GHRH analogues and GH secretagogues

Growth-hormone-releasing hormone analogues and ghrelin-receptor secretagogues.

Two separate pharmacological classes are collected here, and the distinction between them is the most useful thing to carry into the entries.

The first class acts at the growth hormone-releasing hormone receptor: sermorelin, tesamorelin and the two forms of CJC-1295. These are fragments or analogues of a human hormone, and the differences between them are almost entirely about resistance to enzymatic cleavage and about how long the molecule persists in plasma.

The second class acts at the growth hormone secretagogue receptor, the ghrelin receptor: GHRP-6, GHRP-2 and ipamorelin. These are synthetic peptides with no sequence relationship to the natural ligand of that receptor, and their history runs backwards from the usual one — the compounds came first, the receptor second, the hormone third. That story is set out in growth hormone secretagogue receptor research.

Comparisons across and within the two classes: ipamorelin against sermorelin, tesamorelin against sermorelin, GHRP-2 against GHRP-6 and CJC-1295 DAC against CJC-1295 No DAC.

Compounds listed below without a link do not yet have a published entry.

Compounds in this category

8 of 8 entries are published. Compounds without a published entry are listed without a link.

  • CJC-1295 DACCJC-1295 DAC is a synthetic 30-residue analogue of human growth hormone-releasing hormone carrying a maleimidopropionamide group that bonds covalently to serum albumin, giving it a plasma half-life measured in days. It is not approved by the FDA for any indication; clinical development reached phase 2 and stopped.
  • CJC-1295 No DACCJC-1295 no DAC, also listed as modified GRF (1-29), is a synthetic 29-residue analogue of human growth hormone-releasing hormone carrying four amino acid substitutions. It is not approved by the FDA for any indication, and no clinical trial of it has been published under this name.
  • IpamorelinIpamorelin is a synthetic pentapeptide agonist at the growth hormone secretagogue receptor, described in its discovery paper as the first selective growth hormone secretagogue because it released growth hormone in swine without measurable release of ACTH or cortisol. It is not approved by the FDA for any indication.
  • TesamorelinTesamorelin is a synthetic 44-residue analogue of human growth hormone-releasing hormone with a hexenoyl group on its N-terminal tyrosine. It is the one compound in this family with a current United States approval, held by a specific pharmaceutical product in a single HIV-related indication.
  • SermorelinSermorelin is the first 29 amino acids of human growth hormone-releasing hormone, synthesised as a C-terminal amide. It is the shortest fragment of that hormone with full biological activity, and it was formerly approved in the United States as a pharmaceutical product; that product is no longer marketed.
  • GHRP-2GHRP-2, whose international non-proprietary name is pralmorelin, is a synthetic hexapeptide agonist at the growth hormone secretagogue receptor. It is approved in Japan as a diagnostic agent for provocative testing of growth hormone secretion, and is not approved in the United States for any use.
  • GHRP-6GHRP-6 is a synthetic hexapeptide first described in 1984 and the founding member of the growth hormone-releasing peptide family. It is an agonist at the growth hormone secretagogue receptor, the receptor for ghrelin, and it is not approved by the FDA for any indication.
  • HexarelinHexarelin, also named examorelin, is a synthetic six-residue peptide that activates the growth hormone secretagogue receptor GHS-R1a and also binds the scavenger receptor CD36. It was studied in human clinical pharmacology through the 1990s, chiefly as a probe of pituitary growth hormone reserve, and it is not approved by the FDA for any indication.

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