Dosing and uses of Egrifta (tesamorelin)
Adult dosage forms and strengths
injection, subcutaneous
- 2mg/vial (1mg/mL solution after reconstituted)
HIV-Associated Lipodystrophy
2 mg SC qDay, preferably once daily
Inject into abdomen (avoid the navel or any scar tissue) and rotate injection site daily
Limitations of use
Long-term cardiovascular benefit and safety not studied
Not indicated for weight loss management (weight neutral effect)
There are no data to support improved compliance with anti-retroviral therapies in HIV-positive patients taking tesamorelin
Administration
Reconstitute lyophilized powder with supplied 2.1 mL of diluent
Mix by rolling the vial gently in your hands for 30 seconds
Do not shake
Storage
Unopened vial: Store refrigerated between 2-8°C (36-46°F) until the expiration date or below 25°C (77°F) for 3 months or until the expiration date, whichever occurs first
Protect from light
Do not freeze
Store reconstitution diluent (Sterile Water for Injection, USP), syringes, and needles at controlled room temperature of 20-25°C (68-77°F)
Do not freeze or refrigerate the reconstituted solution
Pediatric dosage forms and strengths
Safety and efficacy not established
Should not be used in children with open epiphyses, among whom excess GH and IGF-I may result in linear growth acceleration and excessive growth
Egrifta (tesamorelin) adverse (side) effects
>10%
Arthralgia (13.3%)
1-10%
Injection site reactions (up to 8.5%)
Extremity pain (6.1%)
Myalgia (5.5%)
Paresthesia (4.8%)
Nausea (4.4%)
Hypoesthesia (4.2%)
Rash (3.7%)
Vomiting (2.6%)
Pruritus (2.4%)
Depression (2%)
Dyspepsia (1.7%)
Musculoskeletal pain and stiffness (1.7-1.8%)
Increased CPK (1.5%)
Carpal tunnel syndrome (1.5%)
Joint stiffness/swelling (1.1-1.5%)
Hypertension (1.3%)
Muscle spasms (1.1%)
< 1%
Anemia
Abdominal abscess
Cerebellar syndrome
Mental status changes
Sepsis
Trigeminal neuralgia
Viral bronchitis
Upper respiratory tract infection
Warnings
Contraindications
Hypersensitivity to tesamorelin or mannitoL
Disruption of HP axis caused by hypophysectomy, hypopituitarism, pituitary tumor/surgery, head irradiation, or head trauma
Active malignancy
Pregnancy
Cautions
Caution with history of nonmalignant neoplasms; preexisting malignancy should be inactive and treatment complete prior to initiating therapy
If hypersensitivity suspected, discontinue and provide immediate medical attention
Consider discontinuing with persistent elevations of IGF-I levels (eg, >3 SDS), particularly if efficacy response is not robust
Fluid retention may occur and may include edema, arthralgia, and carpal tunnel syndrome
Increased mortality with acute critical illness due to complications following open heart surgery, abdominal surgery, multiple accidental trauma, or acute respiratory failure following treatment with pharmacologic amounts of growth hormone
May modulate CYP450-mediated antipyrine clearance
Not for use in children when epiphyses open because may cause excessive growth
Inhibits 11-beta-hydroxysteroid dehydrogenase type-1, a microsomal enzyme required for conversion of cortisone and prednisone to their active metabolites
Injections site reactions including irritation, erythema, pain, and bruising may occur; rotate site of injection to different areas of abdomen to reduce incidence of injection site reactions
May increase risk of development of diabetes due to glucose intolerance; evaluate glucose status prior to and during therapy
Not indicated for weight loss management
Pregnancy and lactation
Pregnancy category: X
During pregnancy, visceral adipose tissue increases due to normal metabolic and hormonal changes; modifying this physiologic change offers no known benefit and could result in fetal harm
Administration to rats during organogenesis and lactation resulted in hydrocephaly in offspring at 2-4 times clinical dose
Lactation: Unknown whether distributed in breast milk; not recommended
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 Egrifta (tesamorelin)
Mechanism of action
Growth hormone releasing factor (GRF) analog; stimulates growth hormone production and increases serum IGF-I; elicits anabolic and lipolytic actions;
Pharmacokinetics
Half-Life: 38 minutes
Absorption: <4%
Peak Plasma Time: 9 min
Peak Plasma Concentration (Cmax): 2822.3 pg/mL
Vd: 10.5 L/kg (HIV infected patients); 9.4 L/kg (healthy adults)
Bioavailability: <4% (healthy adults)
