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A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors

Phase 1
Recruiting
Conditions
Breast Cancer
Small Cell Lung Cancer
Ovarian Cancer
Gastric Cancer
Hormone-receptor-positive Breast Cancer
Hormone Receptor Positive HER-2 Negative Breast Cancer
Advanced Solid Tumor
Endometrial Cancer
Prostate Cancer
TNBC - Triple-Negative Breast Cancer
Interventions
Registration Number
NCT06257264
Lead Sponsor
BeiGene
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).

Detailed Description

Not available

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
218
Inclusion Criteria
  • 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.

Part 1 (Safety Expansion) and Part 2 (Dose Expansion) Inclusion Criteria:

  • 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.

General Inclusion Criteria:

  • 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.

General

Exclusion Criteria
  • 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.

Note: Other protocol defined Inclusion/Exclusion criteria may apply.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Part 1 Part A: Dose Escalation and Safety Expansion (BG-68501 Monotherapy)BG-68501Sequential cohorts of increasing dose levels of BG-68501 will be evaluated as monotherapy.
Part 1 Part B: Dose Escalation (BG-68501 + Fulvestrant)BG-68501Sequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant.
Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)BG-68501Sequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant and BGB-43395.
Part 1 Part B: Dose Escalation (BG-68501 + Fulvestrant)FulvestrantSequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant.
Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)FulvestrantSequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant and BGB-43395.
Part 1 Part C: Dose Escalation and Safety Expansion (BG-68501 + Fulvestrant + BGB-43395)BGB-43395Sequential cohorts of increasing dose levels of BG-68501 will be evaluated in combination with fulvestrant and BGB-43395.
Part 1: Food Effect EvaluationBG-68501Participants 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.
Part 1: Food Effect EvaluationFulvestrantParticipants 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.
Part 2: Dose ExpansionBG-68501The RFDE for BG-68501 (as monotherapy and in combination with fulvestrant and BGB-43395) from Part 1 will be evaluated in selected tumor cohorts.
Part 2: Dose ExpansionFulvestrantThe RFDE for BG-68501 (as monotherapy and in combination with fulvestrant and BGB-43395) from Part 1 will be evaluated in selected tumor cohorts.
Part 2: Dose ExpansionBGB-43395The RFDE for BG-68501 (as monotherapy and in combination with fulvestrant and BGB-43395) from Part 1 will be evaluated in selected tumor cohorts.
Primary Outcome Measures
NameTimeMethod
Part 1: Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs)From the first dose of study drug(s) to 30 days after the last dose; approximately 6-12 months

Number of participants with treatment-emergent AEs and SAEs.

Part 1: Maximum Tolerated Dose (MTD) or Maximum Administered Dose (MAD) of BG-68501Up to approximately 24 months

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.

Part 1: Recommended dose(s) for Expansion (RDFE) of BG-68501 monotherapy in participants with solid tumorsUp to approximately 24 months

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

Part 1: RDFE of BG-68501 in combination with fulvestrant and BGB-43395 in participants with HR+/HER2- BCUp to approximately 24 months

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

Part 2: Objective Response Rate (ORR)Up to approximately 20 months

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.

Secondary Outcome Measures
NameTimeMethod
Part 1: ORRUp to approximately 20 months

ORR is defined as the percentage of participants with best overall response of CR or PR. CR and PR that is confirmed by repeat assessments, as assessed by the investigator using RECIST v1.1.

Part 2: Number of participants with AEs and SAEsFrom the first dose of study drug(s) to 30 days after the last dose; approximately 6-12 months

Number of participants with AEs and SAEs, including findings from physical examinations, electrocardiograms (ECGs), and laboratory assessments.

Parts 1 and 2: Duration of Response (DOR)Up to approximately 20 months

DOR is defined as the time from the first confirmed objective response by the investigator using RECIST v1.1 until the first documentation of disease progression after treatment initiation or death, whichever comes first.

Parts 1 and 2: Time to Response (TTR)Up to approximately 20 months

TTR is defined as the time from the treatment initiation to the first determination of overall response by the investigator using RECIST v1.1.

Parts 1 and 2: Disease Control Rate (DCR)Up to approximately 20 months

DCR is defined as the percentage of participants with the best overall response, of a CR, PR, and stable disease assessed by the investigator using RECIST v1.1.

