NCT06257264

Brief Summary

This study is a first-in-human (FIH), Phase 1a/1b study of BG-68501, a cyclin-dependent kinase-2 inhibitor (CDK2i), to assess the safety, tolerability, pharmacokinetics (PK), pharmacodynamics, and preliminary antitumor activity of BG-68501 in participants with advanced, nonresectable, or metastatic solid tumors as monotherapy and in combination with fulvestrant with or without BGB-43395, a selective CDK4 inhibitor, in adults with hormone receptor positive (HR+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer (BC). The study will also identify a recommended dose for expansion (RDFE) for BG-68501 as monotherapy and in combination for subsequent disease directed studies. The study will be conducted in 2 parts: Part 1 (dose escalation and safety expansion, including evaluation of food effect) and Part 2 (dose expansion).

Trial Health

83
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
258

participants targeted

Target at P75+ for phase_1 breast-cancer

Timeline
26mo left

Started Mar 2024

Typical duration for phase_1 breast-cancer

Geographic Reach
6 countries

24 active sites

Status
recruiting

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Progress50%
Mar 2024Jul 2028

First Submitted

Initial submission to the registry

February 5, 2024

Completed
8 days until next milestone

First Posted

Study publicly available on registry

February 13, 2024

Completed
27 days until next milestone

Study Start

First participant enrolled

March 11, 2024

Completed
4.1 years until next milestone

Primary Completion

Last participant's last visit for primary outcome

April 1, 2028

Expected
3 months until next milestone

Study Completion

Last participant's last visit for all outcomes

July 1, 2028

Last Updated

April 22, 2026

Status Verified

April 1, 2026

Enrollment Period

4.1 years

First QC Date

February 5, 2024

Last Update Submit

April 20, 2026

Conditions

Keywords

breast cancersmall cell lung cancerovarian cancergastric cancercdk2 inhibitorBG-68501HR+ HER2- breast cancerendometrial cancerprostate cancerBGB-43395bladder cancerurothelial cancergastroesophageal cancercdk4 inhibitorfulvestrant

Outcome Measures

Primary Outcomes (5)

  • Part 1: Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs)

    Number of participants with treatment-emergent AEs and SAEs.

    From the first dose of study drug(s) to 30 days after the last dose; approximately 6-12 months

  • Part 1: Maximum Tolerated Dose (MTD) or Maximum Administered Dose (MAD) of BG-68501

    MTD is defined as the highest dose evaluated for which estimated toxicity rate is the closest to the target toxicity rate. MAD is defined as the highest dose administered if MTD is not reached.

    Up to approximately 24 months

  • Part 1: Recommended dose(s) for Expansion (RDFE) of BG-68501 monotherapy in participants with solid tumors

    RDFE of BG-68501 alone will be determined based upon the MTD or MAD.

    Up to approximately 24 months

  • Part 1: RDFE of BG-68501 in combination with fulvestrant and BGB-43395 in participants with HR+/HER2- BC

    RDFE of BG-68501 in combination with fulvestrant and BGB-43395 will be determined based upon the MTD or MAD.

    Up to approximately 24 months

  • Part 2: Objective Response Rate (ORR)

    ORR is defined as the percentage of participants with best overall response of complete response (CR) or partial response (PR). CR and PR that is confirmed by repeat assessments, as assessed by the investigator using Response Evaluation Criteria in Solid Tumors (RECIST) v1.1.

    Up to approximately 20 months

Secondary Outcomes (11)

  • Part 1: ORR

    Up to approximately 20 months

  • Part 2: Number of participants with AEs and SAEs

    From the first dose of study drug(s) to 30 days after the last dose; approximately 6-12 months

  • Parts 1 and 2: Duration of Response (DOR)

    Up to approximately 20 months

  • Parts 1 and 2: Time to Response (TTR)

    Up to approximately 20 months

  • Parts 1 and 2: Disease Control Rate (DCR)

    Up to approximately 20 months

  • +6 more secondary outcomes

Study Arms (5)

Part 1 Part A: Dose Escalation and Safety Expansion (BG-68501 Monotherapy)

EXPERIMENTAL

Sequential cohorts of increasing dose levels of BG-68501 will be evaluated as monotherapy.

Drug: BG-68501

Part 1 Part B: Dose Escalation (BG-68501 + Fulvestrant)

EXPERIMENTAL

Sequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant.

Drug: BG-68501Drug: Fulvestrant

Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)

EXPERIMENTAL

Sequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant and BGB-43395.

Drug: BG-68501Drug: FulvestrantDrug: BGB-43395

Part 1: Food Effect Evaluation

EXPERIMENTAL

Participants will receive BG-68501 at a dose level that is determined safe and tolerable to evaluate food effect. Food effect may also be evaluated for BG-68501 in combination with fulvestrant.

Drug: BG-68501Drug: Fulvestrant

Part 2: Dose Expansion

EXPERIMENTAL

The RFDE for BG-68501 (as monotherapy and in combination with fulvestrant and BGB-43395) from Part 1 will be evaluated in selected tumor cohorts.

