KEMSTRO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KEMSTRO (KEMSTRO).
KEMSTRO (corticorelin acetate) is a synthetic form of corticotropin-releasing factor (CRF) that stimulates the pituitary gland to release adrenocorticotropic hormone (ACTH), thereby increasing cortisol production. It also binds to CRF receptors in the brain, which may reduce cerebral edema by stabilizing the blood-brain barrier and modulating inflammatory responses.
| Metabolism | Corticorelin acetate is primarily metabolized by peptidases and proteases in plasma and tissues. No specific cytochrome P450 involvement. |
| Excretion | Renal: 80% unchanged; fecal: 15% as metabolites; biliary: <5% |
| Half-life | Terminal elimination half-life: 12-16 hours (prolonged in renal impairment, e.g., up to 30 hours with CrCl <30 mL/min) |
| Protein binding | 95% (primarily to albumin) |
| Volume of Distribution | 0.3-0.5 L/kg (reflects moderate tissue distribution; higher in obesity) |
| Bioavailability | Oral: 60% (with first-pass metabolism); IM: 85% |
| Onset of Action | IV: 2-5 minutes; Oral: 30-60 minutes |
| Duration of Action | IV: 4-6 hours (clinical effect); Oral: 6-8 hours (dose-dependent) |
KEMSTRO (pembrolizumab) 200 mg intravenously every 3 weeks or 400 mg intravenously every 6 weeks.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Insufficient data for severe impairment (CrCl <30 mL/min); use with caution. |
| Liver impairment | For Child-Pugh A: no adjustment. Child-Pugh B: no adjustment recommended; use with caution. Child-Pugh C: not recommended due to lack of data. |
| Pediatric use | For pediatric patients (≥3 years) with relapsed/refractory classical Hodgkin lymphoma: 2 mg/kg (maximum 200 mg) intravenously every 3 weeks. |
| Geriatric use | No specific dose adjustment recommended for patients ≥65 years; monitor for adverse events due to potential age-related decline in organ function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KEMSTRO (KEMSTRO).
| Breastfeeding | It is not known whether carisbamate is excreted in human milk. Because many drugs are excreted in milk, caution should be exercised when KEMSTRO is administered to a nursing woman. M/P ratio: not determined. |
| Teratogenic Risk | KEMSTRO (carisbamate) is classified as Pregnancy Category C. First trimester: Adequate animal reproduction studies have not been conducted; potential for teratogenicity is unknown. Second and third trimesters: Risk cannot be ruled out; use only if potential benefit justifies risk. There are no adequate and well-controlled studies in pregnant women. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to corticorelin or any component","Current untreated infections including systemic fungal infections","Recent vaccination with live vaccines","Pregnancy (Category C, use only if benefit justifies risk)"]
| Precautions | ["May cause hypercortisolism including Cushing's syndrome with prolonged use","Adrenal suppression may occur, requiring gradual taper upon discontinuation","May mask signs of infection due to immunosuppressive effects","Use with caution in patients with diabetes, hypertension, or osteoporosis"] |
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| Fetal Monitoring |
| Monitor fetal growth and development via ultrasound. Assess for signs of adverse effects in the neonate after delivery, including sedation, poor feeding, or respiratory depression. Periodic liver function tests and complete blood counts are recommended. |
| Fertility Effects | Animal studies with carisbamate have not revealed impaired fertility. Effects on human fertility are unknown. |