INDICATIONS
FDA
Reduction of excess abdominal fat secondary to lipodystrophy in HIV-infected pts.
FORMS
brand
preparation
manufacturer
route
form
dosage^
cost*
Egrifta
Tesamorelin
Theratechnologies, Inc
SQ
vial
1 mg
$77.50
2 mg
$99.70
*Costs (rounded to the nearest dollar) are based on usual adult dosing per day, are representative of "Average Wholesale Price" (AWP), and are current within the prior three months.
^Dosage is indicated in mg unless otherwise noted.
USUAL ADULT DOSING
2 mg SQ once daily
RENAL DOSING
DOSING FOR GLOMERULAR FILTRATION OF 50-80
No data; usual dose likely
DOSING FOR GLOMERULAR FILTRATION OF 10-50
No data; usual dose likely
DOSING FOR GLOMERULAR FILTRATION OF <10 ML/MIN
No data; usual dose likely
DOSING IN HEMODIALYSIS
No data
DOSING IN PERITONEAL DIALYSIS
No data
DOSING IN HEMOFILTRATION
No data
ADVERSE DRUG REACTIONS
GENERAL
Discontinuations due to adverse reactions occurred in 9.6% treated with tesamorelin (vs. 6.8% with placebo).
COMMON
Arthralgia (13%) and myalgia (6%) Injection site erythema and pruritis (8-9%) Pain in extremity (6 %) Peripheral edema (6.1% vs. 2.3% in placebo)
OCCASIONAL
Paresthesia (4.8% vs 2.3% in placebo) Musculoskeletal pain and stiffness (2%) Carpal tunnel syndrome (1.5%) Nausea and Vomiting (3-4%) Pruritis and rash (3-4%) Hyperglycemia (4.5%)
RARE
Hypertension CK elevation
DRUG INTERACTIONS
Glucocorticoid: higher glucocorticoid dose may be needed with tesamorelin co-administration.
PHARMACOLOGY
MECHANISM
Tesamoralin, a synthetic analog of human hypothalamic growth hormone-releasing factor (hGRF), acts on the pituitary cells to stimulate synthesis and release of endogenous growth hormone.
PHARMACOKINETIC PARAMETERS
Absorption
< 4%
Metabolism and Excretion
no data
Cmax, Cmin, and AUC
AUC= 852.8 (CV 91.9) pg.h/mL
T1/2
38 minutes
Distribution
Vd= 10.5 L/kg
DOSING FOR DECREASED HEPATIC FUNCTION
No data
PREGNANCY RISK
Category X: contraindicated
BREAST FEEDING COMPATIBILITY
Not recommended
COMMENTS
Tesamorelin decreases abdominal fat by a modest 14-18% and significantly reduces triglycerides and non-HDL cholesterol in HIV+ pts with lipodystrophy.[3][2] White patients and those with metabolic syndrome and triglycerides >150 mg/dL are more likely to respond.[1] Musculoskeletal adverse effects, local injection site reactions, and cost may prevent routine use of tesamorelin. Benefits tend to reverse with discontinuation of drug. With currently used ARV regimens, most weight gain is due to increased subcutaneous fat rather than visceral fat accumulation.
References
Mangili A, Falutz J, Mamputu JC, et al. Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat. PLoS One. 2015;10(10):e0140358. [PMID:26457580]
Comment: Patients with metabolic syndrome and triglyceride levels >1.7 mmol/L at baseline and those of white race were more likely to respond to tesamorelin therapy at 6 months. Stanley TL, Falutz J, Marsolais C, et al. Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving tesamorelin. Clin Infect Dis. 2012;54(11):1642-51. [PMID:22495074]
Comment: Patients that responded to tesamorelin (defined as at least 8% reduction in visceral adipose tissue) in 2 phase III RCTs experienced significantly greater reductions in triglycerides levels and parameters of glucose homeostasis (hemoglobin A1c, fasting blood glucose) over 52 weeks compared to those nonresponding to tesamorelin. 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(9):4291-304. [PMID:20554713]
Comment: RCT of 806 treatment-experienced HIV-positive patients with excessive abdominal fat randomized to receive tesamorelin 2 mg daily or placebo for 26 or 52 weeks. Visceral adipose tissue decreased significantly (15% decrease) in tesamorelin treated patients at 26 weeks. Treatment also resulted in significant reductions in triglycerides levels and cholesterol to HDL ratio.
Last updated: September 3, 2016