BG-68501 / BeOne Medicines, Ensem Therap - LARVOL DELTA

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=258 | Recruiting | Sponsor: BeiGene | Trial completion date: Feb 2028 ➔ Jul 2028

Platinum resistant • Trial completion date • Bladder Cancer • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastroesophageal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer

A first-in-human, phase 1a/b, dose-escalation/expansion study of BG-68501, a selective CDK2 inhibitor, as monotherapy or in combination with fulvestrant for patients with HR+/HER2- breast cancer and other advanced solid tumors: First disclosure of clinical data. (ASCO 2025) - P1 | "BG-68501 demonstrates a favorable safety/tolerability profile, with no DLTs observed to date during dose escalation. Extensively pretreated patients achieving PR and SD with monotherapy, coupled with signs of PD responses and a favorable safety profile, support continued assessment of BG-68501; updated clinical data will be presented at the time of the conference."

Clinical data • Combination therapy • Metastases • Monotherapy • P1 data • Breast Cancer • Endometrial Cancer • Fatigue • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • CCNE1 • HER-2

BG-68501, a CDK2 inhibitor (Abstract# 3115) (Businesswire) - P1a/1b | N=218 | NCT06257264 | Sponsor: BeiGene | "Dose-escalation data from the first-in-human, Phase 1a study of a novel CDK2 inhibitor, BG-68501, were presented as a poster today....Of the 37 efficacy-evaluable patients (all with monotherapy), unconfirmed overall response rate (ORR) was 5.4% (2/37; 95% CI: 0.7%–18.2%). Two extensively pretreated patients (5.4%) experienced unconfirmed partial response (PR), 15 patients (40.5%) had stable disease (SD), 15 patients (40.5%) had progressive disease (PD), and 5 patients (13.5%) were not evaluable/not assessed. Of the 2 patients with PR, both were breast cancer patients, and one was ongoing with treatment at the time of data cutoff, while the other had discontinued treatment."

P1 data • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=218 | Recruiting | Sponsor: BeiGene | N=138 ➔ 218

Enrollment change • Platinum resistant • Bladder Cancer • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastroesophageal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer

BeiGene Presents Pioneering Cancer Research at ASCO 2025 – Redefining Treatment Across Hematology and Solid Tumors (Businesswire) - "BeiGene, Ltd...announced it will share 23 abstracts featuring new data across its hematology and solid tumor portfolio at the American Society of Clinical Oncology (ASCO) Annual Meeting in Chicago, IL, May 30 – June 3, 2025. With two abstracts selected for rapid oral presentation, these data reflect the Company’s vision to address cancer across multiple fronts and provide innovative medicines to as many patients as possible worldwide."

Clinical data • Chronic Lymphocytic Leukemia • Esophageal Squamous Cell Carcinoma • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Nasopharyngeal Carcinoma • Non Small Cell Lung Cancer • Small Lymphocytic Lymphoma • Squamous Cell Carcinoma of Head and Neck

BeiGene Announces Fourth Quarter and Full Year 2024 Financial Results and Business Updates (Businesswire) - "Anticipate data readouts for BGB-43395 (CDK4 inhibitor), BG-68501 (CDK2 inhibitor) and BG-C9074 (B7H4 ADC) in the first half of 2025"

Clinical data • P1 data • Oncology • Solid Tumor

Ensem Therapeutics To Present Preclinical Data for Potential Best-in-Class Oral CDK2 Inhibitor at San Antonio Breast Cancer Symposium (Businesswire) - "In mouse xenograft studies using a CCNE-amplified ovarian cancer cell line or patient-derived tumors, ETX-197/BG-68501 showed sustained target engagement, dose-dependent tumor growth inhibition with excellent tolerability. ETX-197/BG-68501 demonstrated single agent efficacy in a breast cancer xenograft model that had acquired resistance to a CDK4/CDK6 inhibitor. In addition, ETX-197/BG-68501 showed anti-tumor activity in other in vitro and in vivo tumor models including small cell lung and ovarian cancers, indicating its broad clinical potential beyond breast cancer."

Preclinical • Breast Cancer • Oncology • Ovarian Cancer • Small Cell Lung Cancer • Solid Tumor

Company News丨BeiGene Announces Breast Cancer Pipeline [Google translation] (bydrug.pharmcube.com) - "Recently, BeiGene...presented for the first time at the San Antonio Breast Cancer Symposium (SABCS) and announced the latest data on the company's breast cancer treatment product portfolio. Poster presentations included first-in-human data from BeiGene's investigational cyclin-dependent kinase (CDK) 4 inhibitor BGB-43395 for the treatment of hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer patients. Two posters highlighted the ongoing trial designs for BGB-43395 and CDK2 inhibitor BG-68501/EXT-197, and one poster detailed the preclinical characteristics of BGB-43395."

