EGRIFTA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EGRIFTA (EGRIFTA).

How it works

Tesamorelin is a synthetic analogue of human growth hormone-releasing hormone (GHRH) that stimulates the synthesis and release of endogenous growth hormone (GH) from the anterior pituitary. This leads to increased insulin-like growth factor-1 (IGF-1) production, which reduces visceral adipose tissue in HIV-infected patients with lipodystrophy.

What the body does with it

Metabolism	Metabolized by proteolytic degradation; not primarily dependent on CYP450 enzymes.
Excretion	Primarily metabolized in the body; less than 5% of the administered dose is excreted unchanged in urine. Biliary/fecal excretion is minimal.
Half-life	Terminal elimination half-life is approximately 6-8 hours in HIV patients with lipodystrophy. This supports once-daily dosing.
Protein binding	Highly protein-bound (>90%), primarily to albumin.
Volume of Distribution	Volume of distribution is approximately 0.5 L/kg, indicating distribution primarily into extracellular fluid and plasma.
Bioavailability	Subcutaneous: approximately 30-40% due to proteolysis at the injection site.
Onset of Action	Subcutaneous administration: improvement in visceral adipose tissue (VAT) reduction is typically observed after 2-4 weeks of daily therapy.
Duration of Action	The effect on VAT reduction persists for the duration of treatment. Upon discontinuation, VAT may return towards baseline over several months.

Classification & Brands

Dosing & administration

2 mg subcutaneously once daily at bedtime, to be administered by the patient or caregiver.

Dosage form	POWDER
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not recommended for severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease due to lack of data.
Liver impairment	No formal studies in hepatic impairment; use with caution in patients with Child-Pugh class B or C cirrhosis.
Pediatric use	Safety and efficacy not established; not recommended for use in pediatric patients.
Geriatric use	No specific geriatric dose adjustment; use with caution due to higher prevalence of renal impairment and cardiovascular disease.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EGRIFTA (EGRIFTA).

Breastfeeding	It is unknown whether tesamorelin is excreted in human milk. M/P ratio not available. Caution should be exercised when administered to a nursing woman. Consider risks of infant exposure versus benefits of breastfeeding.
Teratogenic Risk	EGRIFTA (tesamorelin) is a growth hormone-releasing hormone analog. There are no adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Based on mechanism, potential fetal risks include increased growth and metabolic effects. Use only if potential benefit justifies risk to fetus. Trimester-specific risks are unknown.

Warnings & precautions

■ FDA Black Box Warning

No black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to tesamorelin or any component","Active malignancy","Pediatric patients (safety not established)","Pregnancy (no adequate data; use if benefit outweighs risk)"]

Clinical Precautions

Precautions

["Malignancy: Risk of tumor growth due to GH/IGF-1 axis stimulation. Discontinue if malignancy develops.","Impaired glucose tolerance/Diabetes: Monitor blood glucose and HbA1c; may require adjustment of antidiabetic therapy.","Hypopituitarism: Not indicated for GH deficiency; may mask secondary hypogonadism or hypothyroidism.","Intracranial hypertension: Discontinue if papilledema or visual changes occur.","Hypersensitivity reactions: Angioedema, urticaria reported."]

Clinical Tips & Counseling

Drug interactions

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EGRIFTA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EGRIFTA (EGRIFTA).

How it works

What the body does with it

Metabolism	Metabolized by proteolytic degradation; not primarily dependent on CYP450 enzymes.
Excretion	Primarily metabolized in the body; less than 5% of the administered dose is excreted unchanged in urine. Biliary/fecal excretion is minimal.
Half-life	Terminal elimination half-life is approximately 6-8 hours in HIV patients with lipodystrophy. This supports once-daily dosing.
Protein binding	Highly protein-bound (>90%), primarily to albumin.
Volume of Distribution	Volume of distribution is approximately 0.5 L/kg, indicating distribution primarily into extracellular fluid and plasma.
Bioavailability	Subcutaneous: approximately 30-40% due to proteolysis at the injection site.
Onset of Action	Subcutaneous administration: improvement in visceral adipose tissue (VAT) reduction is typically observed after 2-4 weeks of daily therapy.
Duration of Action	The effect on VAT reduction persists for the duration of treatment. Upon discontinuation, VAT may return towards baseline over several months.

Classification & Brands

Dosing & administration

2 mg subcutaneously once daily at bedtime, to be administered by the patient or caregiver.

Dosage form	POWDER
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not recommended for severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease due to lack of data.
Liver impairment	No formal studies in hepatic impairment; use with caution in patients with Child-Pugh class B or C cirrhosis.
Pediatric use	Safety and efficacy not established; not recommended for use in pediatric patients.
Geriatric use	No specific geriatric dose adjustment; use with caution due to higher prevalence of renal impairment and cardiovascular disease.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EGRIFTA (EGRIFTA).

Breastfeeding	It is unknown whether tesamorelin is excreted in human milk. M/P ratio not available. Caution should be exercised when administered to a nursing woman. Consider risks of infant exposure versus benefits of breastfeeding.
Teratogenic Risk	EGRIFTA (tesamorelin) is a growth hormone-releasing hormone analog. There are no adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Based on mechanism, potential fetal risks include increased growth and metabolic effects. Use only if potential benefit justifies risk to fetus. Trimester-specific risks are unknown.

Warnings & precautions

■ FDA Black Box Warning

No black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to tesamorelin or any component","Active malignancy","Pediatric patients (safety not established)","Pregnancy (no adequate data; use if benefit outweighs risk)"]