Tesamorelin is an analogue of GHRH (growth hormone releasing hormone, a naturally-occurring peptide released from the hypothalamus) that was recently approved by the FDA for treatment (reduction) of HIV-induced lipodystrophy-related visceral fat and is now marketed under the trade name Egrifta. Like GHRH, tesamorelin exerts its effects through inducing GH release from the pituitary.
Tesamorelin has a wide variability of pharmacokinetics among individuals. The recommended and best-studied dose is 2mg dosed weekly or daily. It has been demonstrated to have low oral bioavailability and is dosed subcutaneously.
Lipodystrophy is the medical term for a condition characterized by the abnormal condition of fat deposits, specifically lipoatrophy in most cases. In HIV-induced lipodostrophy sometimes normal fat deposits, such as those that give the face its shape, shrink and atrophy while others can grow and pose a risk to patient health. One such example of unhealthy fat deposits is visceral adipose tissue.
Visceral adipose tissue (VAT) refers to fat deposits that are located in the abdomen, but unlike subcutaneous (beneath the skin) deposits, are actually deeper and reside between organs. It is sometimes referred to as “intra-organ” fat. VAT is itself associated with a variety of negative effects:
Visceral fat (VF) accretion is a hallmark of aging in humans. Epidemiologic studies have implicated abdominal obesity as a major risk factor for insulin resistance, type 2 diabetes, cardiovascular disease, metabolic syndrome and death.
The purpose of the study by Huffman and Barzilai, cited above, was to zero in on the link between VF and mortality. The limitations of epidemiological studies makes it difficult to determine causality. They found that “Specific depletion or expansion of the VF depot using genetic or surgical tools in rodents has been shown to have direct effects on disease risk” while the same was not true of SC fat deposits.
In a medium-scale (400 patient) randomized clinical trial where patients were randomly selected to receive 2mg subcutaneous tesamorelin for 52 weeks, placebo for 52 weeks, or 26 weeks of each, tesamorelin reduced visceral adipose tissue by 18% and triglyceride scores improved. The incidence of adverse effects and serious adverse effects were low. Glucose tolerance was not negatively affected. When GH is used for medium or long periods of time, fasted glucose levels and insulin sensitivity are negatively affected[4,5].
Tesamorelin and other GH secretagogues may be of use in treating excess visceral adipose tissue in otherwise-healthy subjects, as was the focus of a study by Stanley, Chen, et al: “Strategies to augment pulsatile GH may be beneficial in patients with excess visceral adiposity, in whom GH secretion is reduced”. Primary endpoint was overnight GH release as determined by frequent sampling, and secondary endpoints were insulin sensitivity as determined by insulin-stimulated glucose uptake, and GH secretion measures including pulse area and pulse frequency compared to basal secretion. The trial lasted 2 weeks and dosing was 2mg subcutaneously once weekly. The GH parameters were found to increase versus basal secretion, and insulin sensitivity was preserved.
Tesamorelin is made with growth hormone-releasing factor (GRF).
Tesamorelin is used to reduce excess fat around the stomach that is caused by taking certain HIV medications. This condition is also called lipodystrophy (LYE-poe-DIS-troe-fee).
Tesamorelin is not a weight-loss medication and should not be used to treat obesity.
Tesamorelin can harm an unborn baby or cause birth defects. Do not use if you are pregnant.
You should not use tesamorelin if you are allergic to it, or if you have a history of tumor or surgery of your pituitary gland, a history of head injury or radiation treatment,
Before using tesamorelin, tell your doctor if you have heart disease, high blood pressure, kidney disease, diabetes, epilepsy, asthma, migraines, an adrenal gland disorder, or if you have ever had cancer, any type of tumor, or open heart surgery.
Also tell your doctor about any major illness or recent trauma or medical emergency.
You should not use tesamorelin if you are allergic to it, or if you have:
- a pituitary gland disorder;
- a history of pituitary gland tumor or surgery;
- a history of head injury or radiation treatment; or
- if you are pregnant.
To make sure you can safely take tesamorelin, tell your doctor if you have any of these other conditions:
- a history of cancer or any tumor (either benign or malignant);
- heart disease, high blood pressure;
- kidney disease;
- diabetes, eye problems caused by diabetes;
- migraine headaches;
- adrenal gland disorder;
- if you have ever had open heart surgery; or
- if you have any major illness, or a recent trauma or medical emergency.
FDA pregnancy category X. This medication can harm an unborn baby or cause birth defects. Do not use tesamorelin if you are pregnant. Tell your doctor right away if you become pregnant during treatment.
Women with HIV or AIDS should not breast feed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.
Do not give this medicine to a child without medical advice.
Tesamorelin Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Stop using tesamorelin and call your doctor at once if you have a serious side effect such as:
- swelling in your hands, ankles, or feet;
- pain or stiffness in your muscles or joints;
- pain in your arms or legs;
- wrist pain or numbness;
- numbness or tingling in your hands or fingers;
- pounding heartbeats or fluttering in your chest;
- high blood sugar (increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss);
Less serious side effects may include:
- depressed mood, sleep problems (insomnia);
- night sweats;
- mild rash or itching;
- muscle spasm;
- nausea, vomiting, upset stomach;
- pain, redness, itching, swelling, bruising, bleeding, or other irritation where the injection was given;
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Do not inject this medicine into scar tissue or on skin that is bruised. Do not inject directly into your navel (belly-button).
Tell your doctor about all other medicines you use, especially:
- testosterone or hormone replacement therapy;
- seizure medication;
This list is not complete and there are many other drugs that can interact with tesamorelin. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.
Tesamorelin is injected under the skin. You may be shown how to use injections at home. Do not self inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.
This medication comes with injection instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.
Tesamorelin is a powder medicine that must be mixed with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medicine.
Prepare your dose in a syringe only when you are ready to give yourself an injection. Do not use the medication if it has changed colors or has particles in it. Call your doctor for a new prescription.
After mixing tesamorelin with a diluent, you must use it right away. Do not store the mixture for later use.
Tesamorelin is usually given once per day. Follow your doctor’s dosing instructions very carefully.
Use a different place on your stomach each time you give the injection. Your care provider will show you the best places on your body to inject the medication. Do not inject into the same place two times in a row.
Never share a tesamorelin syringe with another person, even if you change the needle. Sharing syringes or needles can allow HIV or other diseases to pass from one person to another.
To make sure this medication is helping your condition and not causing harmful effects, your blood will need to be tested often. Do not miss any follow-up visits to your doctor.
Store vials of tesamorelin powder in the refrigerator, do not freeze.
Store the diluent at room temperature away from moisture, heat, and light.
Throw away any unused vials after the expiration date on the label has passed.
Tesamorelin, (formerly known as TH9507), is a type of peptide called a growth hormone-releasing factor (GHRF). GHRF causes growth hormone to be created and spread in the body, which helps increase metabolism, reduce belly fat, improve body shape, and use of energy. Tesamorelin (formerly known as TH9507) is a synthetic growth hormone-releasing factor that stimulates the pituitary gland in the brain to secrete growth hormone; this indirect approach appears to maintain more stable, natural levels, like CJC-1295 DAC,. Clinical trials have shown that tesamorelin significantly reduces abdominal fat with fewer side effects than human growth hormone itself, although abdominal fat may return after the Tesamorlein is discontinued (depending upon the individual). Tesamorelin has been shown to reduce lipodystrophy in HIV-infected individuals as well as similarly reducing abdominal fat in NON-HIV-Infected individuals.