Class: Somatotropin Agonists
Molecular Formula: C221H366N72O67S•C2H4O2
CAS Number: 901758-09-6
Uses for Tesamorelin Acetate
Reduction of excess abdominal fat in patients with HIV-associated lipodystrophy.1 2 3 4 6 9 17 Selectively reduces visceral adipose tissue, preserves subcutaneous fat, and improves body image.1 2 3 4 5 6 12 13
Long-term cardiovascular benefits and safety not known; carefully consider whether to continue the drug in patients who fail to achieve a substantial clinical response (based on degree of visceral adipose tissue reduction as measured by waist circumference or computed tomography [CT] scan).1 17 19
Tesamorelin Acetate Dosage and Administration
Restricted Distribution Program
Tesamorelin acetate is available in the US through a restricted distribution program.23 24 25 The drug can only be obtained through a targeted network of contracted pharmacies via the AXIS Center, a manufacturer-sponsored support service that facilitates access to therapy and provides reimbursement support and patient education.23 24 25 Contact AXIS at 877-714-2947or for further information.9 23 25
Administer sub-Q into the abdomen.1
Direct diluent toward sides of vials rather than directly onto powder to avoid foaming; roll each vial gently between the hands for 30 seconds to dissolve powder (do not shake).10
Combine reconstituted contents of both vials (total volume of approximately 2.2 mL) and administer immediately as a single sub-Q injection.10 Discard reconstituted vials if not used immediately; do not refrigerate or freeze.1
Available as tesamorelin acetate; dosage expressed in terms of tesamorelin.1
2 mg once daily.1
Data suggest that maintenance therapy is required to sustain the drug’s effects on visceral adipose tissue; optimal duration of therapy unknown.1 3 4 6 18 Safety and efficacy beyond 1 year not established.1 3 4
No special population dosage recommendations at this time.1
Cautions for Tesamorelin Acetate
Fetal/Neonatal Morbidity and Mortality
May cause fetal harm; fetal anomalies (i.e., hydrocephaly, delayed skull ossification) demonstrated in rats.1
Possible risk of malignancies; do not use in patients with active malignancy (newly diagnosed or recurrent).1 Confirm that any preexisting malignancy is inactive and its treatment completed prior to initiating therapy.1
Initiate therapy in patients with a history of treated and stable malignancies only after careful consideration of the potential benefits versus risks of reactivation of the underlying malignancy.1
Initiate therapy in patients with a history of nonmalignant neoplasms after carefully considering potential benefits of therapy.1
Consider increased background risk of malignancies in HIV-positive patients before initiating therapy.1
Increased Insulin-like Growth Factor I (IGF-I) Concentrations
Monitor IGF-I concentrations closely (e.g., every 3 months).1 11 Consider discontinuance of therapy in patients who experience persistent IGF-I elevations >3 standard deviations above mean value in a population of similar age and gender, particularly if a substantial response to therapy not achieved.1
Fluid retention (possibly related to excess growth hormone [GH] secretion) reported.1 Typically manifests as increased tissue turgor and musculoskeletal discomfort resulting in adverse effects such as edema, arthralgia, and carpal tunnel syndrome.1 2 3 4 5 6 Symptoms usually are transient and resolve with drug discontinuance.1
Evaluate glucose status carefully prior to initiating therapy and periodically thereafter.1 6 18 Exercise caution in patients who develop glucose intolerance or diabetes mellitus; consider discontinuance of therapy in such patients who fail to demonstrate a clear response to therapy.1
Monitor patients with diabetes mellitus at regular intervals for potential development or worsening of retinopathy.1
Injection Site Reactions
Rotate injection sites daily to reduce incidence of such reactions.1
Increased mortality reported in patients with acute critical illness resulting from complications following cardiac or abdominal surgery or multiple accidental trauma or from acute respiratory failure following pharmacologic dosages of GH.1 14
Consider discontinuance of therapy in patients with acute critical illness, since tesamorelin increases GH production.1
