Summary about Zomacton
Zomacton is a recombinant human growth hormone (GH) indicated for the treatment of pediatric patients with:
- Growth failure due to inadequate secretion of endogenous GH
- Short stature associated with Turner syndrome
- Idiopathic short stature (ISS)
- Short stature or growth failure in short stature homeobox-containing gene (SHOX) deficiency
- Short stature born small for gestational age (SGA) with no catch-up growth by 2 to 4 years
Zomacton is also indicated for the replacement of endogenous GH in adults with GH deficiency.
Zomacton is a proven somatropin therapy that has been trusted for more than 3 years and prescribed for more than 3500 patients.
The goal of GH therapy in pediatric patients is to sustain normal linear growth and achieve a normal adult height. In addition to promoting linear growth, GH has favourable effects on muscle accretion and bone mineral density. GH stimulates osteoblast and osteoclast differentiation and promotes the accretion of bone mass. GH stimulates the proliferation of adipose precursor cells, restricts their differentiation into mature adipocytes, and limits deposition of fat in the abdominal visceral area. Consequently, children with growth hormone deficiency (GHD) demonstrate reduced linear growth, reduced lean body mass, increased body fat with disproportionate deposition of visceral and truncal fat, subnormal bone mineral density and lipid abnormalities. Untreated patients with adult onset GHD demonstrate all the pediatric consequences with the exception of a linear growth effect. Untreated adults with GHD have also decreased muscle strength, impaired cardiac function, and decreased quality of life.
Zomacton for injection is a white, lyophilized powder available as:
- 5 mg vial with a 5 mL vial of bacteriostatic 0.9% sodium chloride [preserved with benzyl alcohol]
- 10 mg vial with a syringe of 1 mL of bacteriostatic water [preserved with metacresol] with a 25G reconstitution needle
- 10 mg vial with a syringe of 1 mL of bacteriostatic water [preserved with metacresol] with a vial adapter
Zomacton is contrainidicated in following cases:
- Acute critical illness
- Children with Prader-Willi Syndrome who are severely obese or have severe respiratory impairment – reports of sudden death
- Active malignancy
- Hypersensitivity to somatropin or its excipients
- Active proliferative or severe non-proliferative diabetic retinopathy
- Children with closed epiphyses
- Known hypersensitivity to somatropin or excipients
- Diabetic retinopathy.
|No data about interaction|
|Caution is recommended. Excretion into human milk is unknown. |
Following subcutaneous administration of radiolabelled medication in animal studies, radioactivity was transferred to milk reaching four times the concentration found in maternal plasma. However, absorption of the intact protein in the gastrointestinal tract of the infant is considered extremely unlikely.
Connective Tissue Metabolism:
Somatropin has been studied following subcutaneous, and intravenous administration in adult healthy subjects. A single subcutaneous dose of 4 mg ZOMACTON in healthy subjects (n=54) with suppressed endogenous growth hormone resulted in a mean (SD) Cmax of 38.1 (19.3) ng/mL after approximately 4.5 hours. The absolute bioavailability of somatropin is approximately 70% after subcutaneous administration.
The mean (SD) apparent volume of distribution of somatropin after single dose subcutaneous administration of 4 mg ZOMACTON in healthy subjects is 53.3 (24.6) L.
Extensive metabolism studies have not been conducted. The metabolic fate of somatropin involves classical protein catabolism in both the liver and kidneys.
In healthy subjects, mean somatropin clearance is 0.133 L/min following intravenous administration. The mean elimination half-life of intravenous somatropin is 0.42 hours, whereas subcutaneously administered somatropin has a mean half-life of 2.3 hours. The longer half-life observed after subcutaneous administration is due to slow absorption from the injection site. Urinary excretion of intact somatropin has not been measured.
Geriatric patients: The pharmacokinetics of somatropin have not been studied in patients greater than 65 years of age.
Pediatric patients: The pharmacokinetics of somatropin in pediatric patients are similar to those of adults.
Male and Female Patients. No gender-specific pharmacokinetic studies have been performed with somatropin. The available literature indicates that the pharmacokinetics of somatropin are similar in men and women.
Patients with Renal or Hepatic Impairment: No studies have been performed with somatropin.
|Approximate Retail Price |
Injectible powder for injection:
lyophilisate for solution for injection:
|Injection for subcutaneous use|
|Administer by subcutaneous injection to the back of upper arm, abdomen, buttock, or thigh with regular rotation of injection sites. |
• Pediatric dosage:
– Divide the calculated weekly dosage into equal doses given either 3, 6, or 7 days per week
– The recommended weekly dose is 0.18 mg/kg/week to 0.3 mg/kg/week
• Adult dosage:
Either of the following two dosing regimens may be used:
– Non-weight based dosing: Initiate with a dose of approximately 0.2 mg/day (range, 0.15 mg/day-0.3 mg/day) and increase the dose every 12 months by increments of approximately 0.1 mg/day-0.2 mg/day, according to individual patient requirements.
