BMS-986463 / BMS - LARVOL DELTA

Discovery and characterization of a clinical-stage molecular glue degrader of WEE1 kinase, BMS-986463, for the treatment of advanced solid tumors (AACR-NCI-EORTC 2025) - "Targeted protein degradation has achieved clinical successes in hematologic malignancies with approvals of lenalidomide, pomalidomide, and thalidomide. Multiple mouse and rat xenograft studies demonstrated robust tumor efficacy and a clear PK/PD/efficacy relationship with sustained WEE1 degradation and phospho-CDK2 reduction. Herein, we report the discovery campaign resulting in BMS-986463, a first-in-class WEE1 CELMoD™ currently undergoing Phase I clinical investigation in advanced solid tumors."

Clinical • Metastases • Hematological Malignancies • Oncology • Solid Tumor • CRBN • DDB1 • IKZF1 • IKZF3

Discovery of a first-in-class molecular glue degrader of WEE1 kinase, BMS-986463, for the treatment of advanced malignant solid tumors (ACS-Fall 2025) - "Co-sponsor - Nominal - MEDI: Division of Medicinal Chemistry; Co-sponsor - Nominal - CHAS: Division of Chemical Health and Safety.Targeted protein degradation has achieved clinical successes in hematologic malignancies with approvals of the immunomodulatory imide drugs (IMiD™) lenalidomide, pomalidomide, and thalidomide. Multiple mouse and rat xenograft studies demonstrated robust tumor efficacy and a clear PK/PD/efficacy relationship with sustained WEE1 degradation and phospho-CDK2 reduction. Herein, we report the discovery campaign resulting in BMS-986463, a first-in-class WEE1 CELMoD™ currently undergoing Phase I clinical investigation in advanced solid tumors."

Metastases • Hematological Malignancies • Oncology • Solid Tumor • Targeted Protein Degradation • CRBN • DDB1 • IKZF1 • IKZF3

A Study to Evaluate the Safety, Tolerability, and Efficacy of Escalating Doses of BMS-986463 in Participants With Select Advanced Malignant Tumors. (clinicaltrials.gov) - P1 | N=240 | Recruiting | Sponsor: Bristol-Myers Squibb | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Endometrial Serous Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Solid Tumor • Uterine Cancer

A Study to Evaluate the Safety, Tolerability, and Efficacy of Escalating Doses of BMS-986463 in Participants With Select Advanced Malignant Tumors. (clinicaltrials.gov) - P1 | N=240 | Not yet recruiting | Sponsor: Bristol-Myers Squibb

Metastases • New P1 trial • Endometrial Serous Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Solid Tumor • Uterine Cancer