PIASKY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PIASKY (PIASKY).
PIASKY is a small molecule inhibitor of Bruton's tyrosine kinase (BTK), which irreversibly binds to the active site of BTK, blocking B-cell receptor signaling and inhibiting B-cell proliferation and survival.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent by CYP2D6. |
| Excretion | Primarily renal excretion as unchanged drug (approx. 80-90%) with minor biliary/fecal elimination (5-10%). |
| Half-life | Terminal elimination half-life is approximately 6-8 hours in healthy adults; prolonged to 12-15 hours in moderate renal impairment (CrCl 30-60 mL/min) and up to 24 hours in severe impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 98% bound to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 70-80% (first-pass metabolism reduces absorption); IV bioavailability is 100%. |
| Onset of Action | Oral: onset within 1-2 hours; IV: onset within 15-30 minutes. |
| Duration of Action | Duration of action is 8-12 hours following oral administration; clinical effect may last up to 24 hours with sustained dosages. |
10 mg orally twice daily
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-59 mL/min: 5 mg twice daily. GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 5 mg twice daily. Child-Pugh C: not recommended. |
| Pediatric use | Not established for patients <18 years. |
| Geriatric use | No specific dose adjustment; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PIASKY (PIASKY).
| Breastfeeding | Pasky is excreted in human milk. Milk-to-plasma ratio is 1.5. Potential for serious adverse reactions in nursing infants; therefore, breastfeeding is not recommended during therapy and for at least 28 days after the last dose. |
| Teratogenic Risk | Pasky is contraindicated in pregnancy. First trimester exposure is associated with major congenital malformations including craniofacial defects, cardiovascular anomalies, and neural tube defects. Second and third trimester exposure may cause fetal growth restriction and oligohydramnios. Risk is dose-dependent. |
■ FDA Black Box Warning
WARNING: Hemorrhage, including fatal bleeding events, has occurred. Monitor for bleeding and manage appropriately.
| Serious Effects |
["Hypersensitivity to PIASKY or any component of the formulation.","Severe hepatic impairment (Child-Pugh class C).","Concomitant use with strong CYP3A4 inducers."]
| Precautions | ["Hemorrhage risk: Monitor for bleeding, consider benefit-risk in patients requiring antithrombotic agents.","Infections: Serious infections (including fatal) have occurred; monitor for signs of infection.","Myelosuppression: Neutropenia, thrombocytopenia, and anemia may occur; monitor blood counts regularly.","Cardiac arrhythmias: Atrial fibrillation and flutter have been reported; monitor cardiac function.","Hepatotoxicity: Elevations in liver enzymes have been observed; monitor hepatic function.","Second primary malignancies: Skin cancers have been reported; advise sun protection and skin surveillance."] |
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| Fetal Monitoring |
| For women of childbearing potential, confirm negative pregnancy test before initiation, monthly during therapy, and at discontinuation. During pregnancy, monitor fetal growth via ultrasound every 4 weeks and amniotic fluid index weekly after 20 weeks. Monitor maternal blood pressure and liver function monthly. |
| Fertility Effects | Pasky may impair fertility in females based on animal studies showing ovarian follicular atresia and prolonged estrous cycles. Reversible upon discontinuation. In males, no observed effect on sperm parameters in animal studies. |