INCRELEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INCRELEX (INCRELEX).
Insulin-like growth factor 1 receptor agonist; promotes linear growth by stimulating chondrocyte proliferation at epiphyseal plates and exerts anabolic effects on muscle, bone, and other tissues.
| Metabolism | Primarily metabolized by proteolysis into smaller peptides and amino acids; not significantly metabolized by CYP enzymes. |
| Excretion | Renal: ~95% of absorbed dose as unchanged drug and metabolites; fecal: <5%. |
| Half-life | Terminal elimination half-life is approximately 8-10 hours in adults; clinically, steady-state is achieved within 2-3 days. |
| Protein binding | Approximately 90% bound to insulin-like growth factor binding proteins (IGFBPs). |
| Volume of Distribution | Vd ~0.3-0.5 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Subcutaneous: 80-100% (high bioavailability). |
| Onset of Action | Subcutaneous: 15-30 minutes for glucose-lowering effect; peak effect at 1-2 hours. |
| Duration of Action | Subcutaneous: Duration of glucose-lowering effect is 4-6 hours; clinical effect may persist up to 8 hours depending on dose. |
Intravenous bolus of 0.1 mg/kg given over 1 minute, followed by continuous intravenous infusion of 0.6 mg/kg/min for 30 minutes. Alternatively, a single intravenous bolus dose of 0.3 mg/kg.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended for renal impairment; use with caution in patients with severe renal impairment (eGFR < 30 mL/min/1.73 m²) due to limited data. |
| Liver impairment | No specific dose adjustment recommended for hepatic impairment; use with caution in patients with Child-Pugh class C cirrhosis due to potential risk of hypoglycemia. |
| Pediatric use | Not approved for use in pediatric patients. Safety and efficacy in children have not been established. |
| Geriatric use | No specific dose adjustment recommended; elderly patients may be more sensitive to hypoglycemic effects; monitor blood glucose closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for INCRELEX (INCRELEX).
| Breastfeeding | Excretion into human milk unknown; molecular weight (7.5 kDa) suggests minimal transfer. M/P ratio not established. Caution recommended; alternative feeding may be considered until more data available. |
| Teratogenic Risk | INCRELEX (mecasermin) is an IGF-1 analog. In animal studies, there is no evidence of teratogenicity; however, data in pregnant women are insufficient. First trimester: No known malformation risk. Second/third trimesters: Fetal overgrowth (macrosomia) may occur if maternal IGF-1 levels are elevated. Caution advised. |
■ FDA Black Box Warning
Increased risk of neoplasms; do not use in patients with active or suspected malignancy. Monitor for progression of pre-existing nevi.
| Serious Effects |
["Active or suspected malignancy (including intracranial tumors)","Closed epiphyses (skeletal maturity)","Acute critical illness (due to increased mortality with ICU use)","Hypersensitivity to mecasermin or any component"]
| Precautions | ["Risk of malignancy (including intracranial tumors)","Lymphoproliferative disorders","Intracranial hypertension (pseudotumor cerebri)","Slipped capital femoral epiphysis","Progression of scoliosis","Pancreatitis","Hypoglycemia (especially with fasting or missed meals)","Fluid retention (edema, pericardial effusion)","Hypersensitivity reactions including anaphylaxis","Thymic hypertrophy"] |
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| Fetal Monitoring |
| Monitor maternal blood glucose and IGF-1 levels. For fetus, serial ultrasound for growth (macrosomia) and amniotic fluid volume. Assess for signs of hypoglycemia or hyperglycemia. |
| Fertility Effects | In animal studies, no adverse effects on fertility. In humans, no known impairment. Use as directed without significant reproductive toxicity anticipated. |