Tesamorelin
- CAS Codes:901758-09-6
- PHARMGKB ID:901758-09-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Egrifta.
Drug combinations
Chemistry
Tesamorelin Acetate: C~221~H~366~N~72~O~67~S xC~2~H~4~O~2~ (x~7.4). Mw: 5579. (3E)-Hex-3-enoylsomatoliberin (human) acetate. The peptide precursor of tesamorelin acetate is produced synthetically and is comprised of the 44 aa sequence of human GRF. Tesamorelin acetate is made by attaching a hexenoyl moiety, a C6 chain with a double bond at position 3, to the tyrosine residue at the N-terminal part of the molecule. CAS-901758-09-6.
Pharmacologic Category
Hormones and Synthetic Substitutes; Somatotropin Agonists. Growth Hormone Releasing Factor (GRF) Analog.
Mechanism of action
In vitro, tesamorelin binds and stimulates human GRF receptors with similar potency to endogenous GRF. GRF, 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. Some, but not all these effects, are primarily mediated by IGF-I produced in the liver and in peripheral tissues.
Therapeutic use
Indicated for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Limitations of use: long-term cardiovascular benefit and safety have not been studied; not indicated for weight loss management (weight neutral effect) and there are no data to support improved compliance with anti-retroviral therapies in HIV-positive patients taking tesamorelin.
Pregnancy and lactiation implications
Contraindicated in pregnant women. HIV-l infected mothers should not breast-feed in order to avoid potential postnatal transmission of HIV-1.
Unlabeled use
Contraindications
Disruption of the hypothalamic-pituitary axis due to hypophysectomy, hypopituitarism or pituitary tumor/surgery, head irradiation or head trauma, active malignancy, known hypersensitivity to tesamorelin and/or mannitol and pregnancy.
Warnings and precautions
Since tesamorrelin is a growth factor analog, any pre-existing malignancy should be inactive and its treatment complete prior to starting therapy. Estimulates GH production and increases serum IGF-I (monitor regularly in all patients; consider discontinuation in patients with persistent elevations). May produce fluid retention (include edema, arthralgia, and carpal tunnel syndrome), glucose intolerance (evaluate glucose status prior to and during therapy), hypersensitivity reactions (e.g. rash, urticaria; in cases of suspected hypersensitivity reactions, should be discontinued immediately), injection site reactions (advise patients to rotate sites) and acute critical illness (consider discontinuation). Since increases IGF-I, patients with diabetes who are receiving ongoing treatment should be monitored at regular intervals for potential development or worsening of retinopathy. As with all therapeutic proteins and peptides, there is a potential for in vivo development of anti-tesamorelin antibodies (cross-reactivity to endogenous GHRH was observed in patients who developed anti-tesamorelin antibodies; clinical studies suggest that the presence of antibodies did not alter the efficacy of treatment).