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Tesamorelin

Pronunciation

(tes a moe REL in)

Index Terms

  • Tesamorelin Acetate
  • TH9507

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

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Solution Reconstituted, Subcutaneous [preservative free]:

Egrifta: 1 mg (1 ea); 2 mg (1 ea)

Brand Names: U.S.

  • Egrifta

Pharmacologic Category

  • Growth Hormone Releasing Factor

Pharmacology

Tesamorelin binds to pituitary growth hormone-releasing factor (GRF) receptors and stimulates the secretion of endogenous growth hormone which has anabolic and lipolytic properties. Growth hormone exerts its effects by interacting with receptors on target cells such as osteoblasts, myocytes, hepatocytes, and adipocytes to promote the reduction of total fat mass. These effects are primarily mediated by IGF-1 produced in the liver and in peripheral tissues.

Distribution

Vd: Healthy adults: 9.4 ± 3.1 L/kg; HIV-infected patients: 10.5 ± 6.1 L/kg

Time to Peak

9 minutes

Half-Life Elimination

Healthy adults: 26 minutes; HIV-infected patients: 38 minutes

Use: Labeled Indications

HIV-associated lipodystrophy: Reduction of excess abdominal fat in HIV-infected patients with lipodystrophy

Contraindications

Hypersensitivity to tesamorelin, mannitol, or any component of the formulation; disruption of hypothalamic-pituitary-axis due to hypophysectomy, hypopituitarism, pituitary tumor/surgery, head irradiation or head trauma; active malignancy (newly diagnosed or recurrent); pregnancy

Dosage

HIV-associated lipodystrophy: Adults: SubQ: 2 mg once daily

Dosing adjustment for toxicity: Consider discontinuing with persistent elevations of IGF-1 (eg, >3 standard deviation scores). Discontinue if symptoms of hypersensitivity occur.

Dosage adjustment in renal impairment: There are no dosage adjustmentsprovided in the manufacturer’s labeling (has not been studied).

Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Reconstitution

Use provided diluent only. Reconstitute 2 mg vial with 2.1 mL diluent; gently roll vial for 30 seconds to mix; do not shake. When using 1 mg vials, reconstitute the first 1 mg vial with 2.2 mL diluent; gently roll vial (do not shake) for 30 seconds to mix; reconstitute the second 1 mg vial with the entire solution from first vial; gently roll vial (do not shake) for 30 seconds to mix. Use reconstituted solution immediately after prepared.

Administration

SubQ: The abdomen is the preferred site of administration; rotate site within the abdomen. Avoid injection into scar tissue, bruises, or the navel.

Storage

Store intact vials refrigerated at 2°C to 8°C (36°F to 46°F). Protect from light and store in original container until time of use. Store diluent, (sterile water for injection), syringes, and needles at 20°C to 25°C (68°F to 77°F). Use reconstituted solution immediately after prepared; do not refrigerate or freeze. Discard if not used immediately.

Drug Interactions

Cortisone: Tesamorelin may decrease serum concentrations of the active metabolite(s) of Cortisone. Consider therapy modification

PredniSONE: Tesamorelin may decrease serum concentrations of the active metabolite(s) of PredniSONE. Consider therapy modification

Adverse Reactions

10%:

Immunologic: Development of IgG antibodies (48% to 50%)

Local: Injection site reactions (6% to 25%; includes erythema [1% to 9%], pruritus [2% to 8%], pain [4%], irritation [3%], hemorrhage [2%], swelling [2%], urticaria [2%], rash [1%])

Neuromuscular & skeletal: Arthralgia (13%)

1% to 10%:

Cardiovascular: Peripheral edema (2% to 6%), hypertension (1% to 2%), chest pain (1%), palpitation (1%)

Central nervous system: Hypoesthesia (2% to 4%), depression (2%), pain (2%), insomnia (1%)

Dermatologic: Rash (4%), pruritus (1% to 2%), urticaria (1%)

Endocrine & metabolic: Diabetes mellitus (5%), Hb A1c increased (5%), hot flush (1%), hyperglycemia

Gastrointestinal: Nausea (4%), vomiting (2% to 3%), dyspepsia (2%), abdominal pain (1%)

