Recent Updates
Recently added Catalysts

Acalabrutinib

Phase 3

Chronic Lymphocytic Leukemia | Small molecule | Oncology |AstraZeneca PLC|Last Updated: Sep 4, 2026

Target and mechanism

Molecular targetBTK
Target classInhibitor
ModalitySmall molecule

Success Probability

Subscribe to view

Market & Valuation

Subscribe to view

Trial Design

RandomizedACTIVE_CONTROLLEDDMCBiomarker
Total Trials2
Total Enrollment1,536

FDA Designations

PRIORITY_REVIEW

Clinical trial landscape

Acalabrutinib · 23 trials · 43 indications

Phase 3 6Phase 2 9Phase 1 8
NCT03836261Study of Acalabrutinib (ACP-196) in Combination With Venetoclax (ABT-199), With and Without Obinutuzumab (GA101) Versus Chemoimmunotherapy for Previously Untreated CLLChronic Lymphocytic Leukemia
ACTIVE NOT_RECRUITING984 Analytics
NCT05057494A Study of Acalabrutinib Plus Venetoclax Versus Venetoclax Plus Obinutuzumab in Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic LymphomaChronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
ACTIVE NOT_RECRUITING607 Analytics
NCT04529772A Combination of Acalabrutinib With R-CHOP in Subjects With Previously Untreated Non-GCB DLBCL (ACE-LY-312)Diffuse Large B-Cell Lymphoma
ACTIVE NOT_RECRUITING611 Analytics
NCT04075292Study of Acalabrutinib Versus Chlorambucil Plus Rituximab in Adult Subjects With Previously Untreated Chronic Lymphocytic LeukemiaUntreated Chronic Lymphocytic Leukemia
ACTIVE NOT_RECRUITING155 Analytics
NCT04008706Acalabrutinib Safety Study in Untreated and Relapsed or Refractory Chronic Lymphocytic Leukemia PatientsChronic Lymphocytic Leukemia
COMPLETED552 Analytics
NCT02972840A Study of BR Alone Versus in Combination With Acalabrutinib in Subjects With Previously Untreated MCLLymphoma, Mantle Cell
ACTIVE NOT_RECRUITING635 Analytics
PHASE3ACTIVE NOT_RECRUITING
Study of Acalabrutinib (ACP-196) in Combination With Venetoclax (ABT-199), With and Without Obinutuzumab (GA101) Versus Chemoimmunotherapy for Previously Untreated CLL
Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
A Study of Acalabrutinib Plus Venetoclax Versus Venetoclax Plus Obinutuzumab in Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
Chronic Lymphocytic Leukemia or Small Lymphocytic LymphomaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
A Combination of Acalabrutinib With R-CHOP in Subjects With Previously Untreated Non-GCB DLBCL (ACE-LY-312)
Diffuse Large B-Cell LymphomaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
Study of Acalabrutinib Versus Chlorambucil Plus Rituximab in Adult Subjects With Previously Untreated Chronic Lymphocytic Leukemia
Untreated Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3COMPLETED
Acalabrutinib Safety Study in Untreated and Relapsed or Refractory Chronic Lymphocytic Leukemia Patients
Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
A Study of BR Alone Versus in Combination With Acalabrutinib in Subjects With Previously Untreated MCL
Lymphoma, Mantle CellUnlock trial analytics

Study Endpoints

Primary Endpoints

To evaluate the efficacy of acalabrutinib with venetoclax (Arm A) compared to chemoimmunotherapy fludarabine/cyclophosphamide/rituximab [FCR] or bendamustine/rituximab [BR] (Arm C): PFS
6 years

Progression-free survival (PFS) after randomization, defined as the time from randomization to the first occurrence of disease progression or death from any cause (whichever occurs first), as determined by the Independent Review Committee (IRC) according to the International Workshop on Chronic Lymphocytic Leukemia (IWCLL) 2018 criteria

Progression-free Survival (PFS)
Until progressive disease (PD) [assessed Up to 6.6 Years].

To assess whether minimal residual disease (MRD)-driven finite AV treatment is NI to MRD-driven finite VO treatment with respect to PFS. PFS is defined as the time from the date of randomization until date of objective progressive disease per International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018 criteria as assessed by the investigator or death from any cause in the absence of progression.

Progression-free survival (PFS) per the Lugano Classification for NHL in Arm A compared to Arm B
at every single visit up to 60 months
Progression Free Survival (PFS) Assessed by BICR
Response evaluations performed every 12 weeks from Cycle 4 Day 1 to Cycle 25, then every 24 weeks until PD or death, up to DCO date of 03 January 2024 (a maximum of approximately 47.5 months)

PFS was defined as the time from randomization to PD (assessed by BICR according to International Workshop on Chronic Lymphocytic Leukaemia \[iwCLL\] 2018 guideline criteria) or death due to any cause. PD was defined as meeting at least 1 of the below criteria of groups(g) A or B. gA: increase of ≥50% from baseline (BL) or from response in lymph nodes or liver and/or spleen size; any constitutional symptoms; increase of ≥50% over nadir with absolute count ≥ 5×10\^9/liter (L) in circulating lymphocyte count (CLC); gB: decrease of ≥50% from BL secondary to CLL in platelet count; decrease of ≥2 gram per deciliter (g/dL) from BL secondary to CLL in hemoglobin (Hb); increase of CLL cells by ≥50% on successive biopsies in bone marrow (BM). Median PFS was calculated using Kaplan-Meier method and its confidence interval (CI) using Brookmeyer-Crowley method.

