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Pirtobrutinib

Phase 3

Chronic Lymphocytic Leukemia | Small molecule | Oncology |Eli Lilly and Company|Last Updated: Jul 17, 2026

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Trial Design
RandomizedACTIVE_CONTROLLEDDMC
Total Trials7
Total Enrollment2,996
FDA Designations
No designations recorded
Clinical trial landscape

Pirtobrutinib · 24 trials · 20 indications

Phase 3 5Phase 2 7Phase 1 12
NCT05254743A Study of Pirtobrutinib (LOXO-305) Versus Ibrutinib in Participants With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)Chronic Lymphocytic Leukemia
RECRUITING737 Analytics
NCT05023980A Study of Pirtobrutinib (LOXO-305) Versus Bendamustine Plus Rituximab (BR) in Untreated Patients With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)Chronic Lymphocytic Leukemia
ACTIVE NOT_RECRUITING309 Analytics
NCT04965493A Trial of Pirtobrutinib (LOXO-305) Plus Venetoclax and Rituximab (PVR) Versus Venetoclax and Rituximab (VR) in Previously Treated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL)Chronic Lymphocytic Leukemia
ACTIVE NOT_RECRUITING600 Analytics
NCT04662255Study of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)Lymphoma, Mantle-Cell
ACTIVE NOT_RECRUITING500 Analytics
NCT04666038Study of LOXO-305 (Pirtobrutinib) Versus Investigator's Choice (Idelalisib Plus Rituximab or Bendamustine Plus Rituximab) in Patients With Previously Treated Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)Chronic Lymphocytic Leukemia
ACTIVE NOT_RECRUITING238 Analytics
PHASE3RECRUITING
A Study of Pirtobrutinib (LOXO-305) Versus Ibrutinib in Participants With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
A Study of Pirtobrutinib (LOXO-305) Versus Bendamustine Plus Rituximab (BR) in Untreated Patients With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
A Trial of Pirtobrutinib (LOXO-305) Plus Venetoclax and Rituximab (PVR) Versus Venetoclax and Rituximab (VR) in Previously Treated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL)
Chronic Lymphocytic LeukemiaUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
Study of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)
Lymphoma, Mantle-CellUnlock trial analytics
PHASE3ACTIVE NOT_RECRUITING
Study of LOXO-305 (Pirtobrutinib) Versus Investigator's Choice (Idelalisib Plus Rituximab or Bendamustine Plus Rituximab) in Patients With Previously Treated Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
Chronic Lymphocytic LeukemiaUnlock trial analytics
Study Endpoints
Primary Endpoints
Percentage of Participants Achieving Complete Response (CR), Complete Remission with Incomplete Hematologic Recovery (Cri), Nodular Partial Remission (nPR) or Partial Response (PR): Overall Response Rate (ORR) Part 1
Baseline to best overall response the best response recorded from Cycle 1 Day 1 until data cutoff date, PD, or start of new anticancer treatment, whichever is the earliest] (approximately 3 years and 5 months)

ORR as assessed by independent review committee (IRC) per International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018 criteria

Percentage of Participants Achieving Complete Response (CR), Complete Remission with Incomplete Hematologic Recovery (CRi), Nodular Partial Remission (nPR) or Partial Response (PR): Overall Response Rate (ORR) Part 2
Baseline to best overall response the best response recorded from Cycle 1 Day 1 until data cutoff date, PD, or start of new anticancer treatment, whichever is the earliest (Approximately 2 years and 3 months)

ORR as assessed by independent review committee (IRC) per International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018 criteria

To evaluate progression-free survival (PFS) of pirtobrutinib (Arm A) compared to bendamustine and rituximab (Arm B)
Up to approximately 5 years

Assessed by blinded independent review committee (IRC) per International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018 Response Criteria

To evaluate progression-free survival (PFS) of pirtobrutinib plus venetoclax and rituximab (Arm A) compared to venetoclax and rituximab (Arm B)
Up to approximately 5 years

Assessed by blinded independent review committee (IRC) per International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018

To compare progression-free survival (PFS) of pirtobrutinib as monotherapy (Arm A) to investigator choice of covalent BTK inhibitor monotherapy (Arm B) in patients with previously treated mantle cell lymphoma (MCL)
Up to approximately 24 months

Assessed per Lugano criteria

Progression-free Survival (PFS) Assessed by Independent Review Committee (IRC)
Randomization to Disease Progression or Death Due to Any Cause (Up to 29 Months)

PFS is defined as the time from the date of randomization to the date of first documentation of progressive disease (PD) or death from any cause, as evaluated by an IRC according to International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018.

The recommended phase 2 dose (RP2D) which will be determined based on the rate of dose-limiting toxicities (DLTs) during the DLT evaluation period.
5 years

To determine the safety and tolerability of mosunetuzumab in combination with pirtobrutinib.

Best very good partial response (VGPR) or better per the modified IWWM6 criteria.1
5 years

To determine the efficacy of the combination of mosunetuzumab and pirtobrutinib.

Complete remission (CR) rate
After cycle 8 of mosunetuzumab (cycle length = 21 days)

Will report the number of CR and the estimated CR rate with 95% exact binomial confidence interval (CI). Will build logistic regression to evaluate the risk factor association with the endpoint of interest.

