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Tesamorelin

Pronunciation: TES-a-moe-REL-in
Class: Growth hormone–releasing factor

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Trade Names

Egrifta
- Injection, lyophilized powder for solution 1 mg

Pharmacology

Acts on the pituitary somatotroph cells to stimulate the synthesis and pulsatile release of endogenous growth hormone.

Pharmacokinetics

Absorption

Absolute bioavailability is less than 4%. AUC and C _max are 634.6 pg•h/mL and 2,874.6 pg/mL, respectively, in healthy patients, and 852.8 pg•h/mL and 2,822.3 pg/mL, respectively, in HIV-infected patients. T _max is 0.15 h.

Distribution

Vd is 9.4 L/kg and 10.5 L/kg in healthy and HIV-infected patients, respectively.

Elimination

Mean elimination half-life is 26 and 39 min in healthy and HIV-infected patients, respectively.

Special Populations

Renal Function Impairment

Pharmacokinetics of tesamorelin have not been established.

Hepatic Function Impairment

Pharmacokinetics have not been established.

Elderly

Pharmacokinetics have not been established.

Children

Pharmacokinetics have not been established.

Indications and Usage

For the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy.

Contraindications

Active malignancy (either newly diagnosed or recurrent); disruption of the hypothalamic-pituitary axis due to head irradiation, head trauma, hypophysectomy, hypopituitarism, or pituitary tumor/surgery; known hypersensitivity to tesamorelin and/or mannitol; pregnancy.

Dosage and Administration

Lipodystrophy
Adults

2 mg subcutaneously once daily.

General Advice

For subcutaneous use in the abdomen only. Rotate injection sites. Do not inject into scar tissue, bruises, or the navel.
For reconstitution directions, refer to the manufacturer's patient instructions for use.
Inject immediately after reconstitution.
Only inject if the solution is clear, colorless, and without particulate matter.

Storage/Stability

Store unreconstituted vials between 36° and 46°F. Store the diluent, syringes, and needles between 68° and 77°F. Protect from light and keep in the original box until time of use. The reconstituted solution should be discarded if it is not used immediately. Do not freeze or refrigerate the reconstituted solution.

Drug Interactions

Ritonavir

In healthy subjects, coadministration of tesamorelin with ritonavir slightly decreased the ritonavir AUC and C _max . The changes are not likely to be clinically important.

Simvastatin

In healthy subjects, coadministration of tesamorelin with simvastatin slightly decreased the extent of simvastatin absorption and slightly increased the rate of absorption. For simvastatin acid, the extent of absorption and rate of absorption slightly decreased. The changes are not likely to be clinically important.

Adverse Reactions

Cardiovascular

Hypertension, palpitation (1%).

CNS

Paresthesia (5%); hypoesthesia (4%); depression, peripheral neuropathy (2%); insomnia (1%).

Dermatologic

Rash (4%); pruritus (2%); hot flush, night sweats, urticaria (1%).

GI

Nausea (4%); vomiting (3%); dyspepsia (2%); upper abdominal pain (1%).

Local

Injection-site reactions (25%); injection-site erythema (9%); injection-site pruritus (8%); injection-site pain (4%); injection-site irritation (3%); injection-site hemorrhage, swelling, urticaria (2%); injection-site rash (1%).

Musculoskeletal

Arthralgia (13%); myalgia, pain in the extremities (6%); carpal tunnel syndrome, joint stiffness, musculoskeletal pain, musculoskeletal stiffness (2%); joint swelling, muscle spasms, muscle strain (1%).

Miscellaneous

Peripheral edema (6%); elevated HbA _1c (5%); hypersensitivity reactions (4%); increased blood CPK, pain (2%); chest pain (1%).

Precautions

Monitor

Monitor efficacy as judged by the degree of reduction in visceral adipose tissue measured by waist circumference or CT scan. Monitor insulinlike growth factor 1 (IGF-1) levels closely. Evaluate glucose status prior to initiating therapy. Monitor patients periodically for changes in glucose metabolism. Monitor patients with diabetes at regular intervals for the development or worsening of diabetic retinopathy.

Pregnancy

Category X . May cause fetal harm. Contraindicated for use in pregnant women.

Lactation

Undetermined. The CDC recommends that HIV-infected mothers not breast-feed.

Children

Safety and efficacy have not been established.

Hypersensitivity

Erythema, flushing, pruritus, urticaria, and other hypersensitivity reactions may occur.

Acute critical illness

Increased mortality in patients with acute critical illness due to complications following abdominal surgery, multiple accidental trauma, or open heart surgery, or those with acute respiratory failure has been reported after treatment with pharmacologic amounts of growth hormone.

Elevated IGF-1

May occur.

Fluid retention

May occur, which is either transient or resolves with discontinuation of treatment.

Glucose intolerance

An increased risk of developing diabetes has been observed.

Immunogenicity

Development of antibodies may occur.

Injection-site reactions

Reactions, including bruising, erythema, irritation, pain, and pruritus, may occur.

Neoplasms

Any preexisting malignancy should be inactive and its treatment complete prior to instituting therapy with tesamorelin.

Overdosage

Symptoms

No data available.

Patient Information

Advise patients that treatment may cause symptoms consistent with fluid retention, including arthralgia, carpal tunnel syndrome, and edema.
Advise patients that hypersensitivity reactions (eg, rash, urticaria) may occur during treatment.
Advise patients of possible injection-site reactions, including bruising, erythema, irritation, pain, and pruritus. To reduce the incidence of injection-site reactions, advise patients to rotate the site of injection.
Counsel patients they should never share a syringe with another person, even if the needle is changed.
Advise women to discontinue tesamorelin if pregnancy occurs.
Instruct mothers receiving tesamorelin not to breast-feed.