An Investigational Study of BG-75202 Alone and in Combination With Other Therapeutic Agents in Adults With Advanced Solid Tumors

NCT07222267 | Recruiting Phase 1 FDA Drug

• 2 other identifiers: BG-75202-1012025-523553-34-00
• Study Type: interventional
• Target: 86
• Locations: 5 countries
• Sites: 23

Brief Summary

The purpose of this study is to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics, and preliminary antitumor activity of BG-75202 (KAT6A/B inhibitor) alone and in combination with other therapies in participants with breast cancer and other advanced solid tumors.

Conditions

Breast Cancer; Advanced Solid Tumor

Keywords

KAT6 inhibitor

Outcome Measures

Primary Outcomes (3)

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

  Number of participants with treatment-emergent adverse events (TEAEs) and serious adverse events (SAEs), including physical examination findings, electrocardiogram results, laboratory values, and AEs meeting protocol-defined dose-limiting toxicity (DLT) criteria.

  From first dose to 30 days after last dose or initiation of a new anticancer therapy, whichever occurs first, up to approximately 12 months

• Part 1: Recommended Dose for Expansion (RDFE)

  The RDFE is based on the maximum tolerated dose (MTD) or maximum administered dose (MAD) with consideration of the tolerability, pharmacokinetics (PK), pharmacodynamics, antitumor activity, and any other available relevant data.

  Estimated approximately 1 year

• Part 2: Overall Response Rate (ORR)

  ORR is defined as the percentage of participants with partial or complete response, as assessed by the investigator using Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1).

  Up to approximately 2 years

Secondary Outcomes (14)

• Part 1: ORR

  Up to approximately 1 year

• Part 1: Duration of Response (DOR)

  Up to approximately 1 year

• Part 1: Time to Response (TTR)

  Up to approximately 1 year

• Part 2: DOR

  Up to approximately 2 years

• Part 2: TTR

  Up to approximately 2 years

Study Arms (5)

Part 1A: Dose Escalation and Safety Expansion, BG-75202 Monotherapy

EXPERIMENTAL

Sequential cohorts of increasing dose levels of BG-75202 will be evaluated as monotherapy.

Drug: BG-75202

Part 1B: Dose Escalation and Safety Expansion, BG-75202 + Estrogen Receptor Antagonist

EXPERIMENTAL

Sequential cohorts of increasing dose levels of BG-75202 will be evaluated in combination with an estrogen receptor antagonist.

Drug: BG-75202; Drug: Estrogen Receptor Antagonist

Part 2A: Dose Optimization, BG-75202 + Estrogen Receptor Antagonist

EXPERIMENTAL

Participants will receive BG-75202 in combination with an estrogen receptor antagonist.

Drug: BG-75202; Drug: Estrogen Receptor Antagonist

Part 2B: Safety Run-In, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor

EXPERIMENTAL

Participants will receive BG-75202 in combination with a cyclin-dependent kinase 4 (CDK4) inhibitor and an aromatase inhibitor.

Drug: BG-75202; Drug: CDK4 Inhibitor; Drug: Aromatase Inhibitor

Part 2C: Dose Expansion, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor

EXPERIMENTAL

Participants will receive BG-75202 in combination with a CDK4 inhibitor and an aromatase inhibitor.

Drug: BG-75202; Drug: CDK4 Inhibitor; Drug: Aromatase Inhibitor

Interventions

BG-75202 DRUG

Administered orally.

Part 1A: Dose Escalation and Safety Expansion, BG-75202 Monotherapy; Part 1B: Dose Escalation and Safety Expansion, BG-75202 + Estrogen Receptor Antagonist; Part 2A: Dose Optimization, BG-75202 + Estrogen Receptor Antagonist; Part 2B: Safety Run-In, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor; Part 2C: Dose Expansion, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor

CDK4 Inhibitor DRUG

Administered orally.

Part 2B: Safety Run-In, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor; Part 2C: Dose Expansion, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor

Estrogen Receptor Antagonist DRUG

Administered by intramuscular injection.

Part 1B: Dose Escalation and Safety Expansion, BG-75202 + Estrogen Receptor Antagonist; Part 2A: Dose Optimization, BG-75202 + Estrogen Receptor Antagonist

Aromatase Inhibitor DRUG

Administered orally.