Immunologic: Antibody development (neutralizing; tesamorelin: 10%; hGHRH: 5%)

Neuromuscular & skeletal: Pain in extremity (3% to 6%), myalgia (1% to 6%), paresthesia (2% to 5%), carpal tunnel syndrome (2%), creatine phosphokinase increased (2%), muscle stiffness (2%), musculoskeletal pain (2%), joint stiffness (2%), peripheral neuropathy (2%), joint swelling (1%), muscle spasm (1%), muscle strain (1%)

Miscellaneous: Hypersensitivity reactions (1% to 4%), night sweats (1%)

<1% (Limited to important or life-threatening): Anemia, abdominal abscess, basal cell carcinoma, bipolar II disorder, cellulitis, cerebellar syndrome, chorioretinopathy, coronary artery arteriosclerosis, dehydration, diarrhea, fracture, heart failure (congestive), impaired glucose tolerance, mental status changes, pneumonia, rectal cancer, sepsis, small intestinal obstruction, spontaneous abortion, trigeminal neuralgia, upper respiratory tract infection, viral bronchitis

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity reactions: Hypersensitivity reactions (eg, pruritus, erythema, flushing, urticaria, rash) may occur. If hypersensitivity is suspected, discontinue and instruct patient to seek immediate medical attention.

• Fluid retention: Use may result in peripheral edema manifested by increased skin turgor and musculoskeletal discomfort. May be transient or resolve upon treatment discontinuation.

• Injection site reactions: Injection site reactions (including erythema, pruritus, pain, irritation, and bruising) may occur; incidence decreases with treatment continued beyond 26 weeks. Rotating the site of injection to different areas of the abdomen may reduce incidence of reactions.

Disease-related concerns:

• Diabetes: May increase risk of development of diabetes due to glucose intolerance. Evaluate glucose status prior to treatment initiation; monitor periodically for glucose metabolism changes. Patients with diabetes should be monitored for the development or worsening of retinopathy due to increased IGF-1 levels.

• Malignancy: Release of endogenous growth hormone and increased serum IGF-1 may increase the risk for development or reactivation of malignancies. Use is contraindicated in patients with active malignancies; treatment for prior malignancy should be completed prior to initiation of tesamorelin. IGF-1 levels should be monitored during treatment; consider discontinuing with persistent IGF-1 elevations (eg, >3 standard deviation scores).

• Acute critical illness: Growth hormone is associated with an increased risk of mortality in patients with acute critical illness due to complications following open heart surgery, abdominal surgery, trauma, or acute respiratory failure. Consider discontinuing in critically ill patients.

Special populations:

• Pediatric: Should not be used in children due to risk of excess growth (gigantism) when epiphyses are open.

Other warnings/precautions:

• Appropriate use: Not indicated for weight loss management. Due to a lack of long-term cardiovascular safety/benefit data, carefully consider whether continuation of treatment is warranted in patients who do not demonstrate efficacy (based on degree of reduction of visceral adipose tissue). There is no data supporting improved compliance of antiretroviral therapy with concomitant tesamorelin.

Monitoring Parameters

Serum IGF-1 levels should be monitored at baseline and during therapy due to the potential increased risk of malignancy from sustained elevation of IGF-1 levels. Serum glucose (prior to treatment initiation); monitor periodically for glucose metabolism changes. Monitor for retinopathy in patients with diabetes. Visceral adipose tissue (by waist circumference or CT scan). Monitor for fluid retention.

Pregnancy Risk Factor

X

Pregnancy Considerations

Studies in animals have shown evidence of fetal abnormalities and use is contraindicated in pregnant women. During pregnancy, there is an increased deposition of visceral adipose tissue due to metabolic and hormonal changes. Tesamorelin decreases the deposition of visceral fat and could potentially cause harm to the unborn fetus. If pregnancy occurs during treatment, discontinue tesamorelin.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea. Have patient report immediately to prescriber signs of hyperglycemia, tachycardia, severe dizziness, syncope, dyspnea, myalgia, arthralgia, joint rigidity, painful extremities, paresthesia, arrhythmia, injection site pain or irritation, mood changes, depression, or edema of extremities (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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