BeOne Medicines initiates US phase I trial for CDK2 PROTAC

On November 10, 2025, BeOne Medicines (formerly BeiGene) registered an international Phase I  trial of BG-75098, as a monotherapy and in combination, for advanced solid tumors on ClinicalTrials.gov.

This Phase I clinical trial plans to enroll 105 patients with advanced solid tumors.

The combination therapy regimen includes the combination of CDK4 inhibitor BGB-43395 and fulvestrant.

According to disclosures from BeOne Medicines' 2025 R&D Day, BG-75098 is a novel CDK2-targeting degrader (CDAC) and a potential first-in-class CDK2 degrader, demonstrating superior potency, selectivity, and pharmacokinetic (PK) properties.

BeOne Medicines is leveraging its leading CDAC technology platform to tackle key drug discovery challenges, including avoiding tissue-specific toxicity, overcoming insufficient potency, breaking through undruggability, enhancing selectivity, disrupting scaffolding functions, and reducing on-target resistance.

BeOne Medicines is positioning its CDK2 CDAC as another potential cornerstone asset in breast and gynecological cancers, despite its existing portfolio of selective CDK4 and CDK2 inhibitors.

Summary

BeOne Medicines has placed a heavy strategic focus on CDACs within its small molecule portfolio, having built a pipeline of over 20 assets. Key CDAC programs that have entered clinical stages include those targeting EGFR, BTK, IRAK4, and CDK2. In the large molecule arena, the company is concentrating its efforts on ADCs, with a particular emphasis on next-generation bispecific ADCs and those conjugated with novel payloads.