– Weight-based dosing (Not recommended for obese patients): Initiate at 0.006 mg/kg daily and increase the dose according to individual patient requirements to a maximum of 0.0125 mg/kg daily
|H01AC – Somatropin and somatropin agonists|
|No known interactions|
|Zomacton sometimes is covered by health insurance if considered medically necessary, but some patients have had coverage denied. The Magic Foundation offers help making the case for coverage or appealing a denial, and outlines patients’ experiences getting approval.|
|Inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1: |
May require the initiation of glucocorticoid replacement therapy. Patients treated with glucocorticoid replacement for previously diagnosed hypoadrenalism may require an increase in their maintenance dosesGlucocorticoid Replacement Therapy:
Should be carefully adjustedCytochrome P450-Metabolized Drugs:
Monitor carefully if used with somatropinOral Estrogen:
Larger doses of somatropin may be required in womenInsulin and/or Oral/Injectable Hypoglycemic Agents:
May require adjustment
Is Available Generically
|No. There is currently no therapeutically equivalent version of Zomacton available.|
Is not subject to the Controlled Substances Act.
|FERRING PHARMACEUTICALS INC.|
Mechanism of Action
|Somatropin binds to the human growth hormone receptor (GHR). Upon binding, soatropin causes dimerization of GHR, activation of the GHR-associated JAK2 tyrosine kinase, and tyrosyl phosphorylation of both JAK2 and GHR. These events recruit and/or activate a variety of signaling molecules, including MAP kinases, insulin receptor substrates, phosphatidylinositol 3′ phosphate kinase, diacylglycerol, protein kinase C, intracellular calcium, and Stat transcription factors. These signaling molecules contribute to the GH-induced changes in enzymatic activity, transport function, and gene expression that ultimately culminate in changes in growth and metabolism.|
Non Proprietary Name
|Short-term overdosage could lead initially to hypoglycemia and subsequently to hyperglycemia. Furthermore, overdose with somatropin is likely to cause fluid retention. |
Long-term overdosage could result in signs and symptoms of gigantism and/or acromegaly consistent with the known effects of excess growth hormone
AU TGA pregnancy category B2: Drugs which have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malformation or other direct or indirect harmful effects on the human fetus having been observed. Studies in animals are inadequate or may be lacking, but available data show no evidence of an increased occurrence of fetal damage.
US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
|Use is not recommended unless clearly needed. |
Animal studies did not show any teratogenicity or adverse effects on gestation, morphogenesis, parturition, lactation, postnatal development, or reproductive capacity of the offspring; a slight increase in fetal death and increased body weight of pups, and reduced pregnancy rate, increased litter size, irregular estrus cycles, and decreased sperm motility in the parents were seen. There are no controlled data in human pregnancy.
|Tesamorelin, Mecasermin rinfabate, Sermorelin, Mecasermin, Somatrem|
Acute Critical Illness: Potential benefit of treatment continuation should be weighed against the potential risk.
Prader-Willi Syndrome in Children: Evaluate for signs of upper airway obstruction and sleep apnea before initiation of treatment for GHD. Discontinue treatment if these signs occur.
Neoplasm: Monitor patients with preexisting tumors for progression or recurrence. Increased risk of a second neoplasm in childhood cancer survivors treated with somatropin – in particular meningiomas in patients treated with radiation to the head for their first neoplasm.
Impaired Glucose Tolerance and Diabetes Mellitus: May be unmasked. Periodically monitor glucose levels in all patients. Doses of concurrent antihyperglycemic drugs in diabetics may require adjustment.
Intracranial Hypertension: Exclude preexisting papilledema. May develop and is usually reversible after discontinuation or dose reduction.
Hypersensitivity: Serious hypersensitivity reactions may occur. In the event of an allergic reaction, seek prompt medical attention.
Fluid Retention (i.e., edema, arthralgia, carpal tunnel syndrome – especially in adults): May occur frequently. Reduce dose as necessary.
Hypoadrenalism: Monitor patients for reduced serum cortisol levels and/or need for glucocorticoid dose increases in those with known hypoadrenalism.
Hypothyroidism: May first become evident or worsen.
Slipped Capital Femoral Epiphysis: May develop. Evaluate children with the
onset of a limp or hip/knee pain.
Progression of Preexisting Scoliosis: May develop.
Pancreatitis: Consider pancreatitis in patients with persistent severe abdominal pain.