Part 2B: Safety Run-In, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor; Part 2C: Dose Expansion, BG-75202 + CDK4 inhibitor + Aromatase Inhibitor

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Part 1A: Participants with histologically or cytologically confirmed advanced, metastatic breast cancer and other solid tumors who have exhausted, are intolerant of all available standard of care therapies, and/or without available standard of care therapies.
• Part 1B and Part 2A: Participants with advanced breast cancer with 1 to 3 prior lines of systemic therapy in the metastatic setting. Prior lines in the advanced/ metastatic setting may not exceed 2 lines of chemotherapy (inclusive of antibody-drug conjugate with cytotoxic payload).
• Parts 2B and 2C: Participants with advanced breast cancer enrolled in regions where cyclin-dependent kinase 4/6 (CDK4/6) inhibitors are not approved and/or not available as the first-line treatment and who are CDK4/6 inhibitor treatment naïve and did not receive any previous systemic treatment for advanced disease.
• Participants with breast cancer must have histologically or cytologically confirmed advanced breast cancer at the time of most recent testing, based on American Society of Clinical Oncology (ASCO)/College of American Pathologists (CAP) guidelines.
• Female participants with metastatic breast cancer must be postmenopausal or receiving ovarian function suppression treatment.
• Measurable disease as assessed by Response Evaluation Criteria in Solid Tumors (RECIST) v 1.1.
• Stable Eastern Cooperative Oncology Group (ECOG) Performance Status of 0 or 1.
• Adequate organ function.

You may not qualify if:

• Prior exposure to KAT6A/B or KAT7 inhibitors/degraders.
• Patients with active leptomeningeal disease or uncontrolled, untreated brain metastasis.
• Participants with any malignancy ≤ 3 years before screening for the study except for the specific cancer under investigation in this study and any locally recurring cancer that has been treated curatively which in the opinion of the investigator is unlikely to require intervention during the study.

Sponsors & Collaborators

• BeOne Medicines: lead

Study Sites (23)

University of Alabama At Birmingham Hospital

Birmingham, Alabama, 35294-0004, United States

RECRUITING

Yale Cancer Center

New Haven, Connecticut, 06520-8028, United States

RECRUITING

Washington University in St Louis

St Louis, Missouri, 63110-1010, United States

RECRUITING

Next Oncology Austin

Austin, Texas, 78758, United States

RECRUITING

The University of Texas Md Anderson Cancer Center

Houston, Texas, 77030-4009, United States

RECRUITING

Blacktown Cancer and Haematology Centre

Blacktown, New South Wales, NSW 2148, Australia

RECRUITING

Chris Obrien Lifehouse

Camperdown, New South Wales, NSW 2050, Australia

RECRUITING

Cancer Research South Australia

Adelaide, South Australia, SA 5000, Australia

RECRUITING

Peter Maccallum Cancer Centre

Melbourne, Victoria, VIC 3000, 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 University Cancer Centerhuangpu Branch

Guangzhou, Guangdong, 510555, China

RECRUITING

Harbin Medical University Cancer Hospital

Harbin, Heilongjiang, 150000, China

RECRUITING

Jiangsu Province Hospital Longjiang Branch

Nanjing, Jiangsu, 210036, China

RECRUITING

Fudan University Shanghai Cancer Centerpudong

Shanghai, Shanghai Municipality, 201321, China

RECRUITING

Tianjin Medical University Cancer Institute and Hospital

Tianjin, Tianjin Municipality, 300060, China

RECRUITING

Istituto Europeo Di Oncologia

Milan, 20141, Italy

RECRUITING

Fondazione Policlinico Universitario Agostino Gemelli

Roma, 00168, Italy

RECRUITING

Istituto Clinico Humanitas

Rozzano, 20089, Italy

RECRUITING

Next Oncology Barcelona

Barcelona, 8023, Spain

RECRUITING

Hospital Universitario 12 de Octubre

Madrid, 28041, Spain

RECRUITING

Hospital Clinico San Carlos

Madrid, 28240, Spain

RECRUITING

Hospital Universitario Virgen de La Victoria

Málaga, 29010, Spain

RECRUITING

MeSH Terms

Conditions

Breast Neoplasms

Interventions

Cyclin-Dependent Kinase Inhibitor p16; Estrogen Receptor Antagonists; Aromatase Inhibitors

Condition Hierarchy (Ancestors)

Neoplasms by Site; Neoplasms; Breast Diseases; Skin Diseases; Skin and Connective Tissue Diseases

Intervention Hierarchy (Ancestors)

Cyclin-Dependent Kinase Inhibitor Proteins; Intracellular Signaling Peptides and Proteins; Peptides; Amino Acids, Peptides, and Proteins; Cell Cycle Proteins; Proteins; Tumor Suppressor Proteins; Neoplasm Proteins; Estrogen Antagonists; Hormone Antagonists; Hormones, Hormone Substitutes, and Hormone Antagonists; Physiological Effects of Drugs; Pharmacologic Actions; Chemical Actions and Uses; Steroid Synthesis Inhibitors; Enzyme Inhibitors; Molecular Mechanisms of Pharmacological Action

Study Officials

• Study Director

  BeOne Medicines

  STUDY DIRECTOR

Central Study Contacts

Study Director

CONTACT

877-828-5568; clinicaltrials@beonemed.com

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: October 28, 2025
• First Posted: October 29, 2025
• Study Start: December 11, 2025
• Primary Completion (Estimated): September 30, 2029
• Study Completion (Estimated): January 13, 2037
• Last Updated: April 22, 2026

Record last verified: 2026-04

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, CSR
• Time Frame: See plan description
• Access Criteria: See plan description

Locations

AU (4); CN (7); IT (3); ES (4); US (5)