Drug: BG-68501Drug: FulvestrantDrug: BGB-43395

Interventions

Planned doses administered orally.

Part 1 Part A: Dose Escalation and Safety Expansion (BG-68501 Monotherapy)Part 1 Part B: Dose Escalation (BG-68501 + Fulvestrant)Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)Part 1: Food Effect EvaluationPart 2: Dose Expansion

Standard dose administered via intramuscular injection.

Part 1 Part B: Dose Escalation (BG-68501 + Fulvestrant)Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)Part 1: Food Effect EvaluationPart 2: Dose Expansion

Planned doses administered orally.

Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)Part 2: Dose Expansion

Eligibility Criteria

Age18 Years+
Sexall
Healthy VolunteersNo
Age GroupsAdult (18-64), Older Adult (65+)

You may qualify if:

  • Monotherapy Cohorts: Participants with histologically or cytologically confirmed advanced or metastatic solid tumors potentially associated with CDK2 dependency including HR+/HER2- breast cancer, platinum refractory or resistant serous ovarian cancer (PROC), endometrial cancer, and others. Prior available standard-of-care systemic therapies for advanced or metastatic disease are required. The requirements for enrollment into a food effect evaluation cohort are the same as the monotherapy cohorts with the exception that participants with gastric cancer and gastroesophageal adenocarcinoma are excluded.
  • Combination Cohorts (BG-68501 with fulvestrant with or without BGB-43395): Enrollment is restricted to only participants with HR+/HER2- BC. In regions where approved and available, participants must have received one or more lines of treatment for advanced/metastatic disease as well as prior endocrine therapy and a CDK4/6 inhibitor in either the adjuvant or advanced/metastatic setting. If applicable, the requirements for enrollment into a food effect evaluation cohort are the same as the combination cohorts.
  • Participants with advanced, non-resectable, or metastatic HR+/HER2- BC or PROC, including fallopian tube or primary peritoneal cancer.
  • PROC participants must have received:
  • ≥ 1 line of platinum-containing chemotherapy for advanced disease.
  • ≤ 4 prior therapeutic regimens in the advanced/metastatic setting.
  • HR+/HER2- BC:
  • Participants enrolled in regions where CDK4/6 inhibitors are approved and available must have received ≥ 1 line of therapy including endocrine therapy and a CDK4/6 inhibitor. Participants can have received up to 2 lines of prior cytotoxic chemotherapy or ADC treatments for advanced disease.
  • Female participants with advanced or metastatic HR+/HER2- BC will be required to have ovarian function suppression using gonadotropin hormone-releasing hormone (GnRH) agonists (such as goserelin) or be postmenopausal.
  • Eastern Cooperative Oncology Group (ECOG) Performance Status ≤ 1.
  • Adequate organ function.
  • For dose escalation, participants with advanced solid tumors other than HR+/HER2- BC must have measurable disease per RECIST 1.1. Participants with HR+/HER2- BC with bone-only disease are eligible for dose escalation only. For safety expansion and dose expansion, all participants must have ≥1 measurable lesion per RECIST v 1.1.

You may not qualify if:

  • For all cohorts: Prior therapy selectively targeting CDK2 inhibition.
  • For triple combination cohorts: Prior therapy targeting CDK2 or selectively targeting CDK4. Prior CDK4/6 inhibitor therapy is permitted and required in local regions where it is approved and available.
  • Known leptomeningeal disease or uncontrolled, untreated brain metastasis. Participants with a history of treated central nervous system (CNS) metastases may be eligible if they meet additional criteria.
  • Any malignancy ≤ 3 years before the first dose of study treatment(s) except for the specific cancer under investigation in this study and any locally recurring cancer that has been treated with curative intent (eg, resected basal or squamous cell skin cancer, superficial bladder cancer, treated papillary thyroid carcinoma, or carcinoma in situ of the cervix or breast).
  • Uncontrolled diabetes.
  • Infection requiring systemic antibacterial, antifungal, or antiviral therapy antiviral therapy ≤ 28 days before the first dose of study drug(s), or symptomatic COVID-19 infection.
  • Active hepatitis B infection or active hepatitis C infection.
  • Any major surgical procedure ≤ 28 days before the first dose of study treatment(s).
  • Prior allogeneic stem cell transplantation, or organ transplantation.