Progression free survival (PFS)
From trial enrollment to disease progression or death, whichever occurs first, assessed at 1 year

Analyses will follow standard methodology by employing Kaplan-Meier (KM) and Cox proportional hazard model methodology. The 1-year PFS rate and 95% CI will be estimated by KM.

Percentage of Participants with Grade 3 or Higher Treatment-emergent Adverse Events
Day 1 through 28 days after last dose or start of new anticancer therapy
Objective response rate (ORR) defined as the proportion of subjects achieving a partial response (PR) or complete response (CR) by Lugano Criteria at Cycle 7.
7 months

To assess the ORR in the study population at Cycle 7.

Overall Response Rate
Baseline up to 3 years

Overall response rate is defined as the proportion of participants who achieve the best overall response at or before the initiation of subsequent anticancer therapy of CR, CRi, nPR, or PR. ORR will be assessed using International Workshop on Chronic Lymphocytic Leukemia (iwCLL) 2018 response criteria.

Rate of complete response after initial therapy
1 year since treatment initiation

Defined by the 2018 International Workshop on Chronic Lymphocytic Leukemia (IWCLL) guidelines

Very Good Partial Response (VGPR) or Better Response Rate
up to 2 years

VGPR or better response rate is defined as proportion of participants experienced VGPR or complete response (CR) based on modified 6th International Workshop on WM \[IWWM\] criteria (NCCN 2014).

Phase 1-Number of Participants with One or More Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration
Baseline Up to Week 4

A summary of TEAEs and SAEs regardless of causality, will be reported in the Reported Adverse Events module

Phase 1-Dose Limiting Toxicity (DLT) of Pirtobrutinib
Baseline Up to Week 4

DLTs of Pirtobrutinib

Phase 1-Number of Participants with Treatment-Related Adverse Events as Assessed by Vital Signs: Blood Pressure, Pulse Rate, and Body Temperature
Baseline Up to Week 16

Blood Pressure, Pulse Rate, and Body Temperature

Phase 1-Number of Participants with Treatment-Related Adverse Events as Assessed by Clinical Lab Tests: Hematology, Clinical Chemistry, Urinalysis, Pregnancy, Hepatitis Serology and Cytomegalovirus (CMV)
Baseline Up to Week 16

Hematology, Clinical Chemistry, Urinalysis, Pregnancy, Hepatitis Serology and Cytomegalovirus (CMV)

Phase 1-Number of Participants with Treatment-Related Adverse Events as Assessed by Electrocardiograms (ECGs): ECG QT Interval
Baseline Up to Week 16

ECG QT Interval

Phase 2-Efficacy of Pirtobrutinib Versus Placebo
Baseline Up to Week 24

Stable platelet response rate is defined as the proportion of participants achieving platelet count of greater than or equal to 50 thousand per microliter (k/μL) and on at least 4 of the 6 consecutive biweekly visits between weeks 14 and 24 in the absence of rescue therapy and prohibited concomitant medication that may impact efficacy

Pharmacokinetics (PK): Maximum Concentration (Cmax) of Rosuvastatin
Day 1, Day 6 and Day 13: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours (h) post-dose.

PK: Cmax of Rosuvastatin

PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-inf]) of Rosuvastatin
Day 1, Day 6 and Day 13: Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours (h) post-dose.

PK: AUC(0-inf) of Rosuvastatin

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: AUC0-24 of Pirtobrutinib

PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: AUC0-t of Pirtobrutinib

PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: AUC0-inf of Pirtobrutinib

PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: %AUCextrap of Pirtobrutinib

PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: CL/F of Pirtobrutinib

PK: Apparent Plasma Terminal Elimination Half-life (t1/2) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: t1/2 of Pirtobrutinib

PK: Maximum Observed Plasma Concentration (Cmax) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: Cmax of Pirtobrutinib

PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: Tmax of Pirtobrutinib

PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: λZ of Pirtobrutinib

PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of Pirtobrutinib
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

PK: Vz/F of Pirtobrutinib

Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Hour 0 to the Last Measurable Concentration (AUC[0-t]) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: AUC\[0-t\] of Digoxin was reported.

PK: Area Under the Concentration During a Dosing Interval (AUC [Tau]) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: AUC \[tau\] of Digoxin was reported.

PK: Apparent Systemic Clearance (CL/F) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: CL/F of Digoxin in plasma was reported.

PK: Maximum Observed Plasma Concentration (Cmax) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: Cmax of Digoxin was reported.

PK: Time to Maximum Observed Plasma Concentration (Tmax) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: Tmax of Digoxin was reported.

PK: Mean Residence Time (MRT) of Digoxin in Plasma
Day 7 and Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: MRT of Digoxin was reported.

PK: Cumulative Amount of Drug Excreted Unchanged in Urine (Ae) of Digoxin
Day 7 and Day 16: Predose, 6, 12, 24 hours post dose

PK: Ae of Digoxin in urine was reported. The urine sampling time points from pre-dose through 24 hours post-dose were used to assess this outcome.

PK: Fraction of Digoxin Excreted Unchanged in Urine (Fe) Expressed as Percentage of Dose Excreted
Day 7 and Day 16: Predose, 6, 12, 24 hours post dose

PK: Fe of Digoxin was reported. The urine sampling time points from pre-dose through 24 hours post-dose were used to assess this outcome.