Number of Participants With Adverse Events (AEs)
Up to safety follow-up period (about 30 days from last dose) (approximately 74 months)

The safety and tolerability of acalabrutinib monotherapy were evaluated in participants with treatment-naïve or relapsed/refractory chronic lymphocytic leukemia. Treatment-emergent AEs (TEAEs) were defined as AEs that started after first dose of acalabrutinib or which started prior to first dose of acalabrutinib but worsened following first dose of acalabrutinib, and where the start date of worsening was also no later than 30 days after the date of last dose of acalabrutinib or the first date starting new anticancer therapy, whichever was earlier. Adverse events of special interest (AESI) were defined as ventricular arrhythmias. Events of clinical interest (ECI) were defined as cardiac events, hepatotoxicity, hypertension, infections, interstitial lung disease/pneumonitis, hemorrhage (major hemorrhage), cytopenias (anemia, leukopenia, thrombocytopenia), second primary malignancies, and tumor lysis syndrome. Common Terminology Criteria for Adverse Events = CTCAE

Progression-free survival per the Lugano Classification for NHL in Arm 1 compared to Arm 2
Up to 6 years

Defined as the time from the date of randomization until disease progression (assessed by the IRC per the Lugano Classification for NHL) or death from any cause, whichever occurs first.

Overall Response Rate (ORR)
ORR assessed at multiple timepoints during treatment period (each cycle is 28 days). Timepoint for primary analysis is at completion of cycle 14

ORR, defined as the proportion of participants who achieve best response of CR, CRi, nPR, or PR per iwCLL criteria as assessed by the investigator.

Cardiac magnetic resonance imaging changes
Baseline to 3-month post acalabrutinib initiation

The cardiac MRI changes that will be assessed include Extracellular volume (ECV), Native T1, and T2, where changes in ECV from baseline to 3-month post acalabrutinib initiation would be the primary endpoint

Percentage of patients with Grade 3 to 4 treatment emergent adverse events (TEAEs)
Cycle 1 Day 1 (Cycles 1 to 8 is 21 days and Cycles 9 to 28 is 28 days) through End of treatment EoT [30 days of discontinuation] (Up to 3.5 Years)
MRD-negative CR rate
At the end of AVR induction, i.e., following completion of Cycle 13 (each cycle is 28 days)

MRD-negative CR rate is defined as the proportion of participants who achieved MRD-negativity in peripheral blood by NGS at a threshold of 10-5 while in CR per the Lugano Classification for NHL at the end of AVR induction

Complete response (CR) rate
Up to start of cycle 6 (each cycle = 28 days)

Complete response rate will be calculated, and a 95% confidence interval will be estimated using the Clopper-Pearson method.

Incidence of grade 3+ adverse events
Up to 30 days post treatment

Assessed by Common Terminology Criteria for Adverse Events (CTCAE) version 5.0.

Disease assessment of bone marrow (BM) undetectable-minimal residual disease,10-4 sensitivity (MRD4) (Treatment-naive [TN] cohort)
Up to 1 year end of cycle 9; each cycle 28 days
Disease assessment of BM undetectable-MRD4 (Relapsed/refractory [R/R] cohort)
Up to 1 year end of cycle 14; each cycle 28 days
Number of Participants With Adverse Events and Serious Adverse Events
Screening to 28 (+3) days after last dose of acalabrutinib (for acalabrutinib + BSC participants) or to 38 (+3) days after randomization (for BSC alone participants)
Percentage of Participants Alive and Free of Respiratory Failure at Day 28
At Day 28

Respiratory failure, is defined based on resource utilization of any of the following modalities: a) Endotracheal intubation and mechanical ventilation b) Oxygen delivered by highflow nasal cannula (heated, humidified, oxygen delivered via reinforced nasal cannula at flow rates \>20 L/min with fraction of delivered oxygen ≥0.5) c) Noninvasive positive pressure ventilation or continuous positive airway pressure d) Extracorporeal membrane oxygenation

Percentage of Participants Alive and Free of Respiratory Failure at Day 14
At Day 14

Respiratory failure, is defined based on resource utilization of any of the following modalities: a) Endotracheal intubation and mechanical ventilation b) Oxygen delivered by high-flow nasal cannula (heated, humidified, oxygen delivered via reinforced nasal cannula at flow rates \>20 L/min with fraction of delivered oxygen ≥0.5) c) Non-invasive positive pressure ventilation or continuous positive airway pressure d) Extracorporeal membrane oxygenation

Randomised Component - Progression free survival (PFS)
Time from randomisation to the date of progression or death from any cause, whichever came first, assessed up to 24 months..

