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RecruitingInterventionalPhase 1

A Phase 1a/1b Study Evaluating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Antitumor Activity of BG-75202, Alone and in Combination With Other Agents in Patients With Advanced Solid Tumors

NCT ID: NCT07222267Sponsor: BeOne MedicinesLast updated: 2026-06-03

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.

Arms & interventions

  • DrugBG-75202

    Administered orally.

  • DrugCDK4 Inhibitor

    Administered orally.

  • DrugEstrogen Receptor Antagonist

    Administered by intramuscular injection.

  • DrugAromatase Inhibitor

    Administered orally.

Outcome measures

Primary

  • 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.

    Time frame: 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.

    Time frame: 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).

    Time frame: Up to approximately 2 years

Secondary

  • Part 1: ORR

    Time frame: Up to approximately 1 year

  • Part 1: Duration of Response (DOR)

    Time frame: Up to approximately 1 year

  • Part 1: Time to Response (TTR)

    Time frame: Up to approximately 1 year

  • Part 2: DOR

    Time frame: Up to approximately 2 years

  • Part 2: TTR

    Time frame: Up to approximately 2 years

  • Part 2: Disease Control Rate (DCR)

    Time frame: Up to approximately 2 years

  • Part 2: Clinical Benefit Rate (CBR)

    Time frame: Up to approximately 2 years

  • Part 2: Progression-Free Survival (PFS)

    Time frame: Up to approximately 2 years

  • Part 2: Number of Participants with Adverse Events (AEs)

    Time frame: Up to approximately 2 years

  • Part 2: Recommended Phase 2 Dose (RP2D)

    Time frame: Up to approximately 2 years

  • Parts 1 and 2: Maximum Observed Plasma Concentration (Cmax) of BG-75202

    Time frame: Up to approximately 4 months

  • Parts 1 and 2: Minimum Observed Plasma Concentration (Ctrough) of BG-75202

    Time frame: Up to approximately 4 months

  • Parts 1 and 2: Area Under the Plasma Concentration-Time Curve (AUC) of BG-75202

    Time frame: Up to approximately 4 months

  • Parts 1 and 2: Terminal Half-Life (t1/2) of BG-75202

    Time frame: Up to approximately 4 months

Eligibility criteria

Sex: AllAge: 18 Years and olderHealthy volunteers: No
Inclusion Criteria: * 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. Exclusion Criteria: * 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. Note: Other protocol defined Inclusion/Exclusion criteria may apply.

Study locations (6)

University of Alabama At Birmingham Hospital

Birmingham, Alabama, 35294-0004

Recruiting

Yale Cancer Center

New Haven, Connecticut, 06510

Recruiting

Washington University in St Louis

St Louis, Missouri, 63110-1010

Recruiting

Next Oncology Austin

Austin, Texas, 78758

Recruiting

The University of Texas Md Anderson Cancer Center

Houston, Texas, 77030-4009

Recruiting

Fred Hutchinson Cancer Research Center

Seattle, Washington, 98109-4433

Recruiting