As with all therapeutic proteins, there is a potential for immunogenicity.1 Possible development of antibodies to tesamorelin acetate.1 Presence of anti-tesamorelin IgG antibodies does not appear to affect clinical response.1 3 4 6
Category X.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)
Visceral adipose tissue increases during pregnancy as a result of normal metabolic and hormonal changes; modification of this process offers no known clinical benefit and may result in fetal harm.1 17
Not known whether tesamorelin is distributed into milk.1
Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.1
Information not available in patients ≥65 years of age with HIV-associated lipodystrophy.1
Safety and efficacy not established in patients with hepatic impairment.1
Safety and efficacy not established in patients with renal impairment.1
Common Adverse Effects
Interactions for Tesamorelin Acetate
Drugs Metabolized by Hepatic Microsomal Enzymes
Drugs Metabolized by 11β-Hydroxysteroid Dehydrogenase Type 1
GH inhibits 11β-hydroxysteroid dehydrogenase type 1, the enzyme required for conversion of cortisone to cortisol; therefore, patients receiving glucocorticoid replacement therapy for hypoadrenalism may require increase in maintenance glucocorticoid dosage or supplemental stress-related glucocorticoid doses following initiation of tesamorelin.1
Anticonvulsants (e.g., carbamazepine, phenobarbital, phenytoin)
Corticosteroids (e.g., cortisone acetate, prednisone)
Glucocorticoids: Possible decreased concentrations of the active glucocorticoid metabolite1
Glucocorticoids: Increased stress or maintenance dosages of the glucocorticoid may be required1
Slight decreases in AUC and peak plasma concentrations of ritonavir1
Sex hormones (e.g., testosterone, estrogens [oral contraceptives])
Slight decrease in extent and slight increase in rate of simvastatin absorption1
Tesamorelin Acetate Pharmacokinetics
Absolute bioavailability <4% in healthy adults following sub-Q administration.1
Peak plasma concentrations achieved in approximately 0.15 hours.1
Not known whether tesamorelin is distributed into milk.1
No formal drug metabolism studies performed to date in humans.1
Adults with HIV: Approximately 38 minutes.1
Healthy individuals: Approximately 26 minutes.1
Powder for Injection
Store diluent and other supplies at 20–25°C.1
Synthetic analog of human GHRF; stimulates synthesis and release of GH from pituitary somatotroph cells.1 2 3 4 5 6 7 12 18 19 Also increases production of IGF-I by the liver and peripheral tissues.1 2 4 7 11
GH (deficient in patients with HIV-associated lipodystrophy) produces anabolic and lipolytic effects by interacting with specific receptors on target cells (e.g., chondrocytes, osteoblasts, myocytes, hepatocytes, adipocytes).1 4 7 13 20 Some of these effects are mediated by IGF-I.1
Does not substantially affect other pituitary hormones (i.e., thyroid-stimulating hormone [TSH], luteinizing hormone [LH], adrenocorticotropic hormone [ACTH], prolactin).1
Advice to Patients
Risk of hypersensitivity; importance of advising patients to immediately discontinue treatment and seek medical attention if a hypersensitivity reaction (e.g., rash, hives, swelling of the face or throat, breathing difficulties, fast heartbeat, feelings of faintness or fainting) occurs.1 9
Importance of women informing clinicians if they are, or plan to become, pregnant or plan to breast-feed.1 9 Risk of fetal harm if administered to pregnant women; if pregnancy occurs during therapy, discontinue drug immediately and apprise patient of potential harm to the fetus.1 9 Importance of advising women to discontinue nursing because of the potential for HIV transmission and serious adverse effects in nursing infants.1 9
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, dietary supplements, and/or herbal products, as well as any concomitant illness (e.g., cancer, diabetes).1 9
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
For injection, for subcutaneous use
1 mg (of tesamorelin)
Egrifta (available with sterile water for injection diluent, syringes, and needles)
AHFS DI Essentials. © Copyright 2017, Selected Revisions January 27, 2012. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. EMD Serono. Egrifta (tesamorelin for injection) prescribing information. Rockland, MA; 2010 Nov.