Progression free survival (PFS) defined as the time from randomisation to the date of progression or death from any cause. Progression will be defined by the modified Cheson criteria (Appendix 1). Patients who are alive and progression free at the time of analysis will be censored at date last seen. Any participants who withdraw or are lost to follow-up will also be censored at date last seen.

Registration Arm - Cohort 1 - Overall Response
Response assessed at 24 weeks of treatment

Overall response after 24 weeks of treatment based on the modified Cheson criteria (Appendix 1). Complete response (CR) and partial response (PR) are considered to be positive responses for assessment of this outcome. Participants who withdraw prior to the 6 month assessment or do not have the 6 month assessment will be considered non responders.

Registration Arm - Cohort 2 - Overall Response
Response assessed after 6 cycles of treatment. Each cycle is 21 days.

Overall response after 6 cycles of treatment, defined by the modified Cheson criteria (Appendix 1). CR and PR are considered to be positive responses for assessment of this outcome. Participants who withdraw prior to the post-cycle-6 assessment or do not have the post-cycle-6 assessment will be considered non-responders.

Incidence of adverse events
Up to 30 days post axicabtagene ciloleucel infusion

Toxicity as defined by the following: grade \>= 3 cytokine release syndrome, grade \>= 3 neurotoxicity within 30 days of infusion of axicabtagene ciloleucel. Grading will be done in accordance with the National Cancer Institute Common Terminology Criteria for Adverse Events version 5.0 for neurotoxicity and the Lee Criteria for cytokine release syndrome, unless otherwise specified.

Recommended Phase 2 Dose for acalabrutinib
5 months

The RP2D will be defined as the highest dose level for which there are no more than 1/6 DLTs observed.

Complete Remission Rate
7 Months

Complete remission (CR) rate after 7 cycles of treatment with AVO in treatment naïve (TN) transplant ineligible MCL and TN transplant-eligible, TP53 mutated MCL, cohort B. CR rate after 7 cycles of treatment with AVO in TN TP53-mutated MCL, expansion cohort D. Complete remission (CR) is defined radiographically using 2014 Lugano criteria and a negative bone marrow biopsy by histology, immunohistochemistry, and flow cytometry, if bone marrow was initially involved by MCL at screening. CR, a primary endpoint measured after 7 cycles of AVO, does not incorporate minimal residual disease (MRD) testing

MRD negative complete remission rate
7 months

Minimal residual disease (MRD) negative (\<1 in 106 cells) CR rate after 7 cycles of treatment with AVO in TN transplant-eligible, TP53 wild type MCL, cohort C

Area under plasma concentration-time curve from time zero to infinity (AUCinf)
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on Day 1, and 24 hours post-dose on Day 2

Assessment of AUCinf for acalabrutinib and ACP-5862 (metabolite of acalabrutinib) following administration of capsule with and without rabeprazole.

Area under the plasma concentration-time curve from time zero to time of last quantifiable concentration (AUClast)
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on Day 1, and 24 hours post-dose on Day 2

Assessment of AUClast for acalabrutinib and ACP-5862 following administration of capsule with and without rabeprazole.

Maximum observed plasma concentration (Cmax)
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on Day 1, and 24 hours post-dose on Day 2

Assessment of Cmax for acalabrutinib and ACP-5862 following administration of capsule with and without rabeprazole.

Phase I: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
From the first dose administration up to 30 days following the date of last dose of study treatment, approximately 25 months.

An AE is the development of an undesirable medical condition or the deterioration of a pre-existing medical condition following or during exposure to a pharmaceutical product, whether or not considered causally related to the product. A SAE is an AE occurring during any study phase, that fulfils 1 or more of the following criteria: death, life-threatening, in-participant hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, congenital abnormality or birth defect, and an important medical event that may jeopardize the participant or may require medical treatment to prevent 1 of the outcomes listed above. AEs leading to discontinuation of acalabrutinib were those with action taken was 'Drug Permanently Discontinued' for acalabrutinib.

Phase I: Area Under the Plasma Concentration-Time Curve From Zero to Infinity (AUCinf) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the AUCinf of acalabrutinib and ACP-5862 in plasma. The AUCinf was determined using non-compartmental method.

Phase I: Area Under the Plasma Concentration-Time Curve From Zero to 12 Hours (AUC0-12) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8 and 12 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the AUC0-12 of acalabrutinib and ACP-5862 in plasma. The AUC0-12 was determined using non-compartmental method.

Phase I: Area Under the Plasma Concentration-Time Curve From Zero to the Time of the Last Quantifiable Concentration (AUClast) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the AUClast of acalabrutinib and ACP-5862 in plasma. The AUClast was determined using non-compartmental method.

Phase I: Maximum Observed Plasma Drug Concentration (Cmax) of Acalabrutinib and ACP-5862 Post Single and Multiple Dose of Acalabrutinib
Single dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8 and 12 hours postdose on Cycle 0 Day 1; Multiple dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the Cmax of acalabrutinib and ACP-5862 in plasma. The Cmax was determined using non-compartmental method.

Phase I: Time to Reach Maximum Observed Concentration (Tmax) of Acalabrutinib and ACP-5862 Post Single and Multiple Dose of Acalabrutinib
Single dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8 and 12 hours postdose on Cycle 0 Day 1; Multiple dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the tmax of acalabrutinib and ACP-5862 in plasma. The tmax was determined using non-compartmental method.

Phase I: Apparent Total Body Clearance of Drug (CL/F) of Acalabrutinib Post Single and Multiple Dose of Acalabrutinib
Single dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8 and 12 hours postdose on Cycle 0 Day 1; Multiple dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Urine samples were collected to determine the CL/F of acalabrutinib. The CL/F was determined using non-compartmental method.

Phase I: Apparent Volume of Distribution (Vz/F) of Acalabrutinib Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the Vz/F of acalabrutinib in plasma. The Vz/F was determined using non-compartmental method.

Phase I: Terminal Elimination Rate Constant (λz) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the λz of acalabrutinib and ACP-5862 in plasma. The λz was determined using non-compartmental method.

Phase I: Terminal Phase Half-Life (t1/2λz) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the t1/2λz of acalabrutinib and ACP-5862 in plasma. The t1/2λz was determined using non-compartmental method.

Phase I: Metabolite/Parent Drug Cmax Ratio (MRCmax) of Acalabrutinib and ACP-5862 Post Single and Multiple Dose of Acalabrutinib
Single dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8 and 12 hours postdose on Cycle 0 Day 1; Multiple dose: Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the MRCmax of acalabrutinib and ACP-5862 in plasma. The MRCmax was determined using non-compartmental method.

Phase I: Metabolite/Parent Drug AUC Ratio (MRAUCinf) of Acalabrutinib and ACP-5862 Post Single Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 0 Day 1

Blood samples were collected to determine the MRAUCinf of acalabrutinib in plasma. The MRAUCinf was determined using non-compartmental method.

Phase I: Area Under the Plasma Concentration-Time Curve Across the Dosing Interval (AUCτ) of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the AUCτ of acalabrutinib and ACP-5862 in plasma. The AUCτ was determined using non-compartmental method.

Phase I: Minimum Observed Plasma Drug Concentration (Cmin) of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the Cmin of acalabrutinib and ACP-5862 in plasma. The Cmin was determined using non-compartmental method.

Phase I: Metabolite/Parent Drug AUCτ Ratio (MRAUCτ) of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the MRAUCτ of acalabrutinib and ACP-5862 in plasma. The MRAUCτ was determined using non-compartmental method.

Phase I: Temporal Change Parameter (TCP) in Systemic Exposure of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the TCP of acalabrutinib and ACP-5862 in plasma. The TCP in systemic exposure was calculated as AUCτ (steady state)/AUCinf (first dose). The TCP was determined using non-compartmental method.

Phase I: Accumulation Ratio of AUCτ (Rac AUC) of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the Rac AUC of acalabrutinib and ACP-5862 in plasma. The Rac AUC was calculated as AUCτ (steady state)/AUCτ (first dose). The Rac AUC was determined using non-compartmental method.

Phase I: Accumulation Ratio of Cmax (Rac Cmax) of Acalabrutinib and ACP-5862 Post Multiple Dose of Acalabrutinib
Pre-dose and 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24 and 48 hours postdose on Cycle 1 Day 8

Blood samples were collected to determine the Rac Cmax of acalabrutinib and ACP-5862 in plasma. The Rac Cmax was calculated as Cmax (steady state)/Cmax (first dose). The Rac Cmax was determined using non-compartmental method.

Phase II: Objective Response Rate (ORR) Assessed by Blinded Independent Central Review (BICR)
Response evaluations performed at the end of Cycles 2, 4 and 6; and then every 12 weeks +/- 7 days through Cycle 25, and then every 24 weeks +/- 7 days thereafter. Assessed until 18 December 2023.

The ORR \[based on International workshop on chronic lymphocytic leukemia (iwCLL) 2018 criteria as assessed by the BICR\] was defined as the percentage of participants who achieved a complete response (CR), CR with incomplete marrow recovery (CRi), nodular partial response (nPR), and partial response (PR). The ORR and the corresponding 95% 2-sided confidence interval (CI) of ORR were presented based on Clopper-Pearson exact method.

Plasma Acalabrutinib PK Parameters
Severe HI: pre-dose, and 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24, 36, 48, 60, 72 hrs post-dose. Normal HI: pre-dose, and 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24 hrs post-dose.

Area Under the Concentration-Time Curve

Maximum Plasma Acalabrutinib Concentration
Severe HI: pre-dose, and 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24, 36, 48, 60, 72 hrs post-dose. Normal HI: pre-dose, and 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24 hrs post-dose.

