Administration of Pirtobrutinib
Recommended Dose of Pirtobrutinib
Dose Modifications
Dose Modifications for Adverse Reactions
Dose Modifications for Patients With Severe Renal Impairment
Dosage Modifications for Concomitant Use with Strong CYP3A Inhibitors
Dosage Modifications for Concomitant Use with CYP3A Inducers
Dose Rationale for Pirtobrutinib
Effect of Food on Pirtobrutinib
References
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Jaypirca ® (pirtobrutinib) tablets
50 mg,100 mg
This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.
How is Jaypirca® (pirtobrutinib) administered and dosed?
The recommended dosage of Jaypirca (pirtobrutinib) is 200 mg orally once daily until disease progression or unacceptable toxicity. The tablets should be swallowed whole with water and can be taken with or without food.
Content Overview
Administration of Pirtobrutinib
Pirtobrutinib tablets should be swallowed whole with water. The tablets should not be crushed, cut, or chewed before swallowing.1
Pirtobrutinib tablets should be taken at the same time each day and can be taken with or without food (Effect of Food on Pirtobrutinib).1
Eli Lilly and Company does not have information to support alternative administration of pirtobrutinib tablets.2
Recommended Dose of Pirtobrutinib
The recommended dosage of pirtobrutinib is 200 mg orally once daily until disease progression or unacceptable toxicity.1
Dose Modifications
Dose Modifications for Adverse Reactions
Dose Modifications Due to Adverse Events describes the recommended dose modifications for adverse reactions to pirtobrutinib.
Dose Modifications for Patients With Severe Renal Impairment
Use in Patients With Renal Impairment describes the recommended dose modifications of pirtobrutinib for patients with renal impairment.
Dosage Modifications for Concomitant Use with Strong CYP3A Inhibitors
Avoid concomitant use of strong CYP3A inhibitors with pirtobrutinib. If concomitant use of a strong CYP3A inhibitor is unavoidable, reduce the pirtobrutinib dose by 50 mg. If the current dosage is 50 mg once daily, interrupt pirtobrutinib treatment for the duration of strong CYP3A inhibitor use. After discontinuation of a strong CYP3A inhibitor for 5 half-lives, resume the pirtobrutinib dose that was taken prior to initiating the strong CYP3A inhibitor.1
Dosage Modifications for Concomitant Use with CYP3A Inducers
Avoid concomitant use of strong or moderate CYP3A inducers with pirtobrutinib. If concomitant use with moderate CYP3A inducers is unavoidable and the current dosage of pirtobrutinib is 200 mg once daily, increase the dose to 300 mg. If the current dosage is 50 mg or 100 mg once daily, increase the dose by 50 mg.1
Dose Rationale for Pirtobrutinib
BRUIN is a global, multicenter phase 1/2 trial evaluating pirtobrutinib (LOXO-305) in patients with previously treated chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), or non-Hodgkin's lymphoma (NHL) who have failed or are intolerant to standard of care (NCT03740529).3,4
All Patient Treated With Pirtobrutinib According to Starting Dosage summarizes the starting dosages in the phase 1/2 BRUIN study.
Pirtobrutinib Starting Dosage (all once daily) |
Number of Patients Dosed |
25 mg |
5 |
50 mg |
6 |
100 mg |
9 |
150 mg |
20 |
200 mg |
569 |
250 mg |
25 |
300 mg |
20 |
Plasma Exposure of Pirtobrutinib Across Dosages displays the plasma concentrations of pirtobrutinib after various dosages. Plasma exposures exceeded minimal inhibitory concentration of 90% (IC90) of Bruton's tyrosine kinase (BTK) throughout the dosing interval at doses ≥100mg daily.5
Figure 1 description: Graph illustrating pirtobrutinib versus time on day 8 shows plasma exposures exceeded minimal inhibitory concentration of 90% (IC90) for BTK throughout the dosing interval at doses ≥100mg daily (left). Graph illustrating estimated AUC versus dose shows plasma exposures were dose-dependent and linear (right).