Parts 1 and 2: Clinical Benefit Rate (CBR)Up to approximately 20 months

CBR is defined as the percentage of participants with best overall response of confirmed CR, PR, or stable disease lasting ≥ 24 weeks assessed by the investigator using RECIST v1.1.

Part 1: Maximum observed plasma concentration (Cmax) for BG-68501 and BGB-433952 times in the first 2 months
Part 1: Observed plasma trough concentration (Ctrough) for BG-68501 and BGB-433955 times in the first 2 months
Part 1: Area under the concentration-time curve (AUC) for BG-68501 and BGB-433952 times in the first 2 months
Part 1: Half-life (t1/2) for BG-68501 and BGB-433952 times in the first 2 months
Part 2: Plasma concentrations for BG-68501 and BGB-433955 times in approximately 3 months

Trial Locations

Locations (33)

The First Affiliated Hospital of Chongqing Medical University

🇨🇳

Chongqing, Chongqing, China

Hoag Memorial Presbyterian

🇺🇸

Newport Beach, California, United States

Florida Cancer Specialists and Research Institute

🇺🇸

Lake Mary, Florida, United States

Washington University School of Medicine

🇺🇸

Saint Louis, Missouri, United States

Titan Health Partners Llc Dba Astera Cancer Care

🇺🇸

East Brunswick, New Jersey, United States

Avera Cancer Institue

🇺🇸

Sioux Falls, South Dakota, United States

Mary Crowley Cancer Research

🇺🇸

Dallas, Texas, United States

Blacktown Cancer and Haematology Centre

🇦🇺

Blacktown, New South Wales, Australia

Saint Vincents Hospital Sydney

🇦🇺

Darlinghurst, New South Wales, Australia

Nepean Hospital

🇦🇺

Kingswood, New South Wales, Australia

Genesiscare North Shore

🇦🇺

St Leonards, New South Wales, Australia

Princess Alexandra Hospital

🇦🇺

Woolloongabba, Queensland, Australia

Cancer Research South Australia

🇦🇺

Adelaide, South Australia, Australia

Monash Health

🇦🇺

Clayton, Victoria, Australia

Peter Maccallum Cancer Centre

🇦🇺

Melbourne, Victoria, Australia

Cancer Hospital Chinese Academy of Medical Sciences

🇨🇳

Beijing, Beijing, China

Beijing Cancer Hospital

🇨🇳

Beijing, Beijing, China

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

🇨🇳

Guangzhou, Guangdong, China

Harbin Medical University Cancer Hospital

🇨🇳

Harbin, Heilongjiang, China

Hunan Cancer Hospital

🇨🇳

Changsha, Hunan, China

Shengjing Hospital Affiliated of China Medical University

🇨🇳

Shenyang, Liaoning, China

The First Affiliated Hospital of Xian Jiaotong University

🇨🇳

Xian, Shaanxi, China

Sichuan Academy of Medical Sciences and Sichuan Provincial Peoples Hospital

🇨🇳

Chengdu, Sichuan, China

Rambam Health Care Center

🇮🇱

Haifa, Israel

Shaare Zedek Medical Center

🇮🇱

Jerusalem, Israel

Seoul National University Bundang Hospital

🇰🇷

BundangGu SeongnamSi, Gyeonggi-do, Korea, Republic of

National Cancer Center (Korea)

🇰🇷

IlsandongGu GoyangSi, Gyeonggi-do, Korea, Republic of

Samsung Medical Center

🇰🇷

GangnamGu, Seoul Teugbyeolsi, Korea, Republic of

Severance Hospital Yonsei University Health System

🇰🇷

SeodaemunGu, Seoul Teugbyeolsi, Korea, Republic of

Seoul National University Hospital

🇰🇷

Seoul, Seoul Teugbyeolsi, Korea, Republic of

Asan Medical Center

🇰🇷

SongpaGu, Seoul Teugbyeolsi, Korea, Republic of

The Institute of Oncology, Arensia Exploratory Medicine

🇲🇩

Chisinau, Moldova, Republic of

Auckland City Hospital

🇳🇿

Auckland, New Zealand

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