P1 data • Preclinical • Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

ETX-197/BG-68501, a potential best-in-class potent, selective, oral, small molecule CDK2 inhibitor, has anti-tumor activity in cancer models with Cyclin E amplification or deficiency in the Retinoblastoma 1 gene. (SABCS 2024) - P1 | "These data suggest that ETX-197 has the potential to be a best-in class CDK2 inhibitor for the treatment of cancer with CCNE amplification or RB1 deficiency, including breast cancer that has progressed on treatment with a CDK4/6 inhibitor because of these genomic alterations. Currently, ETX-197 is being clinically developed by BeiGene in a first-in-human (FIH), Phase 1a/1b study to assess the safety, tolerability, pharmacokinetics (PK), pharmacodynamics, and preliminary antitumor activity in patients with advanced, nonresectable, or metastatic solid tumors (NCT06257264)."

Preclinical • Breast Cancer • Oncology • Solid Tumor • RB1

Trial in progress: A first-in-human phase 1a/b, dose-escalation/expansion study of BG-68501/ETX-197 (CDK2 inhibitor) as monotherapy or in combination with fulvestrant for patients with HR+/HER2- breast cancer and other advanced solid tumors (SABCS 2024) - P1 | "The study is currently recruiting pts, with 14 sites open across two countries and 6 pts enrolled. Enrollment is complete for 1 cohort and cohort 2A is currently enrolling pts."

Clinical • Combination therapy • Metastases • Monotherapy • P1 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CCNA2 • CCNE1 • HER-2 • RB1

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=138 | Recruiting | Sponsor: BeiGene | Trial completion date: Dec 2026 ➔ Feb 2028 | Trial primary completion date: Dec 2026 ➔ Feb 2028

Metastases • Trial completion date • Trial primary completion date • Bladder Cancer • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • HER-2

Ensem Therapeutics Announces Achievement of Milestone Following Entry of Small Molecule CDK2 Inhibitor into Clinical Trials for Solid Tumors (Businesswire) - "Ensem Therapeutics...announced that its partner BeiGene has dosed the first five patients in its first-in-human Phase 1 trial to evaluate BG-68501, a small molecule cyclin-dependent kinase 2 (CDK2) inhibitor for the treatment of solid tumors. The achievement triggers a milestone payment from BeiGene, which licensed the compound (formerly ETX-197) from ENSEM in November 2023....The Phase 1 clinical trial, conducted by BeiGene, is evaluating BG-68501 in advanced or metastatic solid tumors potentially associated with CDK2 dependency, including HR+/HER2- breast cancer, platinum refractory or resistant serous ovarian, fallopian tube, primary peritoneal cancer, small cell lung cancer, and others (NCT06257264)."

Financing • Trial status • Fallopian Tube Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Ovarian Cancer • Peritoneal Cancer • Small Cell Lung Cancer

BeiGene Reports First Quarter 2024 Financial Results and Business Updates (Businesswire) - "BGB-43395 (CDK4 inhibitor): Initiated fourth dose level of monotherapy, which is in the efficacious dose range with no dose limiting toxicities observed; and initiated dosing of combination with fulvestrant just over four months from first monotherapy dose. BG-68501 (CDK2 inhibitor): Initiated second dose level of monotherapy in first-in-human study, with clinical pharmacokinetics as expected and no dose limiting toxicities observed. BG-C9074 (B7H4 ADC): First patient dosed in Australia in global first-in-human Phase 1 study."

Trial status • Endometrial Cancer • Gastric Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=108 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • Endometrial Cancer • Gastric Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • HER-2

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=108 | Not yet recruiting | Sponsor: BeiGene

New P1 trial • Breast Cancer • Endometrial Cancer • Gastric Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • HER-2

BeiGene and Ensem Therapeutics Announce Partnership to Advance Differentiated CDK2 Inhibitor (Businesswire) - "BeiGene...and Ensem Therapeutics...announced an agreement for BeiGene to acquire an exclusive global license to an Investigational New Drug (IND) application-ready oral cyclin-dependent kinase 2 (CDK2) inhibitor....'This CDK2 inhibitor from ENSEM complements our internally discovered Phase 1 CDK4 inhibitor, which has the potential to improve upon current CDK4/6 inhibitors in some breast cancer patients, and strengthens our early development pipeline in breast cancer and other solid tumors'....Under the terms of the agreement, ENSEM will receive an upfront payment, and will be eligible for additional payments upon the achievement of certain development, regulatory, and commercial milestones, totaling up to $1.33 billion, in addition to tiered royalties."

Licensing / partnership • Breast Cancer