Dosing and uses of Increlex (mecasermin)
Adult dosage forms and strengths
Not indicated for adult use
Pediatric dosage forms and strengths
injectable solution
- 10mg/mL
Growth Failure
Indicated for long-term treatment of growth failure in children with severe primary IGF-1 deficiency (Primary IGFD) or with growth hormone (GH) gene deletion who have developed neutralizing antibodies to GH
Increlex: 40-80 mcg/kg SC q12hr, may increase after 1 week by 40 mcg/kg/dose, not to exceed 120 mcg/kg SC q12hr
Rett Syndrome (Orphan)
Orphan designation for treatment of Rett syndrome
Sponsor
- Keck Graduate Institute of Applied Life Sciences; 535 Watson Drive; Claremont, California 91711
Increlex (mecasermin) adverse (side) effects
>10%
Hypoglycemia (42%)
Tonsillar hypertrophy (15%)
1-10%
Cardiac murmur (>5%)
Dizziness (>5%)
Convulsion (>5%)
Headache (>5%)
Lipohypertrophy (>5%)
Thymus hypertrophy (>5%)
Arthralgia (>5%)
Ear problems (>5%)
Otitis media (>5%)
<1%
Anaphylaxis
Generalized urticaria
Angioedema
Dyspnea
Local allergic reactions at the injection site (eg, pruritus, urticaria)
Alopecia, hair texture abnormaL
Postmarketing Reports
General disorders and administrative site conditions: Injection site reactions (eg, erythema, pain, hematoma, hemorrhage, induration, rash, swelling)
Musculoskeletal and connective tissue disorders: Osteonecrosis/avascular necrosis (occasionally associated with slipped capital femoral epiphysis)
Warnings
Contraindications
Hypersensitivity to product or components
Closed epiphyses
Active or suspected neoplasia; discontinue if neoplasia develops
IV administration
Cautions
Do not give without meal/snack 20 min before/after (risk of hypoglycemia)
Not a substitute for GH treatment
Contains benzyl alcohol as preservative (associated with fatal "Gasping Syndrome" in preemies)
Possibility of thickening of facial soft tissues
Allergic reactions reported include localized (injection site) reactions to severe systemic reactions, including anaphylaxis requiring hospitalization
Symptoms associated with intracranial hypertension including nausea, headache, papilledema, vomiting, visual changes reported; funduscopic examinations are recommended
Lymphoid hypertrophy that may lead to complications such as chronic middle ear effusions, snoring, and sleep apnea reported
Children experiencing rapid growth may have progression of scoliosis
Caution in patients at risk for diabetes or patients being treated for diabetes
Treat thyroid deficiency prior to therapy
Evaluate any child with onset of a limp or hip/knee pain for possible slipped capital femoral epiphysis
Pregnancy and lactation
Pregnancy category: C
Lactation: Not known whether excreted in breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Increlex (mecasermin)
Mechanism of action
Recombinant human IGF-1 used as replacement therapy in patients primary severe IGF-I deficiency, growth hormone receptors in the liver that are unresponsive to GH
Pharmacokinetics
Metabolism: Liver, kidney
Half-Life: 5.8 hr (mecasermin); >12 hr (mecasermin rinfabate)
Excretion: Likely as native proteins
Vd: 0.184-0.33 L/kg
Protein binding: 80% bound to IFGBP-3 and an acid-labile subunit
Administration
SC Injection
Give shortly before/after meal or snack (~20 minutes) to avoid hypoglycemia
If hypoglycemia occurs with recommended doses despite adequate food intake, the dose should be reduced
Rotate injection site to avoid lipodystrophy
Storage
Refrigerate unopened vials; after opening, vial contents are stable for 30 days when refrigerated
