 · 另一款进入临床阶段的CDK7抑制剂为XL102，它是一种选择性、口服生物可利用的共价CDK7抑制剂，由Exelixis公司从Aurigene公司引进。 2021年1月，Exelixis公司宣布启动XL102的1期临床，以评估其作为单药和与其它抗癌药联合治疗晚期或转移性实体瘤患者的安全性、 …

This is a Phase 1, open-label, dose-escalation and expansion study evaluating the safety, tolerability, PK, antitumor activity, and effect on biomarkers of XL102 administered orally alone and in multiple combination regimens to subjects with advanced solid tumors.

tps3176 背景： xl102 是一种可口服的、选择性的、共价的细胞周期蛋白依赖性激酶 7 (cdk7) 小分子抑制剂。cdk7 是一种在多种肿瘤类型中过度表达的丝氨酸/苏氨酸激酶。cdk7 通过 cdk（1、2、4 和 6）的磷酸化控制细胞周期进程，并通过 rna 聚合酶 ii 的磷酸化调节转录。

An orally bioavailable, selective inhibitor of cyclin-dependent kinase 7 (CDK7), with potential antineoplastic activity. Upon oral administration, CDK7 inhibitor XL102 selectively targets, covalently binds to and inhibits the activity of CDK7, thereby inhibiting CDK7-mediated signaling.