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Study of the Safety and Pharmacokinetics of BGB-3111 in Subjects With B-Cell Lymphoid Malignancies

Phase 1
Completed
Conditions
B-cell Malignancies
Interventions
Registration Number
NCT02343120
Lead Sponsor
BeiGene
Brief Summary

This study evaluated the safety, tolerability, pharmacokinetic profile and efficacy of BGB-3111 in participants with B-cell lymphoid malignancies.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
385
Inclusion Criteria
  1. Aged ≥ 18 years, voluntarily consented to the study.
  2. WHO classification defined B-lymphoid malignancy, with the exception of Burkitt lymphoma/leukemia, plasma cell myeloma, acute lymphoblastic leukemia, lymphoblastic lymphoma, and plasmablastic lymphoma.
  3. Requirement for treatment in the opinion of the investigator.
  4. Disease which has relapsed, or is refractory, following at least one line of therapy, with no therapy of higher priority available.
  5. Eastern Cooperative Oncology Group (ECOG) performance status of 0-2.
  6. Adequate hematologic function, as defined by neutrophils ≥ 1.0 x 10^9/L and platelets ≥ 50 x 10^9/L; participants with neutrophils < 1.0 x 10^9/L due to marrow infiltration are allowed to receive growth factors to bring pre-treatment neutrophils to ≥ 1.0 x 10^9/L.
  7. Adequate renal function, as defined by creatinine clearance of ≥ 30 ml/min (as estimated by the Cockcroft-Gault equation or as measured by nuclear medicine scan or 24 hour urine collection).
  8. Adequate liver function, as defined by aspartate aminotransferase (AST) and alanine aminotransferase (ALT) ≤ 3 x upper limit of normal (ULN), and bilirubin ≤ 1.5 x ULN (unless documented Gilbert's syndrome).
  9. International normalized ratio (INR) ≤ 1.5 and activated partial thromboplastin time (APTT) ≤ 1.5 x ULN.
  10. Female participants of childbearing potential and non-sterile males must practice at least one of the following methods of birth control with partner(s) throughout the study and for 90 days after discontinuing study drug: total abstinence from sexual intercourse, double-barrier contraception, IUD or hormonal contraceptive initiated at least 3 months prior to first dose of study drug.
  11. Male participants must not donate sperm from initial study drug administration, until 90 days after drug discontinuation.
Exclusion Criteria
  1. Current central nervous system (CNS) involvement by disease
  2. Current histologically transformed disease.
  3. Prior Bruton's tyrosine kinase (BTK) inhibitor treatment.
  4. Allogeneic stem cell transplantation within 6 months, or has active graft-versus-host disease (GVHD) requiring ongoing immunosuppression.
  5. Receipt of the following treatment prior to first dose of zanubrutinib: corticosteroids given with anti-neoplastic intent within 7 days, chemotherapy or radiotherapy within 2 weeks, monoclonal antibody within 4 weeks.
  6. Not recovered from toxicity of any prior chemotherapy to grade ≤ 1.
  7. History of other active malignancies within 2 years of study entry, with exception of (1) adequately treated in-situ carcinoma of cervix; (2) localized basal cell or squamous cell carcinoma of skin; (3) previous malignancy confined and treated locally (surgery or other modality) with curative intent.
  8. Uncontrolled systemic infection requiring parenteral anti-microbial therapy.
  9. Major surgery in the past 4 weeks.
  10. Known HIV, or active hepatitis B or hepatitis C infection (detected positive by PCR).
  11. Cardiovascular disease resulting in New York Heart Association function status of ≥ 3.
  12. Significant active renal, neurologic, psychiatric, hepatic or endocrinologic disease that in the investigator's opinion would adversely impact on his/her participating in the study.
  13. Inability to comply with study procedures.
  14. On medications which are cytochrome P450 (CYP) 3A inhibitors.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
ZanubrutinibZanubrutinibParticipants were administered up to 320 mg total daily dose of zanubrutinib until disease progression, intolerance or death, withdrawal of consent, or loss to follow-up
Primary Outcome Measures
NameTimeMethod
Part 1 and Part 2: Number of Participants With Adverse EventsUp to approximately 6 years and 7 months

Number of participants with adverse events and serious adverse events, including clinically relevant physical examinations and laboratory measurements

Part 1: Recommended Phase 2 Dose (RP2D) for ZanubrutinibMonth 9

RP2D for zanubrutinib was the maximum tolerated dose (MTD) or less, which was determined by testing increasing doses up to 320 mg QD

Secondary Outcome Measures
NameTimeMethod
Part 1 and Part 2: Area Under the Curve From Time 0 to the Last Sampling Time Point Within the Dose Interval (AUClast) of ZanubrutinibWeek 1 Day 1 pre-dose, 0.5, 1, 2, 3, 4, and 8 hours
Part 1 and Part 2: Apparent Clearance (CL/F) of ZanubrutinibWeek 1 Day 1 pre-dose, 0.5, 1, 2, 3, 4, and 8 hours
Part 1 and Part 2: Apparent Terminal Half-life (t1/2) of ZanubrutinibWeek 1 Day 1 pre-dose, 0.5, 1, 2, 3, 4, and 8 hours
Part 1 and Part 2: Area Under the Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of ZanubrutinibWeek 1 Day 1 pre-dose, 0.5, 1, 2, 3, 4, and 8 hours
Part 1 and Part 2: Maximum Observed Plasma Concentration (Cmax) After Administration of ZanubrutinibWeek 2 Day 1 pre-dose and 24 hours
Part 1 and Part 2: Time to Maximum Observed Plasma Concentration (Tmax) of ZanubrutinibWeek 2 Day 1 pre-dose and 24 hours
Part 1 and Part 2: Progression-free Survival (PFS)Up to 6 years and 7 months

PFS is defined as the time from the first dose date of study drug to the date of the earliest occurrence of progressive disease or death due to any cause, whichever occurs first. Efficacy results are reported for each of the B-cell malignancy subtypes: chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), Waldenström macroglobulinemia (WM), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), Richter's Transformation (RT), and Hairy cell leukemia (HCL).

