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Phase 2 Completed N=96 Treatment

Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab

Chronic Lymphocytic Leukemia · Small Lymphocytic Lymphoma · Follicular Lymphoma · Marginal Zone Lymphoma
Source: ClinicalTrials.gov NCT04282018 ↗
Enrolled (actual)
96
Serious AEs
39.6%
Results posted
Feb 2026
Primary outcomePrimary: Part A: The Recommended Dose for Expansion (RDFE) of BGB-10188 Monotherapy in Hematologic Malignancies — NA mg

Summary

The purpose of this study was to determine the maximum tolerated dose (MTD), recommended dose for expansion (RDFE), safety and tolerability of BGB-10188 as monotherapy in participants with relapsed/refractory (R/R) mature B-cell malignancies; in combination with zanubrutinib in participants with R/R follicular lymphoma (FL), R/R mantle cell lymphoma (MCL) or R/R diffuse large B-cell lymphoma (DLBCL); and in combination with tislelizumab in participants with advanced solid tumors.

Outcome Measures

OutcomeResultp-value
PRIMARY
Part A: The Recommended Dose for Expansion (RDFE) of BGB-10188 Monotherapy in Hematologic Malignancies
NA
PRIMARY
Part B: The RDFE of BGB-10188 in Combination With Zanubrutinib in Hematologic Malignancies
NA
PRIMARY
Part D: The RDFE of BGB-10188 in Combination With Tislelizumab in Advanced Solid Tumors
320; 160
PRIMARY
Part E: Overall Response Rate (ORR) as Per Response Evaluation Criteria in Solid Tumors (RECIST) v.1.1
0.0; 0.0
PRIMARY
Number of Participants With Treatment Emergent Adverse Events (AEs), Serious Adverse Events (SAEs), and AEs Leading to Discontinuation
4; 5; 8; 6; 10; 4
SECONDARY
Parts A and B: ORR as Assessed by Investigator
50.0; 20.0; 50.0; 83.3; 66.7; 100
SECONDARY
Part A: Observed Maximum Plasma Concentration (Cmax) of BGB-10188 After a Single Dose
32.9; 54.0; 332.2; 266.2; 1124.5
SECONDARY
Part A: Cmax of BGB-10188 at Steady State
16.8; 60.7; 278.5; 205.2; 642.8
SECONDARY
Part A: Area Under the Plasma Concentration-time Curve From Time 0 to 24 Hours (AUC0-24) After Single Dose
86.5; 277.5; 1091.9; 925.3; 3572.1
SECONDARY
Part B: Duration of Response (DOR)
NA
SECONDARY
Part B: Time to Response (TTR)
1.69
SECONDARY
Part B: Cmax of BGB-10188 After a Single Dose
75.9
SECONDARY
Part B: Cmax of BGB-10188 at Steady State
89.0
SECONDARY
Part B: AUC 0-24 h of BGB-10188 After a Single Dose
418.3
SECONDARY
Part D: Overall Response Rate (ORR)
20.0; 20.0; 0.0; 9.1; 0.0; 14.3
SECONDARY
Parts D and E: Duration of Response (DOR)
4.1; 8.3; NA; 6.2
SECONDARY
Parts D and E: Disease Control Rate (DCR)
60.0; 20.0; 16.7; 36.4; 40.0; 14.3
SECONDARY
Parts D and E: Time to Response (TTR)
2.23; 2.30; 4.24; 2.30
SECONDARY
Part D: Cmax of BGB-10188 After a Single Dose
10.0; 12.5; 29.4; 88.8; 440.5; 811.1
SECONDARY
Part D: Cmax of BGB-10188 at Steady State
6.2; 16.8; 74.5; 115.7; 466.9; 798.3
SECONDARY
Part D: AUC 0-24h of BGB-10188 After Single Dose
98.0; 39.8; 110.7; 357.9; 2204.0; 4646.6
SECONDARY
Part D: AUC 0-24h of BGB-10188 at Steady State
366.6; 153.9; 249.9; 575.9; 3448.2; 4618.5
SECONDARY
Part E: Progression-Free Survival (PFS)
1.9; 1.9
SECONDARY
Part E: Clinical Benefit Rate (CBR)
0.0; 0.0
SECONDARY
Part E: Cancer Antigen (CA)-125 Response Rate Per Gynecological Cancer Intergroup
0.0; 0.0
SECONDARY
Part E: Cmax of BGB-10188 After Single Dose
120.0; 254.5
SECONDARY
Part E: Cmax of BGB-10188 at Steady State
232.2; 568.2
SECONDARY
Part E: AUC0-24h of BGB-10188 After Single Dose
1106.3; 2030.5