PK: Renal Clearance (CLr) of Digoxin in Plasma
Day 7: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: CLr of Digoxin in plasma was reported.

PK: Area Under the Concentration From Hour 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib in Plasma
Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: AUC\[0-t\] of Pirtobrutinib was reported.

PK: Area Under the Concentration During a Dosing Interval (AUCtau) of Pirtobrutinib in Plasma
Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: AUCtau of Pirtobrutinib was reported.

PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib in Plasma
Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: CL/F of Pirtobrutinib in plasma was reported.

PK: Maximum Observed Plasma Concentration (Cmax) of Pirtobrutinib in Plasma
Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: Cmax of Pirtobrutinib was reported.

PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib in Plasma
Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: Tmax of Pirtobrutinib was reported.

PK: Mean Residence Time (MRT) of Pirtobrutinib in Plasma
Day 8: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours postdose; Day 16: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, and 96 hours postdose

PK: MRT of Pirtobrutinib was reported.

Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: Cmax of pirtobrutinib

PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: t½ of pirtobrutinib

PK: Mean Residence Time (MRT) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

MRT is the average time a drug molecule stays in the body, calculated from the AUC0-inf.

PK: Unbound Cmax (Cmax,u) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

Cmax,u was calculated by multiplying Cmax by Fu (i.e., Cmax\*Fu). Fu represents the unbound fraction, which is the portion of the drug in the bloodstream that is unbound to plasma proteins. It is expressed as a decimal and will be calculated from protein binding concentration data as the unbound drug concentration divided by the total drug concentration in plasma. The concentrations of total and unbound drug were determined in a sample of predose plasma fortified with a known concentration of drug.

PK: Unbound AUC0-t (AUC0-t,u) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

AUC0-t,u was calculated by multiplying AUC0-t by Fu (i.e., AUC0-t\*Fu). Fu represents the unbound fraction, which is the portion of the drug in the bloodstream that is unbound to plasma proteins. It is expressed as a decimal and will be calculated from protein binding concentration data as the unbound drug concentration divided by the total drug concentration in plasma. The concentrations of total and unbound drug were determined in a sample of predose plasma fortified with a known concentration of drug.

PK: Unbound AUC0-inf (AUC0-inf,u) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

AUC0-inf,u was calculated by multiplying AUC0-inf by Fu (i.e., AUC0-inf\*Fu). Fu represents the unbound fraction, which is the portion of the drug in the bloodstream that is unbound to plasma proteins. It is expressed as a decimal and will be calculated from protein binding concentration data as the unbound drug concentration divided by the total drug concentration in plasma. The concentrations of total and unbound drug were determined in a sample of predose plasma fortified with a known concentration of drug.

PK: Unbound CL/F (CL/F,u) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

CL/F,u was calculated by multiplying CL/F by Fu (i.e., CL/F\*Fu). Fu represents the unbound fraction, which is the portion of the drug in the bloodstream that is unbound to plasma proteins. It is expressed as a decimal and will be calculated from protein binding concentration data as the unbound drug concentration divided by the total drug concentration in plasma. The concentrations of total and unbound drug were determined in a sample of predose plasma fortified with a known concentration of drug.

PK: Unbound Vz/F (Vz/F,u) of Pirtobrutinib
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

Vz/F,u was calculated by multiplying Vz/F by Fu (i.e., Vz/F\*Fu). Fu represents the unbound fraction, which is the portion of the drug in the bloodstream that is unbound to plasma proteins. It is expressed as a decimal and will be calculated from protein binding concentration data as the unbound drug concentration divided by the total drug concentration in plasma. The concentrations of total and unbound drug were determined in a sample of predose plasma fortified with a known concentration of drug.

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours post-dose on Days 1 and 8

PK: AUC0-24 of pirtobrutinib was reported.

PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib
Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8

PK: AUC0-t of pirtobrutinib was reported.

PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Pirtobrutinib
Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8

PK: AUC0-inf of pirtobrutinib was reported.

PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib
Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8

PK: Cmax of pirtobrutinib was reported.

PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8

PK: Lambda Z of pirtobrutinib was reported.

PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib
Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8

PK: Vz/F of pirtobrutinib was reported

PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Normal Hepatic Function)
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: λZ of pirtobrutinib

PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Mild Hepatic Function)
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: λZ of pirtobrutinib

PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Moderate Hepatic Function)
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: λZ of pirtobrutinib

PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Severe Hepatic Function)
Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose)

PK: λZ of pirtobrutinib

Placebo-corrected Change From Baseline in QT Interval Corrected Using Fridericia's Correction (QTcF) (ΔΔQTcF)
Baseline (Predose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8.5, 12 and 24 hours post-dose

The cardiodynamic assessment was performed through 12-lead electrocardiogram (ECG) extracted from continuous recordings at pre-specified time points. Participants rested in supine position for at least 10 minutes prior to and 5 minutes after each time point for ECG extractions. The QT interval is the time from electrocardiogram Q wave to the end of the T wave corresponding to electrical systole. QT interval was corrected for heart rate using QTcF. Placebo-corrected change from baseline in QTcF (ΔΔQTcF) was calculated based on model-predicted effect.

Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: AUC(0-t) of repaglinide was reported.

PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: AUC(0-inf) of repaglinide was reported.

PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: AUC-inf (%extrap) of repaglinide was reported.

