Sermorelin: Mechanism of Action, Applications and Side Effects

Sermorelin is a synthetic analogue of growth hormone-releasing hormone (GHRH). Like CJC-1295 and temorelin, it is banned for use in sports due to its potential to enhance athletic performance. It contains the first 29 residues of natural GHRH (44 amino acids), which is the minimum necessary sequence for complete biological activity.

Mechanism of Action

Sermorelin binds to the GHRH binding site in the anterior pituitary gland of rats, specifically stimulating the anterior pituitary gland to secrete growth hormone via intravenous or subcutaneous injection. It is as effective as natural forms of GHRH (such as GHRH 1-40 and GHRH 1-44) in stimulating growth hormone release, with similar molar efficacy.

Applications

Sermorelin is a well-tolerated GHRH analogue. When administered as a single intravenous injection of 1 μg/kg body weight in conjunction with conventional detection methods, it can be used as a challenge test for growth hormone deficiency. Limited data suggest that once-daily subcutaneous injection of 30 μg/kg body weight of a growth hormone-releasing hormone analogue can effectively promote growth in some prepubertal children with idiopathic growth hormone deficiency. Furthermore, it responds well to children with slow growth, short stature, and delayed bone age and height development.

Side Effects

The most common adverse event following a single intravenous injection of Sermorelin is transient facial flushing. It occurs in approximately 30% of healthy children and approximately 20% of children with GHD, with the incidence increasing with age.

The most common adverse event following once-daily subcutaneous injection of Sermorelin is injection site reaction, such as pain, swelling, or redness. A minority of cases present with systemic reactions, including headache, flushing, dizziness, and hypothyroidism. Most children receiving long-term subcutaneous Sermorelin treatment develop anti-GHRH serum antibodies. Antibodies gradually appear after 3 months (20%), 6 months (54%), and 12 months (62%) of treatment. Antibody titers decrease sharply after discontinuation of treatment. However, the clinical significance of these antibodies remains uncertain.

References：

[1] A PRAKASH; K L G. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency.[J]. BioDrugs, 1999, 12 2: 139-157. DOI:10.2165/00063030-199912020-00007.

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