Eligibility Criteria

Key Inclusion Criteria

Parts A, B and C

  • Confirmed diagnosis of one of the following:
  • Part A: R/R CLL/SLL, R/R MZL, R/R FL, R/R MCL or R/R DLBCL
  • Part B: R/R FL, R/R MCL, or R/R DLBCL
  • Part C: R/R FL, R/R MCL, or R/R DLBCL

CLL = chronic lymphocytic leukemia; SLL = small lymphocytic lymphoma; MZL = marginal zone lymphoma

  • Participants with MZL, FL, MCL, DLBCL, or SLL must have had at least one bi-dimensionally measurable nodal lesion greater than (>) 1.5 centimeters (cm) in the longest diameter or extranodal lesion that is > 1 cm in the longest diameter by computed tomography (CT) scan or magnetic resonance imaging (MRI), as defined by the Lugano Classification.

Parts D and E

  • Part D: Histologically or cytologically confirmed unresectable locally advanced or metastatic solid tumors previously treated with standard systemic therapy (including prior chemotherapy, radiotherapy, target therapy, and immunotherapy as locally, or guidance approved therapy) or for which treatment is not available or not tolerated. Enrollment was limited to participants with advanced solid tumors for which there was clinical evidence of response to T-cell based immuno-oncology agents (e.g., non-small cell lung cancer [NSCLC], small cell lung cancer [SCLC], head and neck squamous cell cancer, hepatocellular carcinoma, gastric or gastroesophageal junction carcinoma, nasopharyngeal carcinoma, renal cell carcinoma, cervical cancer, triple-negative breast cancer, ovarian cancer (OC), endometrial carcinoma, esophageal cancer, melanoma, urothelial carcinoma or participant with confirmed microsatellite instability-high [MSI-H] or mismatch repair deficient [dMMR] solid tumor, etc.). Enrollment of tumor types beyond above situations required sponsor's approval.
  • Part E: Participants with histologically or cytologically confirmed epithelial OC (including fallopian or primary peritoneal cancer) previously treated with 1 to 3 lines of systemic anticancer treatment; must have been platinum resistant and checkpoint inhibitor (CPI) naïve.
  • Participants must have had measurable disease as assessed by RECIST v1.1.

Key Exclusion Criteria

Parts A, B and C

  • History of allogeneic stem-cell transplantation or chimeric antigen receptor-T (CAR-T) cell therapy.
  • For participants with DLBCL in Part A, classified as T-cell/histiocyte-rich large B-cell lymphoma, high-grade B-cell lymphoma with myelocytomatosis viral oncogene homolog and B-cell lymphoma (BCL)-2 and/or BCL-6 rearrangements, high grade B-cell lymphoma, primary mediastinal large B-cell lymphoma, Epstein-Barr virus positive DLBCL, and transformed DLBCL.

Parts A, B, C, D and E

  • Prior exposure to PI3K inhibitor. For participants in Part B and Part C, prior exposure to BTK inhibitor and/or PI3K inhibitor.
  • Any approved anticancer therapy, including hormonal therapy, or any investigational agent or participation in another clinical study with therapeutic intent within 14 days before first dose.
  • Treatment with systemic immune-stimulatory agents (including, but not limited to, interferons and interleukin-2) within 2 weeks or 5 half-lives of the drug, whichever was later, before first dose.
  • Known human immunodeficiency virus (HIV) infection, or serologic status reflecting active viral hepatitis B (HBV) or viral hepatitis C (HCV) infection as follows:
  • HBsAg (+), or
  • HBcAb (+) and HBV DNA detected, or
  • Presence of HCV antibody. Participants with presence of HCV antibody were eligible if HCV ribonucleic acid (RNA) was undetectable

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

View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT04282018). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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