PK: Maximum Observed Concentration (Cmax) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: Cmax of repaglinide was reported.

PK: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: Tmax of repaglinide was reported.

PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: Lambda Z of repaglinide was reported.

PK: Apparent Systemic Clearance (CL/F) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: CL/F of repaglinide was reported.

PK: Apparent Plasma Terminal Elimination Half-life (t½) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: t½ of repaglinide was reported.

PK: Apparent Volume of Distribution (Vz/F) of Repaglinide
Period 1, Day 1 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose); Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16 and 24 hours post-dose)

PK: Vz/F of repaglinide was reported.

PK: Area Under the Concentration-time Curve During a Dosing Interval (AUCtau) of Pirtobrutinib
Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 24, 42, 78 and 100 hours post-dose)

PK: AUCtau of pirtobrutinib was reported.

PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Pirtobrutinib
Period 2: 24-hour post-dose on Day 12

PK: Ctrough of pirtobrutinib was reported.

PK: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib
Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 24, 42, 78 and 100 hours post-dose)

PK: Tmax of pirtobrutinib was reported.

PK: Apparent Systemic Clearance (CL/F) at Steady State of Pirtobrutinib
Period 2, Day 12 (Pre-dose, 0.17, 0.33, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 24, 42, 78 and 100 hours post-dose)

PK: CL/F at steady state of pirtobrutinib was reported.

Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of Midazolam and Its Metabolite 1-hydroxymidazolam (1-OH-midazolam) Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: AUC0-t of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Area Under the Concentration-Time From Time 0 Extrapolated To Infinity (AUC0-inf) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: AUC(0-inf) of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: %AUCextrap of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Maximum Observed Plasma Concentration (Cmax) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: Cmax of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Time to Maximum Observed Plasma Concentration (Tmax) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: tmax of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Apparent Terminal Elimination Rate Constant (Lambda [λ] z) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: λz of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Apparent Systemic Clearance (CL/F) of Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: CL/F of midazolam following oral dose administration was reported.

PK: Apparent Volume of Distribution (Vz/F) of Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: Vz/F of midazolam following oral dose administration was reported.

PK: Apparent Plasma Terminal Elimination Half-life (t½) of Midazolam and Its Metabolite 1-OH-Midazolam Following Oral Dose Administration
Period 1: Day 3 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 17 (pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: t½ of midazolam and its metabolite 1-OH-midazolam following oral dose administration was reported.

PK: Total Clearance (CL) of Midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: CL of midazolam following intravenous dose administration was reported.

PK: Volume of Distribution (Vz) of Midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: Vz of midazolam following intravenous dose administration was reported.

PK: Volume of Distribution at Steady State (Vss) of Midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: Vss of midazolam following intravenous dose administration was reported.

PK: Area Under the Concentration-Time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: AUC0-t of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Area Under the Concentration-Time From Time 0 Extrapolated To Infinity (AUC0-inf) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: AUC0-inf of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: %AUCextrap of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Maximum Observed Plasma Concentration (Cmax) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: Cmax of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Time to Maximum Observed Plasma Concentration (Tmax) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: tmax of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Apparent Terminal Elimination Rate Constant (λz) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: λz of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

PK: Apparent Plasma Terminal Elimination Half-life (t½) of Midazolam and Its Metabolite 1-OH-midazolam Following Intravenous Dose Administration
Period 1: Day 1 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose); Period 2: Day 15 (pre-dose, 5 minutes, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 hours post-dose)

PK: t1/2 of midazolam and its metabolite 1-OH-midazolam following intravenous dose administration was reported.

Number of Participants With One or More Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Event(s) (SAEs)
Baseline up to 46 days

TEAE is defined as an adverse event (AE) which starts on or after the first administration of study drug. A serious adverse event is defined as any AE occurring at any dose that results in any of the following outcomes: death; a life-threatening adverse drug experience; inpatient hospitalization or prolongation of existing hospitalization; a persistent or significant disability/incapacity; a congenital anomaly/birth defect; an important medical event that may require medical or surgical intervention to prevent any of the above outcomes.

Maximum Tolerated Dose (MTD)
Up to 24 Months

Phase I

Recommended dose for further study
Up to 24 Months

Phase I

To assess the preliminary anti-tumor activity of pirtobrutinib based on ORR as assessed by an Independent Review Committee (IRC).
Up to 24 months

Phase II

To evaluate the safety of pirtobrutinib in combination with venetoclax (Arm A) by assessing incidence and severity of treatment-emergent adverse events as determined by CTCAE v5.0
Up to 24 Months

For Phase 1b

To evaluate the safety of pirtobrutinib in combination with venetoclax and rituximab (Arm B) by assessing incidence and severity of treatment-emergent adverse events as determined by CTCAE v5.0
Up to 24 Months

