JASCAYD
Clinical safety rating: caution
Comprehensive clinical and safety monograph for JASCAYD (JASCAYD).
JASCAYD (tasquinimod) is a selective allosteric inhibitor of S100A9, which binds to toll-like receptor 4 (TLR4) and receptor for advanced glycation end-products (RAGE). It modulates the tumor microenvironment by inhibiting myeloid-derived suppressor cell (MDSC) recruitment and function, reducing angiogenesis, and enhancing anti-tumor immune responses.
| Metabolism | Primarily metabolized by CYP3A4 and CYP1A2; minor contributions from CYP2C9 and CYP2C19. |
| Excretion | Primarily renal excretion (80%) as unchanged drug; 20% fecal via biliary elimination. |
| Half-life | Terminal elimination half-life is 12-15 hours; clinically relevant for once-daily dosing. |
| Protein binding | 98% bound primarily to serum albumin. |
| Volume of Distribution | Vd approximately 0.5 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is 60-70% with no significant food effect. |
| Onset of Action | Oral: 1-2 hours to peak plasma concentration; clinical effect onset within 2-4 hours. |
| Duration of Action | Duration of clinical effect approximately 24 hours, supporting once-daily administration. |
Adults: 300 mg orally twice daily with food.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment required for GFR ≥30 mL/min. Not recommended if GFR <30 mL/min. |
| Liver impairment | Mild (Child-Pugh A): No adjustment. Moderate (Child-Pugh B): 150 mg orally twice daily. Severe (Child-Pugh C): Not recommended. |
| Pediatric use | Not approved for patients <18 years of age. |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for JASCAYD (JASCAYD).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. M/P ratio unknown. Because of potential for serious adverse reactions in nursing infants, advise women not to breastfeed during treatment and for at least 2 weeks after last dose. |
| Teratogenic Risk | JASCAYD (asciminib) is a tyrosine kinase inhibitor with potential teratogenic effects. In animal studies, it caused embryo-fetal toxicity and malformations at clinically relevant exposures. First trimester: risk of major congenital malformations. Second/third trimester: potential for fetal growth restriction and adverse developmental outcomes. Adequate human data are lacking; avoid use during pregnancy unless benefit outweighs risk. |
■ FDA Black Box Warning
No FDA black box warnings reported.
| Serious Effects |
Hypersensitivity to tasquinimod or any excipients; concurrent use with potent CYP3A4 inducers; pregnancy and lactation.
| Precautions | Cardiovascular events (hypertension, thrombosis), hepatotoxicity, gastrointestinal perforation, hemorrhage, thromboembolic events, and embryo-fetal toxicity. |
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| Fetal Monitoring | Monitor complete blood count, hepatic and pancreatic enzymes, and serum uric acid monthly. Assess for fluid retention (pericardial, pleural effusion) and hypertension. In pregnancy, perform serial fetal ultrasound for growth and anatomy. Monitor maternal blood pressure and renal function. |
| Fertility Effects | Based on animal studies, JASCAYD may impair male and female fertility. In females, decreased ovarian function and irregular estrous cycles; in males, reduced sperm count and motility. Human data limited; potential for reversible impairment. |