Maximum Cmax

Adverse Events (AEs), Serious Adverse Events (SAEs) and dose-limiting toxicities (DLTs) as a measure of safety and tolerability.
From the first dose of study treatment to data cut-off date defined as 2 years after last subject enrolled. In Part 1, DLT will be evaluated in Cycle 1 (28 days). In Part 3, DLT will be evaluated in Cycle 2 (28 days).

Acalabrutinib is considered as safe and tolerable if ≦1 of 6 patients experiences a DLT.

Part 1: Incidence of Treatment-emergent Adverse Events.
From the first dose of study drug until study discontinuation, 30 days after the last dose of study drug or one day before the first subsequent anticancer therapy, whichever was earlier, up to 80.7 months (the maximum participant's time on this study).

Treatment-emergent adverse events were used to characterize the safety profile of acalabrutinib alone or in combination with rituximab in participants with relapsed/refractory follicular lymphoma (R/R FL).

Part 2: Investigator Assessed Objective Response Rate (ORR) According to the Lugano Classification for Non-Hodgkin Lymphoma (NHL).
Based on all response assessments since the first dose of study drug until study discontinuation or the initiation of subsequent anticancer therapy, whichever was earlier, up to 65.1 months (the maximum participant's time on this study).

The objective response rate (ORR) is used to characterize the activity of acalabrutinib alone or in combination with rituximab in participants with relapsed/refractory marginal zone lymphoma (R/R MZL).

Part 3: Incidence of Treatment-emergent Adverse Events.
From the first dose of study drug until study discontinuation, 30 days after the last dose of study drug or one day before the first subsequent anticancer therapy, whichever was earlier, up to 54.3 months (the maximum participant's time on this study).

Treatment-emergent adverse events were used to characterize the safety of acalabrutinib in combination with rituximab and lenalidomide in participants with relapsed/refractory follicular lymphoma (R/R FL).

Best Response and Overall Response Rate
from the start of the treatment to the last evaluable disease assessment, an average of 1 year

Best response and overall response rate per the criteria investigator uses for each disease histology. Standardized response and progression criteria is based on established criteria for B-cell malignancies, including WM (Cheson 2014; Owen 2013; Hallek 2008; Bladé 1998; and Durie 2006).

Secondary Endpoints

To evaluate the efficacy of acalabrutinib with venetoclax in combination with obinutuzumab (Arm B) compared with FCR or BR (Arm C): PFS
6 years
To evaluate the efficacy of acalabrutinib with venetoclax (Arm A) compared with FCR or BR (Arm C): PFS defined the same as above per investigator assessment.
6 years
Rate of peripheral blood (PB) undetectable minimal residual disease (uMRD) based on a clonoSEQ^®
Screening (Days -45 through -1); Arm A (AV): Day 28 of Cycles 8, 14 and 24 and post treatment follow up visits; Arm B (VO): Day 28 of Cycles 6, 12 and 24 and post treatment follow up visits
Unlock Study Endpoints

Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Acalabrutinib, VenetoclaxEXPERIMENTALAcalabrutinib in combination with Venetoclax
Acalabrutinib, Venetoclax, ObinutuzumabEXPERIMENTALAcalabrutinib in combination with Venetoclax with Obinutuzumab
ChemoimmunotherapyACTIVE_COMPARATORChemoimmunotherapy FCR: Fludarabine, Cyclophosphamide and Rituximab BR: Bendamustine and Rituximab
Arm A: Acalabrutinib plus Venetoclax (AV)EXPERIMENTALParticipants will receive acalabrutinib and venetoclax orally.
Arm B: Venetoclax plus Obinutuzumab (VO)EXPERIMENTALParticipants will receive Venetoclax orally and Obinutuzumab via IV infusion.
acalabrutinib + R-CHOPEXPERIMENTALAcalabrutinib plus Rituximab, Cyclosphosphamide, Doxorubicin, Vincristine and Prednisone (R-CHOP)
placebo + R-CHOPPLACEBO_COMPARATORPlacebo plus Rituximab, Cyclophosphamide, Doxorubicin, Vincristine and Prednisone (R-CHOP)
AcalabrutinibEXPERIMENTALAcalabrutinib will be orally administered until disease progression or unacceptable toxicity
Rituximab and ChlorambucilACTIVE_COMPARATORChlorambucil orally administered and Rituximab via IV infusion for 6 cycles
Acalabrutinib in combination with bendamustine and rituximabEXPERIMENTALAcalabrutinib administered twice per day (BID) orally (PO) plus bendamustine on Days 1 and 2 and rituximab on Day 1; cycles are repeated every 28 days.
Placebo in combination with bendamustine and rituximabPLACEBO_COMPARATORMatching placebo administered BID PO plus bendamustine on Days 1 and 2 and rituximab on Day 1; cycles are repeated every 28 days.
Acalabrutinib and VenetoclaxEXPERIMENTALFor Cohort 1, each participant will be in the study for approximately 5 years (60 months) counting from C1D1, starting with 2 cycles of acalabrutinib lead-in treatment, followed by 12 cycles of AV combination treatment, and 4 years of follow-up. For Cohort 2, each participant will be in the study for approximately 5 years (60 months) counting from C1D1 starting with 2 cycles of acalabrutinib lead-in treatment, followed by 22 cycles of AV combination treatment, and 3 years of follow-up.
Treatment (acalabrutinib)EXPERIMENTALPatients receive acalabrutinib PO BID on days 1-28 of each cycle. Cycles repeat every 28 days in the absence of disease progression or unacceptable toxicity. Patients also undergo CMR, CT, bone marrow aspiration/biopsy, and collection of blood samples throughout the trial.
Acalabrutinib and RituximabEXPERIMENTALPatients will receive Dose A of acalabrutinib orally in X dosing schedule beginning on Cycle 1 Day 1 for a maximum of 28 cycles or until 2014 Lugano Classification for Non-Hodgkin's Lymphoma (NHL)-defined disease progression or another discontinuation criterion is met. Patients will also receive an intravenous (IV) infusion of Dose B rituximab on Cycle 1 Day 15 and Dose C of rituximab as an subcutaneous (SC) injection on Day 1 of Cycle 2 through Cycle 8.
Acalabrutinib + Venetoclax + RituximabEXPERIMENTALAcalabrutinib + Venetoclax + Rituximab (AVR)
Treatment (acalabrutinib, obinutuzumab)EXPERIMENTALINDUCTION PHASE: Patients receive acalabrutinib PO BID on days 1-28. Patients also receive obinutuzumab IV on days 1, 8, and 15 of cycle 3, then on day 1 of cycles 4-8. Treatments repeat every 28 days for up to 12 cycles in the absence of disease progression or unacceptable toxicity. FOLLOW-UP PHASE: After cycle 12, patients who are in CR are randomized to either discontinue acalabrutinib or to continue acalabrutinib monotherapy in the absence of disease progression or unacceptable toxicity. Patients with PR or SD after cycle 12 continue acalabrutinib monotherapy in the absence of disease progression or unacceptable toxicity. Patients with disease progression after cycle 12 discontinue study treatment. Patients with disease progression at any time prior to the conclusion of cycle 12 may continue study therapy if they are felt to be benefiting by the treating physician, but not past cycle 12.
Arm I (acalabrutinib, venetoclax, obinutuzumab)ACTIVE_COMPARATORPatients receive acalabrutinib orally (PO) twice daily (BID) on days 1-28. Beginning cycle 3, patients receive venetoclax PO once a week on days 1-28, then once daily starting cycle 4. Patients who are BM MRD4-positive or in PR also receive obinutuzumab IV over 4-6 hours on days 1, 2, 8, and 15 of cycle 15 and day 1 of cycles 16-20. Treatment repeats every 28 days (or 42 days for cycle 14) for up to 26 cycles in the absence of disease progression or unacceptable toxicity.
Arm II (acalabrutinib, venetoclax, early obinutuzumab)EXPERIMENTALPatients receive acalabrutinib PO BID on days 1-28 beginning cycle 2 and venetoclax PO once a week on days 1-28, then once daily starting cycle 4. Patients also receive obinutuzumab IV over 4-6 hours on days 1, 2, 8, and 15 of cycle 1 and day 1 of cycles 2-6. Patients who are BM MRD4-positive or in PR receive obinutuzumab IV over 4-6 hours on day 1 cycles 15-20. Treatment repeats every 28 days (or 42 days for cycle 14) for up to 26 cycles in the absence of disease progression or unacceptable toxicity.
Arm 1EXPERIMENTALAcalabrutinib+ Best Supportive Care
Arm 2NO_INTERVENTIONBest Supportive Care
