In clinical trials, pirobrutinib (Jaypirca™) was effective in restoring BTK inhibition in patients that experienced progression after previously receiving a covalent BTK inhibitor. Pirobrutinib became the first-available noncovalent (reversible) BTK inhibitor in January 2023 when the U.S. Food and Drug Administration granted it accelerated approval.
Targeted therapy; tyrosine kinase inhibitor
Mechanism of Action
Pirobrutinib is a small molecule inhibitor of BTK kinase activity. It prevents BTK signaling to activate pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion.
Treatment of adult patients with relapsed or refractory mantle cell lymphoma after at least two lines of systemic therapy, including a BTK inhibitor
200 mg orally once daily
Swallow whole with water once a day at the same time each day; do not cut, crush, or chew the tablets. If you miss or vomit a dose within 12 hours of your regularly scheduled time, take another dose. If more than 12 hours have passed, skip the dose and resume your normal dosage time the next day.
The most common adverse reactions are fatigue, pain, diarrhea, edema, dyspnea, pneumonia, and bruising. The most significant adverse reactions are cytopenias leading to hemorrhage or infection; dysrhythmias, including atrial fibrillation and atrial flutter; and secondary malignancies.
Complete an oral adherence assessment and assess patients’ ability to safely take the drug. While patients are on treatment, monitor their:
- Lab values, including hematology (hemoglobin, platelets, neutrophils, lymphocytes) and chemistry (creatinine, calcium, AST, potassium, sodium, lipase, alkaline phosphatase, ALT) panels
- Cardiac activity
- Respiratory status
- Signs and symptoms of infection
Because of the risk for fetal toxicity, assess pregnancy status in patients of reproductive potential.
Teach patients about the common side effects and the signs and symptoms of infection, hemorrhage, and dysrhythmias. Educate about proper administration. Advise patients about the risk for fetal toxicity and instruct them to use effective contraception during treatment and for one week after the last dose. Advise patients not to breastfeed during treatment and for one week following the last dose.
The drug’s safety and effectiveness have not been established in pediatric patients. Severe renal impairment can increase pirobrutinib exposure; decrease the dosage accordingly.
Store at room temperature and keep out of reach of children. Because it can cause fetal toxicity, use hazardous drug precautions.
Visit Lilly Oncology Support or call 866-472-8663.