INCRELEX
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 7649 |
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 | INCRELEX (mecasermin) is teratogenic in animals; use only if potential benefit justifies risk to fetus. |
| 2nd trimester | Avoid use; insufficient human data; may cause fetal hypoglycemia or overgrowth. |
| 3rd trimester | Avoid near term due to risk of neonatal hypoglycemia and potential for excessive growth. |
Clinical note
Comprehensive clinical and safety monograph for INCRELEX (INCRELEX).
| Placental transfer | Expected to cross placenta due to molecular weight and similarity to endogenous IGF-1; animal studies confirm transfer. |
| Breastfeeding | Excretion into human milk unknown; caution advised. Consider benefits vs risks; monitor infant for hypoglycemia. |
| Lactation Rating | L4 |
| 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. |
| 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. |
■ 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 |
Hypersensitivity to mecasermin or any componentActive or suspected neoplasiaEpiphyseal closure (for growth promotion)Intracranial hypertension
| 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 |
| Food/Dietary | Must be administered within 20 minutes of a meal or snack containing carbohydrates to reduce risk of hypoglycemia. Avoid fasting or skipping meals. Grapefruit/grapefruit juice may alter CYP3A4 metabolism; avoid concurrent use. Alcohol can increase hypoglycemia risk; limit or avoid. |
| Clinical Pearls | INCRELEX (mecasermin) is recombinant human insulin-like growth factor-1 (IGF-1) used for growth failure in severe primary IGF-1 deficiency. Monitor blood glucose closely due to risk of hypoglycemia; administer within 20 minutes of a meal or snack. Do not use in patients with closed epiphyses, active malignancy, or history of malignancy. Can cause intracranial hypertension (pseudotumor cerebri); monitor for headache, visual disturbances. Injection site reactions common. |
| Patient Advice | Do not use INCRELEX if you have cancer or a history of cancer. · Take exactly as prescribed; inject within 20 minutes after a meal or snack to prevent low blood sugar. · Do not inject into the same site repeatedly; rotate injection sites. · Watch for signs of low blood sugar (shakiness, sweating, confusion) and have fast-acting sugar (e.g., juice, glucose tablets) available. · Report severe headache, vision changes, or nausea immediately (possible increased pressure in the skull). · Inform all healthcare providers you are using this medication. |
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