Standard of Care Arm (CHOP-R)ACTIVE_COMPARATORArm in the randomised trial. CHOP-R chemoimmunotherapy will continue for up to 6 cycles (each cycle is 21 days), and will be given according to the following schedule: Rituximab, 375 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Cyclophosphamide, 750 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Doxorubicin, 50 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Vincristine, 1.4 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Prednisolone, 40 mg/m2, PO, OD, 6 cycles, days of cycle: 1-5
Experimental Arm (CHOP-R + Acalabrutinib)EXPERIMENTALArm in the randomised trial. CHOP-R chemoimmunotherapy will continue for up to 6 cycles (each cycle is 21 days), and will be given according to the following schedule: Rituximab, 375 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Cyclophosphamide, 750 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Doxorubicin, 50 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Vincristine, 1.4 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Prednisolone, 40 mg/m2, PO, OD, 6 cycles, days of cycle: 1-5 Acalabrutinib 100 mg, PO, BD will be taken on days 6-21, of each cycle - up to cycle 6. Acalabrutinib treatment will be continuous thereafter until disease progression toxicity, patient choice or death.
Cohort 1 - Acalabrutinib Monotherapy - Platform TrialEXPERIMENTALRegistration arm in platform study. Patients registered to Cohort 1 will receive 100 mg acalabrutinib monotherapy, twice daily, continuously from day 1 until disease progression, toxicity, patient choice or death.
Cohort 2 - CHOP-R + Acalabrutinib - Platform TrialEXPERIMENTALRegistration arm in platform study. CHOP-R chemoimmunotherapy will continue for up to 6 cycles (each cycle is 21 days), and will be given according to the following schedule: Rituximab, 375 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Cyclophosphamide, 750 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Doxorubicin, 50 mg/m2, IV bolus, OD, 6 cycles, days of cycle: 1 Vincristine, 1.4 mg/m2, IV infusion, OD, 6 cycles, days of cycle: 1 Prednisolone, 40 mg/m2, PO, OD, 6 cycles, days of cycle: 1-5 Acalabrutinib 100 mg, PO, BD will be taken on days 6-21, of each cycle - up to cycle 6. Acalabrutinib treatment will be continuous thereafter until disease progression toxicity, patient choice or death.
Treatment (acalabrutinib, axicabtagene ciloleucel)EXPERIMENTALBeginning up to 3 weeks and at least 24 hours prior to leukapheresis, patients receive acalabrutinib PO every 12 hours. Treatment continues in the absence of disease progression or unacceptable toxicity. Patients also receive axicabtagene ciloleucel IV at 36-96 hours after completion of lymphodepleting chemotherapy.
Acalabrutinib, Venetoclax, and ObinutuzumabEXPERIMENTALThe study will consist of 4 parts (Parts A, B, C, and D). In the relapsed/refractory (R/R) MCL setting (Part A), the phase 1 portion consists of a dose finding stage to determine the recommended phase 2 dose (RP2D). It will follow a 3+3 dose finding schema with a minimum of 6 participants. 11 participants will be enrolled in the Part A expansion cohort. Part B will enroll 24 participants with untreated mantle cell lymphoma who are transplant ineligible and/or TP53 mutated. Part C will enroll 12 participants with untreated mantle cell lymphoma who are transplant eligible and TP53 wild type. Part D will enroll 16 participants with untreated mantle cell lymphoma with a TP53 mutation determined by next generation sequencing, regardless of transplant eligibility. Each study drug is given according to a different schedule. Each treatment cycle lasts 28 days (4 weeks). * Acalabrutinib: * Obinutuzumab: * Venetoclax:
Arm AEXPERIMENTALParticipants will receive single oral dose of acalabrutinib capsule with 100 mL of water.
Arm BEXPERIMENTALParticipants will receive single oral dose of acalabrutinib capsule taken with 100 mL of COCA-COLA along with 20 mg rabeprazole.
Subjects with Severe Hepatic ImpairmentEXPERIMENTALSubjects with severe hepatic impairment (score of 10 to 15 on the Child-Pugh scale) will be administrated a 50-mg single oral dose of acalabrutinib.
Matched-Control SubjectsEXPERIMENTALSubjects with normal hepatic function will be administrated a 50-mg single oral dose of acalabrutinib.
Part 1 / Part 2EXPERIMENTALAcalabrutinib
Part 3EXPERIMENTALAcalabrutinib in combination with Obinutuzumab
Part 1: acalabrutinib Regimen 1EXPERIMENTALacalabrutinib Regimen 1 for relapsed, refractory Follicular Lymphoma subjects
Part 1: acalabrutinib Regimen 2EXPERIMENTALacalabrutinib Regimen 2 + rituximab for relapsed, refractory, or treatment naive Follicular Lymphoma subjects
Part 2: acalabrutinib Regimen 1EXPERIMENTALacalabrutinib Regimen 1 for relapsed, refractory Marginal Zone Lymphoma subjects
Part 2: acalabrutinib Regimen 2EXPERIMENTALacalabrutinib Regimen 2 + rituximab for relapsed, refractory Marginal Zone Lymphoma subjects
Part 3: acalabrutinib Regimen 1EXPERIMENTALacalabrutinib Regimen + lenalidomide + rituximab for relapsed, refractory Follicular Lymphoma subjects
Dose Escalation and ExpansionEXPERIMENTALThe acalabrutinib dose will be fixed and the ACP-319 dose will be escalated in each of three cohorts, and each cohort will take both study drugs by mouth, twice per day (BID) at approximately 12 hour intervals. Expansion groups of up to 12 subjects for Germinal center B-cell (GCB) DLBCL and Non-GCB DLBCL to take a fixed dose of acalabrutinib and ACP-319. Each disease group will take both study drugs by mouth, twice per day (BID) at approximately 12 hour intervals.