For Phase 1b

Secondary Endpoints
IRC-assessed Progression-Free Survival (PFS)
Randomization to PD (per iwCLL 2018 criteria) or death from any cause (approximately 5 years 8 months)
Investigator assessed Progression-Free Survival (PFS)
Randomization to PD (per iwCLL 2018 criteria) or death from any cause (approximately 5 years 8 months)
Event-Free Survival (EFS)
Randomization to first occurrence of treatment discontinuation due to adverse event/toxicity, treatment-emergent atrial fibrillation or atrial flutter of any grade, progressive disease (PD) or death (approximately 4 years)
Unlock Study Endpoints
Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Pirtobrutinib Part 1EXPERIMENTALParticipants will receive pirtobrutinib orally.
Ibrutinib Part 1ACTIVE_COMPARATORParticipants will receive ibrutinib orally.
Pirtobrutinib Part 2EXPERIMENTALParticipants will receive pirtobrutinib orally.
Arm A (Pirtobrutinib)EXPERIMENTALPirtobrutinib administered orally
Arm B (BR)ACTIVE_COMPARATORBendamustine plus rituximab administered intravenously (IV)
Arm A (PVR)EXPERIMENTALFixed duration pirtobrutinib in combination with venetoclax and rituximab
Arm B (VR)ACTIVE_COMPARATORVenetoclax with rituximab
Arm B (Ibrutinib, Acalabrutinib, or Zanubrutinib)ACTIVE_COMPARATORInvestigator's choice (based on local availability) of ibrutinib, acalabrutinib or zanubrutinib orally. Options are limited to those that are available/approved in the specific country.
Arm A - PirtobrutinibEXPERIMENTALParticipants received 200 milligrams (mg) of pirtobrutinib administered orally once daily (QD) on Days 1 through 28 of a 28-day cycle. The treatment was continued until progressive disease, a discontinuation criterion, or unacceptable toxicity.
Arm B - Idelalisib plus Rituximab or Bendamustine plus RituximabACTIVE_COMPARATORParticipants received either 150 mg of idelalisib administered twice-daily (BID) orally on Days 1 through 28 of a 28-day cycle in combination with 375 milligram per square meter (mg/m\^2) of rituximab by intravenous (IV) infusion on day 1 of cycle 1, then 4 IV infusions of rituximab 500 mg/m\^2 every 2 weeks (Q2W) and 3 IV infusions of rituximab 500 mg/m\^2 every 4 weeks (Q4W) or 70 mg/m\^2 of bendamustine administered IV on day 1 and 2 of each 28-day cycle from cycles 1 to 6 in combination with 375 mg/m\^2 of rituximab IV on day 1 of cycle 1, then 500 mg/m\^2 of rituximab on day 1 of each 28-day cycle from cycles 2 to 6.
Dosing Strategy 1-Mosunetuzumab and PirtobrutinibEXPERIMENTALParticipants receive pirtobrutinib daily on days 1-21 of 21 day cycles. Mosunetuzumab will be administered subcutaneously starting on cycle 2, day 1. If patients have a complete response to treatment, after 9 cycles, they will continue with on pirtobrutinib for a total of 18 cycles. If patients receive a very good partial or minor response, they will continue to receive Mosunetuzumab and Pirtobrutinib for a total of 18 cycles.
Dosing Strategy 2- Mosunetuzumab and PirtobrutinibEXPERIMENTALParticipants receive pirtobrutinib daily on days 1-21 of 21 day cycles. Mosunetuzumab will be administered subcutaneously starting on cycle 3, day 1. If patients have a complete response to treatment, after 9 cycles, they will continue with on pirtobrutinib for a total of 19 cycles. If patients receive a very good partial or minor response, they will continue to receive Mosunetuzumab and Pirtobrutinib for a total of 19 cycles.
Treatment (pirtobrutinib, mosunetuzumab)EXPERIMENTALPatients receive pirtobrutinib PO QD on 7 days prior to the start of mosunetuzumab (day -7) and continue it until up to 52 weeks. Patients receive mosunetuzumab subcutaneously (SC) or intravenously (IV) on days 1, 8, and 15 of cycle 1 then on day 1 of remaining cycles. Cycles of mosunetuzumab repeat every 21 days for up to 17 cycles in the absence of disease progression or unacceptable toxicity. Patients with a CR after cycle 8 discontinue mosunetuzumab. Patients also undergo blood sample and oral swab and/or rectal swab collection, tissue biopsy, CT, and PET/CT throughout the study. Additionally, patients may undergo bone marrow aspiration and biopsy at screening and after cycle 8.
PirtobrutinibEXPERIMENTALPirtobrutinib administered orally.
Rituximab+Pirtobrutinib, Pirtobrutinib AloneEXPERIMENTALThis arm included participants who had a complete response to Rituximab and Pirtobrutinib in Stage 1. In Stage 1, all participants will receive Rituximab and Pirtobrutinib for 6 Cycles (42 days). In Stage 2, subjects who experience a complete response will discontinue rituximab and continue treatment with pirtobrutinib only for 6 additional cycles. Participants in this arm will not have Stage 3 treatment. After completing Stage II treatment, subjects will discontinue treatment and proceed to End of Treatment (EOT) and Long-Term Follow-Up (LTFU) visits.
Rituximab+Pirtobrutinib, Continuded Rituximab+Pirtobrutinib, Pirtobrutinib Alone (6 Cycles)EXPERIMENTALThis arm included participants who had a Partial Response or Stable Disease response to Rituximab and Pirtobrutinib in Stage 1 and a Complete Response to continued Rituximab and Pirtobrutinib in Stage 2. In Stage 1, all participants will receive Rituximab and Pirtobrutinib for 6 Cycles (42 days). In Stage II, subjects who experienced a Partial Response or Stable Disease will continue Rituximab and Pirtobrutinib treatment for 6 additional cycles. In Stage III, subjects who experienced a Complete Response will discontinue rituximab and continue treatment with Pirtobrutinib only for 6 additional cycles. After completing Stage III treatment, subjects will discontinue treatment and proceed to End of Treatment (EOT) and Long-Term Follow-Up (LTFU) visits.
Rituximab+Pirtobrutinib, Continuded Rituximab+Pirtobrutinib, Pirtobrutinib Alone (24 Cycles)EXPERIMENTALThis arm included participants who had a Partial Response or Stable Disease response to Rituximab and Pirtobrutinib in Stage 1 and a Progressive Disease after continued Rituximab and Pirtobrutinib in Stage 2. In Stage I, all participants will receive Rituximab and Pirtobrutinib for 6 Cycles (42 days). In Stage II, subjects who experience a Partial Response or Stable Disease will continue Rituximab and Pirtobrutinib treatment for 6 additional cycles. In Stage III, subjects who experience Progressive Disease will discontinue treatment and proceed to End of Treatment (EOT) and Long-Term Follow-Up (LTFU) visits.