Part 1 and Part 2: Overall Survival (OS)Up to 6 years and 7 months

OS is defined as the time from the date of the first dose to death due to any cause. Efficacy results are reported for each of the B-cell malignancy subtypes: chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), Waldenström macroglobulinemia (WM), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), Richter's Transformation (RT), and Hairy cell leukemia (HCL).

Part 1 and Part 2: Apparent Volume of Distribution of Zanubrutinib During the Terminal Phase (Vz/F)Week 1 Day 1 pre-dose, 0.5, 1, 2, 3, 4, and 8 hours
Part 1 and Part 2: Overall Response Rate (ORR)Up to 6 years and 7 months

ORR is defined as the percentage of participants with partial or complete response (CR), as assessed by the investigator. For CLL/SLL, ORR includes partial response (PR) with lymphocytosis (PR-L) or better (includes PR-L, PR, nodular PR or nPR and CR with incomplete marrow recovery or CRi) and for MW, ORR includes minor response or better. Efficacy results are reported for each of the B-cell malignancy subtypes: chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), Waldenström macroglobulinemia (WM), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), Richter's Transformation (RT), and Hairy cell leukemia (HCL).

Part 1 and Part 2: Duration of Response (DOR)Up to 6 years and 7 months

DOR for responders is defined as time from the date of the earliest qualifying response to the date of progressive disease or death for any cause, whichever occurs earlier. Efficacy results are reported for responders (defined as PR or better, except CLL/SLL and WM) in each of the B-cell malignancy subtypes: chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL; PR with lymphocytosis or better), Waldenstrom macroglobulinemia (WM; minor response or better), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), Richter's Transformation (RT), and Hairy cell leukemia (HCL).

Part 1 and Part 2: Complete Response Rate (CRR)Up to 6 years and 7 months

CRR is defined as the percentage of participants who achieve a complete response, as assessed by the investigator. For CLL/SLL, CRR includes CRi or better. For WM, CRR includes very good partial response (VGPR) or better. Efficacy results are reported for each of the B-cell malignancy subtypes: chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), Waldenström macroglobulinemia (WM), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), Richter's Transformation (RT), and Hairy cell leukemia (HCL).

Part 1 and Part 2: Partial Response (PR) or BetterUp to 6 years and 7 months

PR or better is defined as the percentage of participants who achieve a partial response or better, as assessed by the investigator. For CLL/SLL, includes PR, nPR, CRi, CR and for WM includes PR, VGPR, and CR. Efficacy results are reported for the B-cell malignancy subtypes chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) and Waldenström macroglobulinemia (WM).

Number of Participants With Greater Than 75% Bruton's Tyrosine Kinase (BTK) OccupancyWeek 1 Day 1 (W1D1) predose, W1D1 4 hours, W1D2 24 hours, W1D3 predose, and W2D1 predose

Number of participants with greater than 75% BTK occupancy of zanubrutinib in peripheral blood mononuclear cells (PBMCs)

Trial Locations

Locations (23)

St George Hospital

🇦🇺

Sydney, New South Wales, Australia

Sir Charles Gairdner Hospital

🇦🇺

Nedlands, Western Australia, Australia

Peter MacCallum Cancer Centre, East Melbourne

🇦🇺

Parkville, Victoria, Australia

Derriford Hospital

🇬🇧

Plymouth, Devon, United Kingdom

Banner MD Anderson Cancer Centre

🇺🇸

Gilbert, Arizona, United States

University of Michigan

🇺🇸

Ann Arbor, Michigan, United States

Mayo Clinic

🇺🇸

Rochester, Minnesota, United States

M.D. Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Concord Repatriation General Hospital

🇦🇺

Concord, New South Wales, Australia

Westmead Hospital

🇦🇺

Westmead, New South Wales, Australia

Princess Alexandra Hospital

🇦🇺

Brisbane, Queensland, Australia

Monash Health

🇦🇺

Clayton, Victoria, Australia

Austin Health

🇦🇺

Heidelberg, Victoria, Australia

St Vincent's Hospital

🇦🇺

Melbourne, Victoria, Australia

Policlinico S.Orsola Malpighi, AOU di Bologna

🇮🇹

Bologna, Italy

Dong-A University Medical Centre

🇰🇷

Busan, Korea, Republic of

Melbourne Health

🇦🇺

Parkville, Victoria, Australia

Ospedale Maggiore Policlinico, Fondazione IRCCS Ca' Granda

🇮🇹

Milano, Italy

Inje University Busan Paik Hospital

🇰🇷

Busan, Korea, Republic of

Samsung Medical Center

🇰🇷

Seoul, Korea, Republic of

National Cancer Center

🇰🇷

Goyang-si, Korea, Republic of

North Shore Hospital

🇳🇿

Auckland, New Zealand

Royal Hobart Hospital

🇦🇺

Hobart, Tasmania, Australia

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