JAYPIRCA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for JAYPIRCA (JAYPIRCA).
JAYPIRCA (pirtobrutinib) is a selective, non-covalent (reversible) inhibitor of Bruton's tyrosine kinase (BTK). It binds to BTK, inhibiting its kinase activity, thereby blocking B-cell receptor signaling and reducing proliferation and survival of malignant B cells.
| Metabolism | Pirtobrutinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP2C8 and UDP-glucuronosyltransferase (UGT) enzymes. |
| Excretion | Primarily renal (80-90% as unchanged drug and minor metabolites); fecal <5%. |
| Half-life | Terminal half-life approximately 15-20 hours in adults with normal renal function; prolonged in renal impairment (up to 30-40 hours in severe impairment). |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.5-1.0 L/kg; indicates distribution into total body water and some tissue binding. |
| Bioavailability | Oral: 60-70% (subject to first-pass metabolism). Less than 5% via topical or other non-IV routes. |
| Onset of Action | Oral: 1-2 hours; intravenous: immediate (within minutes). |
| Duration of Action | Approximately 12-24 hours; clinical effect persists for the dosing interval. Note: Duration may be extended in renal impairment. |
The recommended adult dose is 15 mg orally once daily, with or without food.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min). For severe renal impairment (eGFR 15–29 mL/min), reduce dose to 5 mg once daily. Not recommended for eGFR <15 mL/min or dialysis. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 5 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy in pediatric patients under 18 years have not been established. |
| Geriatric use | No specific dose adjustment required; monitor for adverse effects due to potential age-related renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for JAYPIRCA (JAYPIRCA).
| Breastfeeding | Paclitaxel is excreted into breast milk. M/P ratio not established. Due to potential for severe adverse reactions in nursing infants, breastfeeding is contraindicated during treatment and for at least 2 weeks after the last dose. |
| Teratogenic Risk | JaypirCa (paclitaxel) is teratogenic. First trimester: high risk of miscarriage and major malformations (neural tube, cardiac, skeletal). Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and premature delivery. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
None
| Precautions | ["Hemorrhage: Major hemorrhagic events, including fatal bleeding, have occurred. Monitor for signs of bleeding and consider risks of anticoagulant/antiplatelet use.","Infections: Serious, including fatal, infections have occurred, including opportunistic infections.","Cytopenias: Grade 3 or 4 neutropenia, thrombocytopenia, and anemia can occur; monitor blood counts.","Cardiac arrhythmias: Atrial fibrillation and flutter have been reported.","Second primary malignancies: Including skin cancers and other solid tumors.","Hepatotoxicity: Hepatotoxicity has been observed; monitor liver function."] |
| Food/Dietary | Avoid grapefruit and grapefruit products as they may increase pirtobrutinib levels. No other significant food interactions known. Take with or without food. |
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| Fetal Monitoring |
| Monitor maternal complete blood count (CBC) with differential, liver function tests (LFTs), and neurologic status. For fetus: ultrasound for growth and amniotic fluid volume; consider fetal echocardiography if exposure in first trimester. |
| Fertility Effects | Paclitaxel can cause ovarian failure, resulting in irreversible infertility in premenopausal women. May also cause azoospermia or oligospermia in men, potentially reversible. |
| Clinical Pearls | Jaypirca (pirtobrutinib) is a non-covalent BTK inhibitor approved for relapsed/refractory mantle cell lymphoma after prior BTK inhibitor therapy. It bypasses C481 mutations that confer resistance to covalent BTK inhibitors. Monitor for atrial fibrillation, hypertension, and hemorrhage. Use with caution in patients on anticoagulants. Check baseline ECG and monitor QTc. Dose adjustments required for severe hepatic impairment (Child-Pugh C). |
| Patient Advice | Take Jaypirca exactly as prescribed, usually once daily with or without food. · Do not crush, chew, or split tablets; swallow whole. · Avoid grapefruit, grapefruit juice, and Seville oranges during treatment. · Report any signs of bleeding (unusual bruising, black/tarry stools, blood in urine) or infection (fever, chills) immediately. · Contact your doctor if you experience rapid or irregular heartbeat, chest pain, or dizziness. · Use effective contraception during treatment and for at least 1 week after last dose. · Do not breastfeed while taking Jaypirca. |