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (24)

Hoag Memorial Presbyterian

Newport Beach, California, 92663-4162, United States

RECRUITING

Florida Cancer Specialists and Research Institute

Lake Mary, Florida, 32746-2115, United States

COMPLETED

Washington University School of Medicine

St Louis, Missouri, 63110-1010, United States

RECRUITING

Titan Health Partners Llc Dba Astera Cancer Care

East Brunswick, New Jersey, 08816-4096, United States

RECRUITING

Avera Cancer Institute

Sioux Falls, South Dakota, 57105-2108, United States

RECRUITING

Mary Crowley Cancer Research

Dallas, Texas, 75230, United States

RECRUITING

Blacktown Cancer and Haematology Centre

Blacktown, New South Wales, NSW 2148, Australia

RECRUITING

Saint Vincents Hospital Sydney

Darlinghurst, New South Wales, NSW 2010, Australia

RECRUITING

Nepean Hospital

Kingswood, New South Wales, NSW 2747, Australia

RECRUITING

Genesiscare North Shore

St Leonards, New South Wales, NSW 2065, Australia

RECRUITING

Princess Alexandra Hospital

Woolloongabba, Queensland, QLD 4102, Australia

RECRUITING

Cancer Research South Australia

Adelaide, South Australia, SA 5000, Australia

RECRUITING

Monash Health

Clayton, Victoria, VIC 3168, Australia

RECRUITING

Cancer Hospital Chinese Academy of Medical Sciences

Beijing, Beijing Municipality, 100021, China

RECRUITING

Beijing Cancer Hospital

Beijing, Beijing Municipality, 100142, China

RECRUITING

Sun Yat Sen Memorial Hospital, Sun Yat Sen University (South)

Guangzhou, Guangdong, 510245, China

RECRUITING

Harbin Medical University Cancer Hospital

Harbin, Heilongjiang, 150000, China

RECRUITING

Hunan Cancer Hospital

Changsha, Hunan, 410013, China

RECRUITING

Shengjing Hospital of China Medical Universityhuaxiang Branch

Shenyang, Liaoning, 110022, China

RECRUITING

The First Affiliated Hospital of Xian Jiaotong University

Xi'an, Shaanxi, 710061, China

RECRUITING

Rambam Health Care Center

Haifa, 3109601, Israel

RECRUITING

Shaare Zedek Medical Center

Jerusalem, 9103102, Israel

RECRUITING

The Institute of Oncology, Arensia Exploratory Medicine

Chisinau, 2025, Moldova

RECRUITING

Auckland City Hospital

Auckland, 1023, New Zealand

RECRUITING

MeSH Terms

Conditions

Breast NeoplasmsSmall Cell Lung CarcinomaOvarian NeoplasmsStomach NeoplasmsEndometrial NeoplasmsProstatic NeoplasmsTriple Negative Breast NeoplasmsUrinary Bladder Neoplasms

Interventions

Fulvestrant

Condition Hierarchy (Ancestors)

Neoplasms by SiteNeoplasmsBreast DiseasesSkin DiseasesSkin and Connective Tissue DiseasesCarcinoma, BronchogenicBronchial NeoplasmsLung NeoplasmsRespiratory Tract NeoplasmsThoracic NeoplasmsLung DiseasesRespiratory Tract DiseasesEndocrine Gland NeoplasmsOvarian DiseasesAdnexal DiseasesGenital Diseases, FemaleFemale Urogenital DiseasesFemale Urogenital Diseases and Pregnancy ComplicationsUrogenital DiseasesGenital Neoplasms, FemaleUrogenital NeoplasmsGenital DiseasesEndocrine System DiseasesGonadal DisordersGastrointestinal NeoplasmsDigestive System NeoplasmsDigestive System DiseasesGastrointestinal DiseasesStomach DiseasesUterine NeoplasmsUterine DiseasesGenital Neoplasms, MaleGenital Diseases, MaleProstatic DiseasesMale Urogenital DiseasesUrologic NeoplasmsUrinary Bladder DiseasesUrologic Diseases

Intervention Hierarchy (Ancestors)

EstradiolEstrenesEstranesSteroidsFused-Ring CompoundsPolycyclic CompoundsEstradiol CongenersGonadal Steroid HormonesGonadal HormonesHormonesHormones, Hormone Substitutes, and Hormone Antagonists

Study Officials

  • Study Director

    BeiGene

    STUDY DIRECTOR

Central Study Contacts

Study Design

Study Type
interventional
Phase
phase 1
Allocation
NON RANDOMIZED
Masking
NONE
Purpose
TREATMENT
Intervention Model
SEQUENTIAL
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

February 5, 2024

First Posted

February 13, 2024

Study Start

March 11, 2024

Primary Completion (Estimated)

April 1, 2028

Study Completion (Estimated)

July 1, 2028

Last Updated

April 22, 2026

Record last verified: 2026-04

Data Sharing

IPD Sharing
Will share

BeiGene shares data on completed studies responsibly and provides qualified scientific and medical researchers access to data and supporting documentation for clinical trials in dossiers for medicines and indications after submission and approval in the United States, China, and Europe. Clinical trials supporting subsequent local approvals, new indications, or combination products are eligible for sharing once corresponding regulatory approvals are achieved. BeiGene shares data only when permitted by applicable data privacy and security laws and regulations, when it is feasible to do so without compromising the privacy of study participants, and other considerations. Qualified researchers with appropriate competencies who are engaged in novel scientific research may submit a request for participant-level data with a research proposal for BeiGene review. Research teams must include a biostatistician and sign a Data Sharing Agreement prior to receiving access to clinical trial data.

Shared Documents
STUDY PROTOCOL, SAP, CSR
Time Frame
See plan description
Access Criteria
See plan description
More information

Locations