Abbreviations: AUC = area under the curve; BTK = Bruton's tyrosine kinase inhibitor; IC90 = minimal inhibitory concentration of 90%; LOXO-305 = pirtobrutinib; QD = daily; WT = wild type.
After evaluation of the totality of efficacy, clinical pharmacokinetics (PK), and safety data, the study authors decided that further dose escalation was not medically justified. Therefore, no maximum tolerated dose (MTD) was established for pirtobrutinib. The study identified the recommended phase 2 dose as 200 mg daily.2
Effect of Food on Pirtobrutinib
An assessment of food effects in healthy subjects showed that
- a standard meal defined as approximately 50% carbohydrates, 30% fat, and 20% protein, decreased the maximum plasma concentration (Cmax) of pirtobrutinib by 20% and delayed time of maximal plasma concentration (Tmax) by 0.5 hours, and
- a high-fat meal defined as approximately 800 to 1000 calories (with 150 calories from protein, 250 calories from carbohydrate, and 500 to 600 calories from fat) decreased the Cmax of pirtobrutinib by 23% and delayed Tmax by 1 hour.1,2
The analysis showed no effect on pirtobrutinib AUC from time 0 to infinity (AUC0-inf). Administration with meals was not considered to be associated with a clinically relevant effect on pirtobrutinib exposure.1,2
Phase 2 Dose Optimization Study
A phase 2, dose optimization study is currently ongoing. The study is a randomized and open-label trial evaluating the efficacy and safety of pirtobrutinib in patients with CLL and SLL. It includes two parts:
- Part 1 focuses on dose optimization in patients with 1-3 prior lines of treatment, including covalent BTK inhibitors (cBTKi), and
- Part 2 evaluates treatment-naïve patients with del(17p).6 7
The study involves 28-day cycles of pirtobrutinib until discontinuation criteria are met.6
Patients in Part 1 of the study will be randomized to receive either pirtobrutinib 200mg once daily or one of two other pirtobrutinib dose levels. Patients in Part 2 of the study will receive pirtobrutinib 200mg once daily.6
The primary endpoint for Part 1 is investigator-assessed overall response rate (ORR). The primary endpoint for Part 2 is ORR assessed by independent review committee.6
Enclosed Prescribing Information
References
1Jaypirca [package insert]. Indianapolis, IN: Eli Lilly and Company; 2025.
2Data on file, Eli Lilly and Company and/or one of its subsidiaries.
3A study of oral LOXO-305 in patients with previously treated CLL/SLL or NHL. ClinicalTrials.gov identifier: NCT03740529. Updated September 25, 2025. Accessed November 19, 2025. https://www.clinicaltrials.gov/ct2/show/NCT03740529
4Mato AR, Shah NN, Jurczak W, et al. Pirtobrutinib in relapsed or refractory B-cell malignancies (BRUIN): a phase 1/2 study. Lancet. 2021;397(10277):892-901. https://doi.org/10.1016/S0140-6736(21)00224-5
5Mato AR, Pagel JM, Coombs CC, et al. LOXO-305, a next generation, highly selective, non-covalent BTK inhibitor in previously treated CLL/SLL: results from the phase 1/2 BRUIN Study. Poster presented at: 62nd Annual Meeting of the American Society of Hematology (ASH Virtual); December 5-8, 2020. Accessed January 24, 2022.
6Danilov A, Alencar A, Gao J, et al. The efficacy and safety of pirtobrutinib in patients with CLL/SLL: a phase 2 dose optimization trial in progress. Poster presented at: 21st International Workshop on Chronic Lymphocytic Leukemia; September 12-15, 2025; Krakow, Poland. Accessed December 8, 2025.
7A study evaluating the efficacy and safety of pirtobrutinib in participants with relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma. Clinicaltrials.gov identifier: NCT06588478. Updated November 20, 2025. Accessed December 2, 2025. https://clinicaltrials.gov/ct2/show/NCT06588478
Date of Last Review: October 15, 2025
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