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A phase 1 dose-escalation and expansion-cohort study of the oral …
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 ...
Definition of CDK7 inhibitor XL102 - NCI Drug Dictionary - NCI
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.
Exelixis Announces Initial Dose-Escalation Results from the First-in ...
Sep 7, 2022 — XL102 is a potent, selective and orally bioavailable small molecule CDK7 inhibitor, which is an important regulator of the cellular transcriptional and cell cycle machinery. CDK7 helps regulate cell cycle progression, with overexpression observed in multiple cancers, such as breast, prostate and ovarian cancers.
Exelixis Announces Initiation of Phase 1 Trial Evaluating XL102 …
Jan 25, 2021 — XL102 is a potent, selective and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), an important regulator of the cell cycle that has been implicated in cancer.
Exelixis Announces Initiation of Phase 1 Trial Evaluating XL102 …
Jan 25, 2021 — XL102 is a potent, selective and orally bioavailable covalent inhibitor of CDK7, which is an important regulator of the cellular transcriptional and cell cycle machinery.
Abstract P4-01-35: A Phase 1 Study of the Oral CDK7 Inhibitor XL102 …
Mar 1, 2023 — 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 ...
Study of XL102 as Single-Agent and Combination Therapy in …
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.
Novel covalent CDK7 inhibitor potently induces apoptosis in acute ...
Jul 29, 2023 — • 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
Exelixis In-Licenses Aurigene’s Novel CDK7 Inhibitor and Files ...
Dec 7, 2020 — XL102 is a potent, selective, and orally bioavailable covalent inhibitor of cyclin-dependent kinase 7 (CDK7), which is an important regulator of the cellular transcriptional and...
- Some results have been removed