Overview
11 DESCRIPTION Tesamorelin is a human growth hormone-releasing factor (GRF) analog produced synthetically. It is comprised of the 44 amino acid sequence of human GRF and a hexenoyl moiety, a C6 chain with a double bond at position 3, attached to the tyrosine residue at the N-terminal part of the molecule. Tesamorelin is prepared as an acetate salt.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action In vitro, tesamorelin binds and stimulates human GRF receptors with similar potency as the endogenous GRF [see Clinical Pharmacology ( 12.2 )]. Growth hormone-releasing factor (GHRF), also known as growth hormone-releasing hormone (GHRH), is a hypothalamic peptide that acts on the pituitary somatotroph cells to stimulate the synthesis and pulsatile release of endogenous growth hormone (GH), which is both anabolic and lipolytic. GH exerts its effects by interacting with specific receptors on a variety of target cells, including chondrocytes, osteoblasts, myocytes, hepatocytes, and adipocytes, resulting in a host of pharmacodynamic effects.
Indications
- 1 INDICATIONS AND USAGE EGRIFTA SV is indicated for the reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy. Limitations of Use: Long-term cardiovascular safety of EGRIFTA SV has not been established. Consider risk/benefit of continuation of treatment in patients who have not had a reduction in visceral adipose tissue. EGRIFTA SV is not indicated for weight loss management as it has a weight neutral effect. There are no data to support improved compliance with anti-retroviral therapies in HIV-positive patients taking EGRIFTA SV.
Common Doses
- 2 mg
- 1 mg
- 1.4 mg
- 0.35 mL
Dosage
2 DOSAGE AND ADMINISTRATION The recommendations in this prescribing information only apply to EGRIFTA SV (tesamorelin) for injection 2 mg per vial formulation. For recommendations for tesamorelin for injection 1 mg per vial formulation, see the EGRIFTA prescribing information. These two formulations and strengths have differences in the dosage, the number of vials required to prepare a dose, reconstitution instructions, and storage requirements. ( 2.1 ). The dose of EGRIFTA SV is 1.4 mg (0.35 mL of the reconstituted solution) injected subcutaneously once daily. ( 2.
Contraindications
- 4 CONTRAINDICATIONS EGRIFTA SV is contraindicated in: Patients with disruption of the hypothalamic-pituitary axis ( 4 ) Patients with active malignancy ( 4 ) Patients with known hypersensitivity to tesamorelin or excipients in EGRIFTA SV ( 4 ) Pregnancy ( 4 ) EGRIFTA SV is contraindicated in: Patients with disruption of the hypothalamic-pituitary axis due to hypophysectomy, hypopituitarism, pituitary tumor/surgery, head irradiation or head trauma. Patients with active malignancy.
Side Effects
- 6 ADVERSE REACTIONS The following important adverse reactions are also described elsewhere in the labeling: Increased risk of neoplasms [see Warnings and Precautions ( 5.1 )] Elevated IGF-1 levels [see Warnings and Precautions ( 5.2 )] Fluid retention [see Warnings and Precautions ( 5.3 )] Glucose intolerance or diabetes mellitus [see Warnings and Precautions ( 5.4 )] Hypersensitivity reactions [see Warnings and Precautions ( 5.5 )] Injection site reactions [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS Cytochrome P450-metabolized drugs : Monitor patients for potential interactions when administering with EGRIFTA SV . ( 7.1 ) Glucocorticoids : Patients receiving glucocorticoid replacement for previously diagnosed hypoadrenalism may require an increase in maintenance or stress doses following initiation of EGRIFTA SV. ( 7.2 ) 7.1 Cytochrome P450-Metabolized Drugs Co-administration of tesamorelin with simvastatin, a CYP3A substrate had no significant impact on the pharmacokinetics profiles of simvastatin in healthy subjects [see Clinical Pharmacology ( 12.3 )] .