Drug intelligence / Profile preview

BG-75098

Development stage
Phase 1
Lead developer
BeOne Medicines
Modality
Small Molecules
Administration
Oral
01

Overview

**BG-75098** is an investigational oral small molecule developed by BeOne Medicines as a selective **CDK2 degrader** (termed CDAC, chimaeric degradation activation compound) for advanced solid tumors. It promotes the degradation of **cyclin-dependent kinase 2 (CDK2)**, a protein critical for cancer cell proliferation, offering potentially superior selectivity over CDK2 inhibitors (e.g., improved CDK2 vs. CDK1 selectivity) to overcome resistance mechanisms in tumors dependent on CDK2 activity, such as those with RB1 wild-type status. Currently in Phase 1 dose escalation/expansion (NCT07226349), evaluating safety, tolerability, PK/PD, and preliminary antitumor activity as monotherapy and in combination with BGB-43395 (CDK4 inhibitor) + fulvestrant, with early preclinical data supporting entry into clinic by end-2025.[1][2][5][7][9][14][15]

02

Targets

CDK2 (Cyclin-dependent kinase 2)

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