2. Falutz J, Allas S, Blot K et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007; 357:2359-70. [PubMed 18057338]
3. Falutz J, Allas S, Mamputu JC et al. Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation. AIDS. 2008; 22:1719-28. [PubMed 18690162]
4. Falutz J, Potvin D, Mamputu JC et al. Effects of tesamorelin, a growth hormone-releasing factor, in HIV-infected patients with abdominal fat accumulation: a randomized placebo-controlled trial with a safety extension. J Acquir Immune Defic Syndr. 2010; 53:311-22. [PubMed 20101189]
5. Falutz J, Allas S, Kotler D et al. A placebo-controlled, dose-ranging study of a growth hormone releasing factor in HIV-infected patients with abdominal fat accumulation. AIDS. 2005; 19:1279-87. [PubMed 16052083]
6. Falutz J, Mamputu JC, Potvin D et al. Effects of tesamorelin (TH9507), a growth hormone-releasing factor analog, in human immunodeficiency virus-infected patients with excess abdominal fat: a pooled analysis of two multicenter, double-blind placebo-controlled phase 3 trials with safety extension data. J Clin Endocrinol Metab. 2010; 95:4291-304. [PubMed 20554713]
7. Wang Y, Tomlinson B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin Investig Drugs. 2009; 18:303-10. [PubMed 19243281]
8. Grinspoon S, Carr A. Cardiovascular risk and body-fat abnormalities in HIV-infected adults. N Engl J Med. 2005; 352:48-62. [PubMed 15635112]
9. EMD Serono. Egrifta (tesamorelin for injection) patient information. Rockland, MA; 2010 Nov.
10. EMD Serono. Egrifta (tesamorelin for injection) patient instructions for use. Rockland, MA; 2010 Nov.
11. US Food and Drug Administration. Briefing document from the endocrinologic and metabolic drugs advisory committee. May 27, 2010. From FDA website .
12. Moyle G, Moutschen M, Martínez E et al. Epidemiology, assessment, and management of excess abdominal fat in persons with HIV infection. AIDS Rev. 2010 Jan-Mar; 12:3-14.
13. Koutkia P, Canavan B, Breu J et al. Growth hormone-releasing hormone in HIV-infected men with lipodystrophy: a randomized controlled trial. JAMA. 2004; 292:210-8. [PubMed 15249570]
14. Takala J, Ruokonen E, Webster NR et al. Increased mortality associated with growth hormone treatment in critically ill adults. N Engl J Med. 1999; 341:785-92. [PubMed 10477776]
15. Cheung NW, Liddle C, Coverdale S et al. Growth hormone treatment increases cytochrome P450-mediated antipyrine clearance in man. J Clin Endocrinol Metab. 1996; 81:1999-2001. [PubMed 8626872]
16. Malgarini RB, Pimpinella G. Effects of growth hormone-releasing factor in HIV-infected patients. N Engl J Med. 2008; 358:969; author reply 969-70.
17. US Food and Drug Administration. Center for Drug Evaluation and Research: Application number 22-505: Summary review for tesamorelin. From FDA website .
18. Leung VL, Glesby MJ. Pathogenesis and treatment of HIV lipohypertrophy. Curr Opin Infect Dis. 2011; 24:43-9. [PubMed 21124215]
19. Grunfeld C, Dritselis A, Kirkpatrick P. Tesamorelin. Nat Rev Drug Discov. 2011; 10:95-6. [PubMed 21283099]
20. EMD Serono, Rockland, MA: Personal communication.
21. Ferdinandi ES, Brazeau P, High K et al. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol. 2007; 100:49-58. [PubMed 17214611]
22. Michalets EL. Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy. 1998 Jan-Feb; 18:84-112.
23. EMD Serono. The AXIS Center. Available at: . Accessed 2011 Jun 17.
24. EMD Serono. Patient support with the AXIS center. Available at: . Accessed 2011 Jun 17.
25. Health Education Online, Inc. Tesamorelin (Egrifta) now available to manage HIV-related lipodystrophy. Available at: . Accessed 2011 Jun 20.
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Other brands: Egrifta