Rituximab+Pirtobrutinib, Continuded Rituximab+PirtobrutinibEXPERIMENTALThis arm included participants who had a Partial Response or Stable Disease response to Rituximab and Pirtobrutinib in Stage 1 and a Partial Response or Stable Disease to continued Rituximab and Pirtobrutinib in Stage 2. In Stage I, all participants will receive Rituximab and Pirtobrutinib for 6 Cycles (42 days). In Stage II, subjects who experience a Partial Response or Stable Disease will continue Rituximab and Pirtobrutinib treatment for 6 additional cycles. In Stage III, subjects who experience a Partial Response or Stable Disease will discontinue rituximab and continue treatment with Pirtobrutinib only until progression or other treatment discontinuation criteria are met. After progression or other treatment discontinuation criteria are met, subjects will discontinue treatment and proceed to End of Treatment (EOT) and Long-Term Follow-Up (LTFU) visits.
Rituximab+Pirtobrutinib OnlyEXPERIMENTALThis arm included participants who had Progressive Disease after Rituximab and Pirtobrutinib treatment in Stage 1. In Stage 1, all participants will receive Rituximab and Pirtobrutinib for 6 Cycles (42 days). If participants had Progressive Disease after Stage I, they will not have Stage II or Stage III of treatment. After completing Stage I treatment, subjects will discontinue treatment and proceed to End of Treatment (EOT) and Long-Term Follow-Up (LTFU) visits.
Pirtobrutinib Standard Dose (Dose 1)-Part 1ACTIVE_COMPARATORPirtobrutinib administered orally.
Pirtobrutinib Dose 2-Part 1EXPERIMENTALPirtobrutinib administered orally.
Pirtobrutinib Dose 3-Part 1EXPERIMENTALPirtobrutinib administered orally.
Pirtobrutinib Standard Dose-Part 2EXPERIMENTALPirtobrutinib administered orally.
Pirtobrutinib-ObinutuzumabEXPERIMENTALEligible participants will receive initial treatment with pirtobrutinib and obinutuzumab for 12 cycles. Participants with progressive chronic lymphocytuc leukemia or small lymphocytic lymphoma during the off-treatment follow-up will receive continuous pirtobrutinib monotherapy.
PIRTOBRUTINIB + VENETOCLAXEXPERIMENTALParticipants will receive: * Standard of care bone marrow aspirate \& biopsy within 90 days of Cycle 1 Day 1. * Computed Tomography (CT) scan of chest, pelvis \& abdomen within 90 days of Cycle 1 Day 1. * Electrocardiogram at screening. * Cycle 1 * Electrocardiogram. * Day 1-28: Predetermined dose of Pirtobrutinib 1x daily. * Cycle 2 -Day 1-28: Predetermined dose Pirtobrutinib \& Venetoclax 1x daily. Tumor lysis syndrome (TLS) prophylaxis, predetermined dose Allopurinol at least 72 hrs prior to 1st administration of Venetoclax and dose escalation at Day 8 \& Day 15. * Cycles 3-24 * Day 1-28: Predetermined dose of Pirtobrutinib \& Venetoclax 1x daily. * Electrocardiogram: Cycles 3, 6, 9,12,15,18,21,24 * CT scan of chest, pelvis \& abdomen: Cycles 7, 13, End of Treatment if extramedullary disease at baseline unresolved in previous CT scan * Standard of care bone marrow aspirate and biopsy: Cycles 7, 13, End of Treatment * Follow up every 12 wks for 4 yrs.
Pirtobrutinib Phase 1EXPERIMENTALPirtobrutinib administered orally
Pirtobrutinib Phase 2EXPERIMENTALPirtobrutinib administered orally
Placebo Phase 2PLACEBO_COMPARATORPlacebo administered orally
Rosuvastatin + PirtobrutinibEXPERIMENTALParticipants received study intervention through oral administration as follows: * Day 1: 20 milligram (mg) rosuvastatin alone * Day 6: 20 mg rosuvastatin co-administered with 200 mg pirtobrutinib * Days 7 to 12: Once daily (QD) doses of 200 mg pirtobrutinib alone * Day 13: 20 mg rosuvastatin co-administered with 200 mg pirtobrutinib * Days 14 to 17: QD doses of 200 mg pirtobrutinib alone.
200 mg Pirtobrutinib (Sequence R/T)EXPERIMENTALPeriod 1: Participants received a reference formulation (R) of oral pirtobrutinib 200 milligrams (mg) on day 1. Period 2: Participants received a test formulation (T) of oral pirtobrutinib 200 mg on day 8. There was a washout period of 7 days between the doses of pirtobrutinib.
200 mg Pirtobrutinib (Sequence T/R)EXPERIMENTALPeriod 1: Participants received a test formulation (T) of oral pirtobrutinib 200 mg on day 1. Period 2: Participants received a reference formulation (R) of oral pirtobrutinib 200 mg on day 8. There was a washout period of 7 days between the doses of pirtobrutinib.
Digoxin + PirtobrutinibEXPERIMENTALParticipants received oral dose of * 0.25 mg digoxin twice daily (BID) on Day 1 * 0.25 mg digoxin once daily (QD) from Day 2 to Day 7 * 200 mg Pirtobrutinib in combination with 0.25 mg digoxin QD starting from Day 8 to Day 16
Pirtobrutinib (Normal Renal Function)EXPERIMENTALParticipants with normal renal function (eGFR \>= 90 mL/min/1.73 m2) received a single dose of Pirtobrutinib 200 milligrams (mg) administered orally on Day 1.
Pirtobrutinib (Severe Renal Impairment)EXPERIMENTALParticipants with severe renal impairment (eGFR: \< 30 mL/min/1.73 m2) received a single dose of Pirtobrutinib 200 mg administered orally on Day 1.
200 mg Pirtobrutinib: Treatment ABEXPERIMENTALParticipants received a single oral dose of 200 milligrams (mg) of pirtobrutinib administered in the morning on Day 1, under fasted conditions (Treatment A) followed by 200 mg pirtobrutinib administered orally in the morning on Day 8, under fed condition (Treatment B). A washout period of 7 days was maintained between Treatments A and B.
200 mg Pirtobrutinib: Treatment BAEXPERIMENTALParticipants received a single oral dose of 200 mg pirtobrutinib administered in the morning on Day 1, under fed conditions (Treatment B) followed by 200 mg of pirtobrutinib administered orally in the morning on Day 8, under fasted conditions (Treatment A). A washout period of 7 days was maintained between Treatments A and B.