Interventions

NameTypeDescription
AcalabrutinibDRUGAcalabrutinib,
VenetoclaxDRUGVenetoclax
ChemoimmunotherapyDRUGfludarabine/cyclophosphamide/rituximab (FCR), bendamustine/rituximab (BR)
ObinutuzumabDRUGObinutuzumab
placeboDRUGPlacebo comparator
PrednisoneDRUGInvestigational Product
RituximabDRUGInvestigational Product
CyclophosphamideDRUGInvestigational Product
VincristineDRUGInvestigational Product
DoxorubicinDRUGInvestigational Product
ChlorambucilDRUGChlorambucil: 0.5 mg/kg body weight orally on Day 1 and Day 15 of Cycles 1-6
BendamustineDRUGAdministered intravenously (IV)
Biospecimen CollectionPROCEDUREUndergo collection of blood samples
Bone Marrow AspirationPROCEDUREUndergo bone marrow aspiration
Bone Marrow BiopsyPROCEDUREUndergo bone marrow biopsy
Computed TomographyPROCEDUREUndergo CT
Magnetic Resonance Imaging of the HeartPROCEDUREUndergo CMR
Quality-of-Life AssessmentOTHERAncillary studies
Questionnaire AdministrationOTHERAncillary studies
PrednisoloneDRUG40mg/m\^2, PO, OD
Axicabtagene CiloleucelBIOLOGICALGiven IV
RabeprazoleDRUGParticipants will receive twice daily oral dose of 20 mg rabeprazole on days -3, -2, and -1.
rituximab (IV)DRUG -
LenalidomideDRUG -
ACP-319DRUGOral
Unlock Study Design Details

Eligibility Criteria

Age Range18 Years to 130 Years
SexALL
Healthy VolunteersNo
Study Sites170

Inclusion Criteria: * Men and women ≥18 years of age. * Eastern Cooperative Oncology Group (ECOG) performance status of 0-2. * Diagnosis of CLL that meets published diagnostic criteria (Hallek et al. 2018) * Active disease per IWCLL 2018 criteria that requires treatment. * Participants must use hig...

Countries:United StatesArgentinaAustraliaAustriaBrazilBulgariaCanadaChinaCzechiaDenmarkFranceGermanyHungaryIsraelItalyNetherlandsPolandRussiaSaudi ArabiaSlovakiaSouth AfricaSouth KoreaSpainSwedenTaiwanTurkey (Türkiye)United KingdomBelgiumIndiaJapanMexicoPortugalUkrainePhilippinesThailandVietnamFinlandNorwayGreeceHong KongNew ZealandPeruRomaniaIrelandPuerto RicoChile
Unlock Eligibility Criteria

Recent Changes (Last 90 Days)

LOWSep 4, 2026NCT05952024lastUpdatePostDate: changed
LOWSep 2, 2026NCT05057494lastUpdatePostDate: changed
LOWSep 2, 2026NCT05951959lastUpdatePostDate: changed
LOWSep 2, 2026NCT05057494lastUpdatePostDate: changed
LOWSep 2, 2026NCT05951959lastUpdatePostDate: changed
LOWSep 2, 2026NCT05057494lastUpdatePostDate: changed
LOWSep 2, 2026NCT05951959lastUpdatePostDate: changed
LOWAug 6, 2026NCT05952024lastUpdatePostDate: changed
LOWAug 6, 2026NCT07024706lastUpdatePostDate: changed
LOWAug 6, 2026NCT05952024lastUpdatePostDate: changed
LOWAug 6, 2026NCT07024706lastUpdatePostDate: changed

Frequently asked questions about Acalabrutinib

What is Acalabrutinib used for?

Acalabrutinib is an investigational small molecule being studied for mantle-cell lymphoma, chronic lymphocytic leukemia, advanced B-cell malignancies, B-cell non-Hodgkin lymphoma, non-Hodgkin lymphoma, and infectious disease. It is also being evaluated in Richter syndrome and COVID-19. The drug is in clinical development and has not been approved for these uses.

How does Acalabrutinib work?

Acalabrutinib is a kinase inhibitor, belonging to the -tinib class of drugs. It targets and inhibits Bruton's tyrosine kinase (BTK), a protein involved in B-cell receptor signaling. By blocking this kinase, acalabrutinib is intended to disrupt the survival and proliferation of malignant B cells.

Who is developing Acalabrutinib?

Acalabrutinib is being developed by AstraZeneca PLC, a biopharmaceutical company listed on the stock exchange under the ticker AZN. AstraZeneca is conducting clinical trials to evaluate the drug's safety and efficacy across multiple oncology and infectious disease indications.

What phase is Acalabrutinib in?

Acalabrutinib is in Phase 1 clinical development. It has received priority review designation from the FDA. The drug is investigational and has not been approved for any indication. Clinical trials are ongoing to assess its potential as a treatment for various B-cell malignancies and other conditions.

What clinical trials is Acalabrutinib in?

Acalabrutinib is being studied in several clinical trials. NCT02180711 is a Phase 1 study in B-cell non-Hodgkin lymphoma. NCT03899337 is a Phase 2 trial in Richter syndrome. NCT04346199 and NCT04380688 are Phase 2 studies in hospitalized COVID-19 patients. These trials are active or completed, with a total enrollment of over 1,500 participants.

Is Acalabrutinib the same as Acalabrutinib in combination with BR?

Acalabrutinib is the same drug as Acalabrutinib in combination with BR and Acalabrutinib + R-CHOP standard of care. These names refer to acalabrutinib when used alongside specific chemotherapy regimens, such as bendamustine and rituximab (BR) or R-CHOP, in clinical trial settings.