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. |
| Molecular Weight | 362.47 |
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 | Avoid due to known teratogenicity (major congenital malformations). |
| 2nd trimester | Contraindicated due to fetal toxicity. |
| 3rd trimester | Contraindicated due to risk of fetal harm. |
Clinical note
Comprehensive clinical and safety monograph for JASCAYD (JASCAYD).
| Placental transfer | Crosses placenta in animal studies; human data limited but expected due to low molecular weight. |
| Breastfeeding | Excretion into human milk unknown; risk of serious adverse reactions in infant. Recommend discontinue drug or breastfeeding. |
| Lactation Rating | L5 (Contraindicated) |
■ FDA Black Box Warning
No FDA black box warnings reported.
| Serious Effects |
PregnancyHypersensitivity to JASCAYD
| Precautions | Cardiovascular events (hypertension, thrombosis), hepatotoxicity, gastrointestinal perforation, hemorrhage, thromboembolic events, and embryo-fetal toxicity. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase JASCAYD plasma concentrations. No other significant food interactions reported. Take with or without food. |
| Clinical Pearls | JASCAYD (asciminib) is a BCR-ABL1 inhibitor specifically targeting the myristoyl pocket (STAMP inhibitor). It is indicated for Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase previously treated with two or more tyrosine kinase inhibitors. Monitor pancreatic enzymes regularly due to risk of pancreatitis. Avoid use with strong CYP3A4 inducers. QT interval prolongation possible; obtain ECG before and during treatment. |
Loading safety data…
| 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. |
| 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. |
| Patient Advice | Take JASCAYD exactly as prescribed, usually once daily with or without food. · Do not crush, cut, or chew tablets; swallow whole. · Report any signs of pancreatitis (severe abdominal pain, nausea, vomiting) immediately. · Avoid grapefruit and grapefruit juice while taking this medication due to potential interaction. · Inform your doctor of all medications, including over-the-counter drugs and supplements. · JASCAYD may cause QT prolongation; notify your doctor if you experience fainting or irregular heartbeat. |