Pirtobrutinib (Normal Hepatic Function)EXPERIMENTALParticipants received a single dose of Pirtobrutinib 200 milligrams (mg) administered orally on Day 1.
Pirtobrutinib (Mild Hepatic Impairment)EXPERIMENTALParticipants received a single dose of Pirtobrutinib 200 mg administered orally on Day 1.
Pirtobrutinib (Moderate Hepatic Impairment)EXPERIMENTALParticipants received a single dose of Pirtobrutinib 200 mg administered orally on Day 1.
Pirtobrutinib (Severe Hepatic Impairment)EXPERIMENTALParticipants received a single dose of Pirtobrutinib 200 mg administered orally on Day 1.
PlaceboPLACEBO_COMPARATORPlacebo (matched to Pirtobrutinib) a single oral dose on Day 1, 12 and 23 following a fast of at least 8 hours prior to and 6 hours after dosing.
MoxifloxacinACTIVE_COMPARATORMoxifloxacin a single oral dose on Day 1, 12 and 23 following a fast of at least 8 hours prior to and 6 hours after dosing.
Period 1: 0.5 mg RepaglinideEXPERIMENTALParticipants received a single oral dose of 0.5 milligrams (mg) repaglinide tablet, in the morning on Day 1.
Period 2: 200 mg Pirtobrutinib QDEXPERIMENTALParticipants received oral doses of 200 mg pirtobrutinib tablets, once daily (QD) in the morning from Day 2 to Day 11.
Period 2: 200 mg Pirtobrutinib QD + 0.5 mg RepaglinideEXPERIMENTALParticipants received oral doses of 200 mg pirtobrutinib QD and 0.5 mg repaglinide tablets, in the morning on Day 12.
Midazolam (Intravenous [IV] Bolus)EXPERIMENTALA single IV bolus dose of midazolam will be administered in the morning following a 10-hour fast prior to dosing and a 4-hour fast postdose on Day 1 and Day 15.
Midazolam OralEXPERIMENTALA single oral dose of midazolam will be administered in the morning following a 10-hour fast prior to dosing and a 4-hour fast postdose on Day 3 and Day 17.
Cohort 1: 300 mg PirtobrutinibEXPERIMENTALParticipants received a single dose of Pirtobrutinib 300 milligram (mg) administered orally on Day 1.
Cohort 2: 600 mg PirtobrutinibEXPERIMENTALParticipants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
Cohort 3: 800 mg PirtobrutinibEXPERIMENTALParticipants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
Cohort 4: 900 mg PirtobrutinibEXPERIMENTALParticipants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
Phase I Dose Escalation (Pirtobrutinib Monotherapy)EXPERIMENTALDose Escalation and determination of MTD; multiple dose levels of pirtobrutinib to be evaluated
Phase 2 (Pirtobrutinib Monotherapy) Cohort 3EXPERIMENTALCLL/SLL patients with no prior therapy.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 1EXPERIMENTALNon-blastoid MCL patients treated with a prior BTK-inhibitor containing regimen.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 4EXPERIMENTALCLL/SLL patients treated with prior therapy, BTK inhibitor naïve.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 2EXPERIMENTALCLL/SLL patients treated with 2 or more prior regimens, including a BTK inhibitor-containing regimen.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 5EXPERIMENTALWM patients treated with a prior BTK inhibitor-containing regimen.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 6EXPERIMENTALMZL patients treated with a prior BTK inhibitor-containing regimen.
Phase 2 (Pirtobrutinib Monotherapy) Cohort 7EXPERIMENTALDefined as CLL/SLL or NHL not otherwise specified in Cohorts 1 through 6, inclusive of CLL/SLL, Richter's transformation, or low grade NHL with transformation, blastoid MCL, and patients with history of CNS involvement or primary CNS lymphoma. In the event the Sponsor electively closes Cohorts 2-4 prior to completion, patients with CLL/SLL who are ineligible to participate in or unable to access late phase studies of pirtobrutinib may be eligible to enroll in this cohort Diffuse large B-cell lymphoma (DLBCL) is excluded. MCL without prior BTK inhibitor treatment is excluded. Patients enrolling to Cohort 7 must have received one or more prior therapies or have no available approved therapy with demonstrated clinical benefit with the exception of untreated Richter's transformation, which is allowed.
Phase 1b Dose Expansion (Pirtobrutinib Combination Therapy) Arm AEXPERIMENTALRelapsed/Refractory CLL will receive the recommended Phase 2 dose of pirtobrutinib in combination with venetoclax
Phase 1b Dose Expansion (Pirtobrutinib Combination Therapy) Arm BEXPERIMENTALRelapsed/Refractory CLL will receive the recommended Phase 2 dose of pirtobrutinib in combination with venetoclax and rituximab
Phase 1 Dose Expansion (Pirtobrutinib Monotherapy)EXPERIMENTALPatients to receive the recommended Phase 2 dose of pirtobrutinib
Interventions
NameTypeDescription
PirtobrutinibDRUGAdministered orally.
IbrutinibDRUGAdministered orally.
BendamustineDRUGIV
RituximabDRUGIV
VenetoclaxDRUGOral
AcalabrutinibDRUGOral
ZanubrutinibDRUGOral
IdelalisibDRUGOral
MosunetuzumabDRUGAdministered subcutaneously on day one of applicable cycles.
Biospecimen CollectionPROCEDUREUndergo blood sample and oral swab and/or rectal swab collection
Biopsy ProcedurePROCEDUREUndergo tissue biopsy
Computed TomographyPROCEDUREUndergo CT and PET/CT
Positron Emission TomographyPROCEDUREUndergo PET/CT
Bone Marrow AspirationPROCEDUREUndergo bone marrow aspiration and biopsy
Bone Marrow BiopsyPROCEDUREUndergo bone marrow aspiration and biopsy
Questionnaire AdministrationOTHERAncillary studies
ObinutuzumabDRUGObinutuzumab is given intravenously from Cycle 7 to Cycle 12, for total 6 cycles during initial treatment only. Initial treatment: \- Obinutuzumab intravenous (IV) following the standard schedule from Cycle 6 through Cycle 12 (total 6 cycles: 100 mg on Cycle 6 Day 1, 900 mg on Cycle 6 Day 2, 1000 mg on Cycle 6 Day 8 and Cycle 6 Day 15, 1000 mg on Day 1 of Cycle 7 through Cycle 12).
PlaceboDRUGAdministered orally
RosuvastatinDRUGAdministered Orally.
DigoxinDRUGAdministered Orally.
MoxifloxacinDRUGAdministered orally
RepaglinideDRUGAdministered orally.
Midazolam SyrupDRUGAdministered Orally.
Midazolam SolutionDRUGAdministered IV bolus.
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Eligibility Criteria
Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites143

