Where it comes from
- Made in
- The shared tail of the longer kisspeptins; unlike the 54, 14 and 13 it has not been isolated from tissue, and the peptide used in people is synthetic
- Sent out by
- With kisspeptin-54
- Acts on
- GnRH neurons
- Pituitary gonadotrophs, weakly
What it does
- Releases GnRH and so LH within minutes of an infusion starting
- The smallest fully active piece: the amidated RF-amide end is what the receptor reads 1
- Cleared in minutes, so it is infused rather than given as a single shot
In medicine
- Infused in research to probe the reproductive axis in delayed puberty, hypothalamic amenorrhoea and in men with type 2 diabetes and low testosterone
- In 16 children with delayed puberty, every child whose LH rose by 0.8 mIU/ml or more went through puberty, and every flat responder reached 18 without it 2
Beyond the body’s own use
- Put side by side with kisspeptin-54 and GnRH in healthy men, the two kisspeptins did much the same and GnRH was the stronger stimulus, so the short form is used where convenience matters 3
- Longer-acting analogues were built from its active end. Steady exposure shuts the axis down instead of switching it on: TAK-448 drove testosterone into the castration range in healthy men and in men with prostate cancer 4
- MVT-602, from the same work, is still being tested as an ovulation trigger. Neither analogue is approved, and kisspeptin-10 itself is a research tool
Sources
- Kotani et al., KiSS-1 encodes kisspeptins, the natural ligands of GPR54, Journal of Biological Chemistry 2001
- Chan et al., Using kisspeptin to predict pubertal outcomes for youth with pubertal delay, Journal of Clinical Endocrinology and Metabolism 2020
- Jayasena et al., Direct comparison of intravenous kisspeptin-10, kisspeptin-54 and GnRH in healthy men, Human Reproduction 2015
- MacLean et al., Sustained exposure to the kisspeptin analog TAK-448 in men, Journal of Clinical Endocrinology and Metabolism 2014
This card describes what a medicine is for and what the evidence says; it recommends nothing. Talk to your clinician about anything you read here.