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Oct 12

Sermorelin – an overview | ScienceDirect Topics

Sermorelin, Somatropin, and Mecasermin Lanreotide, Octreotide and Pegvisomant

Sermorelin, somatropin, and mecasermin are given for growth hormone deficiency syndromes, and lanreotide, octreotide, and pegvisomant are used to treat growth hormone excess.

Growth hormonereleasing hormone induces the anterior pituitary to secrete growth hormone (somatotropin). Growth hormone induces its own feedback inhibition by stimulating growth hormone inhibitory hormone (somatostatin) release from the hypothalamus (Fig. 12-6). Recombinant DNA versions of growth hormone (somatotropin) can be used to treat growth hormone deficiency (dwarfism). Several different recombinant products are available and differ from in terms of route of administration (intramuscular or subcutaneous) and frequency of injection (three to seven times per week). A growth hormonereleasing hormone biologic, sermorelin (consisting of the first 29 amino acids of growth hormonereleasing hormone), is available for patients who have a hypothalamic deficiency. In addition, an insulinlike growth factor therapy, mecasermin, has been approved for children who may not necessarily have a growth factor deficiency but may be resistant to the effects of growth hormone due to the production of neutralizing antibodies to growth hormone. Mecasermin is also used for children with severe insulinlike growth factor-1 deficiency. Mecasermin is administered subcutaneously before meals to avoid a hypoglycemic response. This is yet another example of how targeting a signal transduction cascade (insulinlike growth factor-1 tyrosine kinase receptors) yields a novel therapeutic strategy.

Figure 12-6. Growth hormone feedback inhibition. GHIH, growth hormone inhibitory hormone (somatostatin); GHRH, growth hormonereleasing hormone.

In contrast, synthetic forms of growth hormone inhibitory hormone (somastatin), such as lanreotide and octreotide, are effective for managing growth hormone excess (acromegaly or gigantism). Acromegaly is often the result of a benign pituitary tumor; pharmacologic treatment is often initiated because of inadequate responses to surgery and radiation. These biologics are 40 times more potent at inhibiting growth hormone secretion than is endogenous somatostatin. However, subcutaneously administered lanreotide and intramuscularly administered octreotide are associated with abdominal cramps, reduced gallbladder contractility, gallstones, reduced serum levels of vitamin B12, and altered absorption of dietary fats. A newer, more specific therapy uses a growth factor receptor antagonist such as pegvisomant to treat acromegaly. Injection site reactions, flulike symptoms, diarrhea, and elevated liver enzyme levels can occur. Hepatoxicity must therefore be closely monitored.

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Sermorelin - an overview | ScienceDirect Topics

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