Tesamorelin

What is Tesamorelin?

• Tesamorelin (EGRIFTA SV) is a growth hormone releasing factor (GHRF) analog used in the treatment of visceral adiposity in human immunodeficiency virus (HIV) infected patients with lipodystrophy.

Tesamorelin

What are the uses of this medicine?

• Tesamorelin (EGRIFTA SV) is an injectable prescription medicine used to reduce the excess stomach-area (abdominal) fat in HIV-infected adult patients with lipodystrophy. EGRIFTA SV is a growth hormone-releasing factor (GHRF).

Limitations of use:

• The long-term safety of EGRIFTA SV on the heart and blood vessels (cardiovascular) is not known.
• EGRIFTA SV is not for weight loss management.
• It is not known whether taking EGRIFTA SV helps improve how well you take (compliance with) antiretroviral medicines.
• EGRIFTA SV is not recommended to be used in children with open or closed bone growth plates (epiphyses).

How does this medicine work?

• Tesamorelin (tes" a moe rel' in) is a synthetic 44 amino acid polypeptide analogue of growth hormone releasing hormone (GHRH).
• The N terminal portion of the molecule has been modified to improve its stability and pharmacokinetics in comparison to native GHRH.
• Tesamorelin activates GHRH receptors in the pituitary which leads to synthesis and release of growth hormone that acts on multiple cells of the body including hepatocytes where it stimulates production of insulin like growth factor-1 (IGF-1).
• IGF-1 mediates many of the effects of growth hormone, which in the liver include growth, inhibition of programmed cell death, glucose update and lipolysis.
• Serum IGF-1 levels tend to be low in patients with obesity, diabetes and particularly in those with lipodystrophy.
• Tesamorelin was evaluated and found to be effective in decreasing visceral adiposity in patients with lipodystrophy associated with antiretroviral therapy of human immunodeficiency virus (HIV) infection.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have a pituitary gland tumor, have had pituitary gland surgery, have other problems related to your pituitary gland, or have had radiation treatment to your head or a head injury.
• have active cancer. Any previous cancer should be inactive and any previous cancer treatment should be complete before starting EGRIFTA SV.
• are allergic to tesamorelin or any of the ingredients in EGRIFTA SV.
• are pregnant or plan to become pregnant.

What drug interactions can this medicine cause?

• Monitor patients for potential interactions when administering EGRIFTA SV in combination with other drugs known to be metabolized by CYP450 liver enzymes.
• EGRIFTA SV stimulates GH production; therefore, patients receiving glucocorticoid replacement for previously diagnosed hypoadrenalism may require an increase in maintenance or stress doses following initiation of EGRIFTA SV.

Is this medicine FDA approved?

• Tesamorelin was approved for use in the United States as therapy to reduce excess abdominal fat in HIV-infected patients with antiviral therapy-related lipodystrophy in 2010.
• Tesamorelin is also being evaluated as therapy of insulin resistance, obesity and nonalcoholic fatty liver.

How should this medicine be used?

Recommended dosage:

• The dose of EGRIFTA SV is 1.4 mg (0.35 mL of the reconstituted solution) injected subcutaneously once daily.

Administration:

• Use EGRIFTA SV exactly as your healthcare provider tells you to use it.
• Inject EGRIFTA SV under the skin (subcutaneously) of your stomach-area (abdomen).
• Change (rotate) the injection site on your stomach-area with each dose. Do not inject EGRIFTA SV into scar tissue, bruises or your belly button.
• Do not share your EGRIFTA SV syringe or needles with other people, even if the needle has been changed. You may give other people a serious infection or get a serious infection from them.
• Use only the diluent provided, Sterile Water for Injection, USP, to reconstitute EGRIFTA SV.
• Reconstitute one vial of lyophilized powder with 0.5 mL of diluent. Mix by rolling the vial gently in your hands for 30 seconds. Do not shake.
• Inspect the reconstituted vial visually for particulate matter and discoloration. Use only if the solution is clear, colorless and without particulate matter.
• Administer 0.35 mL of EGRIFTA SV immediately following reconstitution and throw away any unused solution and diluent.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As EGRIFTA SV for injection 2 mg single-dose vial with a diluent of 10 mL of Sterile Water for Injection, USP

This medicine is available in fallowing brand namesː

• EGRIFTA SV

What side effects can this medication cause?

The most common side effects of this medicine include:

• pain in legs and arms
• muscle pain

EGRIFTA SV may cause serious side effects, including:

• increase risk of new cancer in HIV positive patients or your cancer coming back (reactivation)
• increased levels of your insulin-like growth factor-1 (IGF-1)
• fluid retention
• increase in blood sugar (glucose) or diabetes
• serious allergic reaction
• injection site reactions
• increased risk of death in people who have critical illnesses

What special precautions should I follow?

• Carefully consider the decision to start treatment with EGRIFTA SV based on the increased background risk of malignancies in HIV-positive patients. Preexisting malignancy should be inactive and its treatment complete prior to starting EGRIFTA SV. Discontinue EGRIFTA SV if there is any evidence of recurrent malignancy.
• EGRIFTA SV stimulates GH production and increases serum IGF-1, a growth factor. The effects of prolonged elevations in IGF-1 levels are unknown. Monitor IGF-1 levels during EGRIFTA SV therapy. Consider discontinuing in patients with persistent elevations.
• Fluid retention may occur during EGRIFTA SV therapy and is thought to be related to the induction of GH secretion.
• EGRIFTA SV treatment can result in glucose intolerance. Evaluate glucose prior to and during therapy.
• Hypersensitivity reactions occurred in 4% of patients treated with EGRIFTA. Advise patients to seek immediate medical attention and discontinue treatment if suspected.
• EGRIFTA SV treatment may cause injection site reactions, including injection site erythema, pruritus, pain, irritation, and bruising. Rotate injection sites to different areas of the abdomen to decrease injection site reactions.
• Increased mortality in patients with acute critical illness due to complications following open heart surgery, abdominal surgery or multiple accidental trauma, or those with acute respiratory failure has been reported. Consider discontinuation in critically ill patients.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• EGRIFTA SV is contraindicated in pregnant women because modifying visceral adipose tissue offers no benefit in pregnant women and could result in fetal harm.
• If EGRIFTA SV is used during pregnancy, or if the patient becomes pregnant while taking it, discontinue EGRIFTA SV.

Can this medicine be used in children?

• The safety and effectiveness of EGRIFTA SV in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: tesamorelin acetate
• Inactive ingredients: mannitol, sucrose, histidine, polysorbate 20

Who manufactures and distributes this medicine?

• Distributed by: Theratechnologies Inc., Montréal, Québec, Canada
• EGRIFTA SV™ is a trademark of Theratechnologies Inc.

What should I know about storage and disposal of this medication?

• You will be given two boxes from the pharmacy when you get your prescription of EGRIFTA SV:
• Store the 2 mg EGRIFTA SV vials in the Medication Box they come in, at room temperature between 68°F to 77°F (20°C to 25°C).
• Store the Sterile Water for Injection, syringes and needles that come in the Injection Box at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep EGRIFTA SV vials out of the light.
• After mixing, use EGRIFTA SV right away. Throw away any unused EGRIFTA SV after mixing.
• Do not store, freeze or refrigerate EGRIFTA SV after it has been mixed with the Sterile Water.
• Throw away any Sterile Water for Injection left in the bottle after use.
• Do not use EGRIFTA SV after the expiration date (EXP) printed on the carton and vial labels.

• Dailymed label info on Tesamorelin
• FDA Tesamorelin

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