Jaypirca

Mantle cell lymphoma (MCL) — relapsed or refractory after at least two lines of systemic therapy, including a BTK inhibitor; Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) — in adults who have received at least two prior lines of therapy, including a BTK inhibitor and a BCL-2 inhibitor

200 mg orally once daily until disease progression or unacceptable toxicity
Take with or without food
Swallow whole; do not break, crush, or chew
Dose reductions: 150 mg, then 100 mg, then 50 mg
Strong CYP3A inhibitors: Reduce to 100 mg once daily

Tablets: 50 mg, 100 mg, 200 mg

None listed.

• Hemorrhage: Serious hemorrhagic events in 3.5% (including fatal events in 0.4%). Withhold for Grade 3+ hemorrhage. Consider risk-benefit with anticoagulants/antiplatelets.
• Infections: Serious infections in 16% (including fatal 3.5%). Including COVID-19 pneumonia, pneumonia, sepsis. Consider prophylaxis for opportunistic infections.
• Cytopenias: Grade 3-4 neutropenia (22%), anemia (9%), thrombocytopenia (8%). Monitor CBC monthly.
• Atrial Fibrillation/Flutter: In 3.5%. Monitor.
• Second Primary Malignancies: In 10%, including non-melanoma skin cancers.

Fatigue (36%), musculoskeletal pain (27%), diarrhea (22%), edema (22%), neutropenia (22%), dyspnea (15%), pneumonia (15%), bruising (14%), rash (13%), hemorrhage (12%), abdominal pain (11%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Pirtobrutinib is a highly selective, non-covalent (reversible) inhibitor of Bruton's tyrosine kinase (BTK). Unlike covalent BTK inhibitors (ibrutinib, acalabrutinib, zanubrutinib) that bind irreversibly to C481, pirtobrutinib inhibits both wild-type BTK and C481S-mutant BTK through reversible binding. This allows it to maintain activity against tumors harboring the C481S resistance mutation that emerges during covalent BTK inhibitor therapy. It inhibits BTK autophosphorylation and downstream BCR signaling.

Tmax: 1-2 hours. Half-life: approximately 19 hours. Protein binding: 96%. Metabolized by CYP3A4. Steady-state by Day 8 with once-daily dosing. Excreted in feces (57%) and urine (23%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• BRUIN — Pirtobrutinib in relapsed/refractory B-cell malignancies including CLL after prior BTK inhibitor. Phase I/II.
  🔬 NCT03740529 ↗ 📄 Primary Publication ↗

Jaypirca has FDA-approved indications across the following cancer types covered on PipelineEvidence: