What to Know About Egrifta (Tesamorelin)

Egrifta (tesamorelin) is an injectable, synthetic form of growth-hormone-releasing hormone (GHRH) approved by the Food and Drug Administration for the treatment of HIV-associated lipodystrophy.

This synthetic form of GHRH is more potent and stable than GHRH is in its natural state. When injected, Egrifta stimulates the production of growth hormone (GH), which binds to receptors on organs and tissues that regulate body composition.

In addition to having an anabolic (tissue- and muscle-building) effect, Egrifta is also lipolytic, meaning that it alters the pathways by which triglycerides are metabolized. It is this latter effect that is attributed to the improvement of lipodystrophy (abnormal body fat redistribution) in people with HIV.

Egrifta is the only drug specifically approved for the treatment of HIV-associated lipodystrophy. It is not indicated for weight loss management, and there are no generic versions of the drug.

Uses

Egrifta is approved for use in people with HIV who have excessive visceral fat due to lipodystrophy. Visceral fat is fat that resides in the abdominal cavity and around internal organs. Egrifta does not appear to have any effect on lipoatrophy (fat loss) of the face, buttock, or limbs, or in reducing accumulated fat in the breasts or the back of the neck.

HIV-associated lipodystrophy is characterized by the sometimes disfiguring redistribution of body fat. The condition commonly presents with a thinning of the face, buttocks, or extremities, while causing the accumulation of fat around the abdomen, breasts, or back of the neck (referred to as a "buffalo hump").

HIV-associated lipodystrophy has been linked to certain antiretroviral drugs, including protease inhibitors (PIs) like Crixivan (indinavir) and nucleoside reverse transcriptase (NRTIs) like Zerit (stavudine) and Videx (didanosine). The condition may also be a consequence of HIV itself, particularly in those who delayed antiretroviral therapy.

Though lipodystrophy is seen far less often with the introduction of newer antiretroviral drugs—and the retirement of older ones like Zerit and Crixivan—it remains a serious concern since the condition is rarely reversible once it occurs.

Before Taking

Prior to starting Egrifta, you will typically be given a computed tomography (CT) scan to assess the degree of visceral fat accumulation. This, along with a waistline circumference measurement, allows the healthcare provider to monitor your response to treatment.

Baseline blood tests will also be performed, including:

• Blood glucose test
• Complete blood count (CBC)
• Lipid panel
• Liver function tests (LFTs)

There is no established threshold by which Egrifta treatment is started. Expert consultation is needed to determine if other interventions, such as diet and exercise, are more appropriate or if the fat accumulation has occurred as a direct result of HIV infection or treatment.

Dosage

Egrifta comes in a single-use vial, each of which contains 1 milligram (mg) of tesamorelin in powdered form. It is reconstituted with sterile water from a separate 10-milliliter (mL) vial.

The recommended dosage of Egrift is 2 mg injected subcutaneously (beneath the skin) once daily.

It is recommended that Egrifta be injected into the abdomen just beneath the navel. Rotating the injection site helps reduce scarring and the formation of hardened nodules.

Duration of Treatment

Because the long-term effects of Egrifta are not fully known, the treatment should be monitored by an HIV specialist experienced in GHRH therapy, often in consultation with an endocrinologist.

To evaluate your response to treatment, comparative CT scans and waist circumference measurements would be performed. Blood glucose levels would also be monitored as Egrifta may cause glucose intolerance, increasing the risk of type 2 diabetes.

How to Take and Store

Non-reconstituted Egrifta must be stored in the refrigerator at temperatures between 36 and 46 degrees F (2 and 8 degrees C). The vials should be protected from light and be kept in their original box until the time of use. The syringes and needles used to inject Egrifta can be stored at room temperature between 68 and 77 degrees F (20 to 25 degrees C).  

Once reconstituted, Egrifta must be used immediately. It should be clear and free of floating particles. Do not inject Egrifta if it is discolored or has visible particles.

Discard the needle and syringe immediately after the injection. Never share needles or syringes.

Side Effects

Side effects of Egrifta tend to be mild and improve over time as your body adapts to treatment. With that said, there are a number of potentially serious complications that can occur with ongoing use. It is important to report any side effects to your healthcare provider immediately, particularly if they persist or worsen.

Common

The most common side effects, reported by at least 2% of Egrifta users, are (by order of frequency):

• Joint pain
• Injection site swelling
• Injection site itching
• Pain in the limbs
• Swelling of the limbs
• Muscle pain
• Injection site pain
• Injection site irritation

Joint stiffness, chest pain, muscle spasm, injection site rash, and joint swelling are less common side effects. Carpal tunnel syndrome has also been reported in some users.

Severe

One of the major concerns about the ongoing use of Egrifta is the effect it has on hormone levels and how this may stimulate the growth of hormone-sensitive cancers. Immunoreactive GHRH is present in several tumor types, including carcinoid tumors, pancreatic cell tumors, and small-cell lung cancers.

Although hypersensitive reactions have been known to occur with Egrifta, mainly in the form of a mild rash or hives, severe reactions like anaphylaxis are considered rare.

Warnings and Interactions

Caution should be exercised when using Egrifta in people with diabetes. The drug may increase insulin growth factor 1 (IGF-1) levels and contribute to the onset or worsening of diabetic retinopathy (retina damage).

Egrifta can also interact with certain drugs. With that said, the interaction appears to affect the accompanying drug more than Egrifta by lowering its blood concentration. Among some of the possible interactions are:

• Anticonvulsants like Tegretol (carbamazepine), Lamictal (lamotrigine), or Neurontin (gabapentin)
• Corticosteroids like hydrocortisone or prednisone
• Cyclosporine

In some cases, the reduced drug concentration will be of little consequence. In others, the accompanying drug dose may need to be increased to maintain its effectiveness.