BG-68501-101

This study is a first-in-human, Phase 1a/1b study of BG-68501, a cyclin-dependent kinase-2 (CDK2) inhibitor, to assess the safety, tolerability, pharmacokinetics (how the drug behaves in your body), pharmacodynamics (how your body responds), and early signs of effectiveness in participants with advanced, nonresectable, or metastatic HR+/HER2- breast cancer. The study will assess BG-68501 as monotherapy or in combination with fulvestrant with or without BGB-43395, a selective CDK4 inhibitor.

The study has 2 parts: 

Part 1 will be finding the highest dose of BG-68501 that can be given that is most tolerated and safest (called dose escalation and safety expansion). There will also be an evaluation of the effects of food on the drug. 

Part 2 will be looking at the dose for BG-68501, found in Part 1, in a number of different groups of patients with different tumour types to make sure consistent results for dose is tolerated (dose expansion).

If you decide to participate in this trial you don't have to do both parts. You could be involved in either Part 1 or Part 2.

The study will be assessing BG-68501 in different tumour types, but the information on this page relates to breast cancer only.

Background of BG-68501

BG-68501 has been thoroughly studied in the lab and has now been approved to be studied in humans. This trial will be the first to investigate BG-68501 in humans (first in human trial) and so the aim of the study is to find the highest dose of the drug that is best tolerated and safest.

This trial is being conducted in multiple countries, including, the USA, Australia, China, South Korea, Israel, Moldova and New Zealand.

Who is it for?

General Inclusion Criteria:

• Female participants aged 18 years or over with advanced or metastatic HR+/HER2- breast cancer
• Previous treatment requirements:
  • Part 1 (Dose Escalation):
    • Monotherapy cohort: Prior available standard-of-care systemic therapies for advanced or metastatic disease are required.
    • Combination Cohorts (BG-68501 with fulvestrant with or without BGB-43395): participants must have received ≥ 1 line of therapy including endocrine therapy and a CDK4/6 inhibitor in either the adjuvant or advanced/metastatic setting. 
  • Part 1 (Safety Expansion) and Part 2 (Dose Expansion):
  • Participants 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 antibody drug conjugates for advanced disease.
    
• Participants 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 and adequate organ function.
• Participants who have HR+/HER2- breast cancer with bone-only metastases 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 (unable to participate):

• Like all clinical trials, some exclusion criteria apply. It is best to talk to your medical oncologist or the study centre to find our if you are eligible for this study.

What does it involve?

This study is in two parts. 

Part 1 is a dose escalation and safety assessment, which will also look at the effect of food on the drug.

Part 2 is a dose expansion assessment.

Part 1: If you are eligible for this study and agree to take part you will be allocated to one of three groups: 

• Group 1: BG-68501 given alone (as monotherapy). 

• Group 2: BG-68501 given with fulvestrant (combination group). 

• Group 3: BG-68501 given with fulvestrant + BGB-43395 (triple combination group). 

This means there are three separate groups of patients, and each group is testing a different way of giving the drug — either BG-68501 by itself, or in combination with other treatments.

Each patient is placed into just one group.

Within that group, the study tests different dose levels — but each patient only receives one dose level (not multiple increasing doses).

The purpose is to find the safest and most tolerated dose for each group, by testing higher doses in new patients, not by increasing the dose in the same patient.

Researchers will also look at whether taking the drug with or without food changes absorption or tolerance.

Part 2: Dose Expansion. Once a safe and promising dose is identified from Part 1 (the recommended dose for expansion), that dose is given to additional groups of patients to further explore safety and early efficacy in specific tumour types.

How are the drugs given?

BG-68501 will be given orally; fulvestrant will be given as intramuscular injection; and BGB-43395 will be given orally.

More trial information can be found here