Tesamorelin

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

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

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

  1. 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.

  2. 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.

  3. 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.

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