Your Health, We Care
Release date: 2026-03-25 15:58:48 Recommended: 7
Pirtobrutinib is a BTK inhibitor developed by Eli Lilly and Company in the United States. It was first approved by the U.S. Food and Drug Administration (FDA) on January 27, 2023.
Pirtobrutinib is indicated for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (MCL) who have received at least two prior lines of systemic therapy, including a BTK inhibitor.
Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
Pirtobrutinib is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) who have received at least two prior lines of therapy, including a BTK inhibitor and a BCL-2 inhibitor (e.g., venetoclax).
(1). Mantle Cell Lymphoma
Administer 200 mg of pirtobrutinib orally once daily until disease progression or unacceptable toxicity.
(2). Chronic Lymphocytic Leukemia and Small Lymphocytic Lymphoma
Administer 200 mg of pirtobrutinib orally once daily until disease progression or unacceptable toxicity.
(1). Interrupt pirtobrutinib treatment for Grade 3 or higher non-hematologic toxicity.
(2). Modify dose for ANC <1000 to 500 cells/mm³ with fever and/or infection, or ANC <500 cells/mm³ persisting for ≥7 days.
(3). Modify dose of pirtobrutinib for platelet count <50,000 to 25,000 cells/mm³ with bleeding, or platelet count <25,000 cells/mm³.
(4). Assess potential risks and benefits before resuming treatment at the same dose after resolution of Grade 4 non-hematologic toxicity.
(5). Dose modification of pirtobrutinib is not recommended for asymptomatic lymphocytosis.
(6). Dose modification may not be required for asymptomatic elevation of lipase.
Following adverse reactions, modify the dose of pirtobrutinib as follows:
First dose modification: 200 mg once daily, restart
Second dose modification: 100 mg once daily, restart
Third dose modification: 50 mg once daily, restart
Fourth dose modification: Discontinue pirtobrutinib.
a. Avoid concomitant use; if unavoidable, reduce the daily dose by 50 mg (interrupt treatment if current dose is 50 mg).
b. Resume the original dose after discontinuing the strong CYP3A inhibitor for 5 half-lives.
Avoid concomitant use; if unavoidable:
a. Increase dose to 300 mg once daily when current dose is 200 mg once daily.
b. Increase by 50 mg when current dose is 50 mg or 100 mg once daily.
c. Concomitant use with strong CYP3A inducers should be avoided entirely.
Due to space limitations, please refer to the official prescribing information for complete details. Specific medication should be administered under the guidance of a physician.
Adverse Reactions (Reported in ≥20% of patients)
Fatigue, musculoskeletal pain, diarrhea, COVID-19, bruising, cough.
Grade 3 or 4 Laboratory Abnormalities (Reported in ≥10% of patients)
Neutropenia, lymphopenia, thrombocytopenia, anemia.
Due to space limitations, please refer to the official prescribing information for complete details. Specific medication should be administered under the guidance of a physician.
Serious and sometimes fatal infections, including bacterial, fungal, or viral infections, as well as opportunistic infections, have been observed. Consider prophylaxis for patients at increased risk for opportunistic infections, including vaccinations and antimicrobial prophylaxis. Monitor for signs and symptoms of infection during treatment and treat promptly if infection occurs. If infection occurs, based on severity, reduce the dose of pirtobrutinib, temporarily interrupt, or permanently discontinue pirtobrutinib.
Serious hemorrhagic events, including fatal cases, have been observed. Concomitant use of pirtobrutinib and antithrombotic agents may increase the risk of hemorrhagic events. Consider the risks and benefits and monitor patients for signs of bleeding during concomitant use. If bleeding occurs, based on severity, reduce the dose of pirtobrutinib, temporarily interrupt, or permanently discontinue pirtobrutinib. Consider the potential benefits and risks of interrupting pirtobrutinib therapy for 3-7 days before and after surgery.
Cytopenias, including neutropenia, thrombocytopenia, and anemia. Serious (Grade 3 or 4) cytopenias have been observed. Monitor complete blood counts regularly. If myelosuppression occurs, interrupt treatment, reduce the dose, or discontinue treatment as appropriate.
Cardiac arrhythmias (e.g., atrial fibrillation, atrial flutter, supraventricular tachycardia, cardiac arrest) have been observed. Patients with cardiac risk factors, including hypertension or prior arrhythmias, may be at increased risk. Monitor for symptoms of arrhythmias and manage appropriately. If arrhythmia occurs, interrupt treatment, reduce the dose, or discontinue pirtobrutinib therapy as appropriate.
Second primary malignancies, including skin cancer and other solid tumors, were reported in 9% of patients treated with pirtobrutinib in clinical trials. Non-melanoma skin cancer was the most frequently reported second primary malignancy, occurring in 4.6% of patients treated with pirtobrutinib. Monitor patients for the development of second primary malignancies and advise patients to avoid sun exposure.
Hepatotoxicity has occurred. Assess bilirubin and transaminases at baseline and during treatment. If liver function abnormalities occur, monitor patients for clinical signs and symptoms of hepatotoxicity and monitor liver function tests more frequently. If drug-induced liver injury is suspected, interrupt pirtobrutinib and discontinue upon confirmation.
May cause fetal harm. Embryo-fetal toxicity observed in animals. If used during pregnancy, advise of the potential hazard to the fetus. Advise females of reproductive potential to use effective contraception during treatment and for 1 week after the last dose.