Inclusion Criteria: * Confirmed diagnosis of CLL/SLL requiring therapy per iwCLL 2018 criteria * Part 1 - Known 17p deletion status (wildtype or deleted). Part 2 - Must have deletion of 17p as determined by FISH testing * Eastern Cooperative Oncology Group (ECOG) Performance Status 0-2 * Adequate o...

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LOWJul 17, 2026NCT05254743lastUpdatePostDate: changed
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MEDIUMJun 25, 2026NCT06721013Enrollment: 58 → 68
MEDIUMJun 25, 2026NCT06721013Enrollment: 58 → 68
MEDIUMJun 25, 2026NCT06721013Enrollment: 58 → 68
LOWJun 18, 2026NCT05254743lastUpdatePostDate: changed
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MEDIUMJun 9, 2026NCT05254743Enrollment: 662 → 737
MEDIUMJun 9, 2026NCT05254743Enrollment: 662 → 737
MEDIUMJun 9, 2026NCT05254743Enrollment: 662 → 737
MEDIUMJun 9, 2026NCT05254743Enrollment: 662 → 737
MEDIUMJun 4, 2026NCT06948786lastUpdatePostDate: changed
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MEDIUMMay 29, 2026NCT05734495Status: RECRUITING → ACTIVE_NOT_RECRUITING
MEDIUMMay 29, 2026NCT05734495Status: RECRUITING → ACTIVE_NOT_RECRUITING
MEDIUMMay 29, 2026NCT05734495Status: RECRUITING → ACTIVE_NOT_RECRUITING