Alpha-MSH
Animal / in-vitro onlyAlpha-melanocyte-stimulating hormone · melanotropin
The natural melanocortin hormone behind pigmentation, appetite regulation and anti-inflammatory melanocortin signalling. Its structure was solved in 1959 and it remains the reference point for the whole melanocortin drug class.
Ac-SYSMEHFRWGKPV-NH2
Endogenous hormone. Not marketed itself; approved medicines use analogues such as afamelanotide and bremelanotide.
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Oxytocin
Approved drugPitocin · Syntocinon
A posterior pituitary hormone driving uterine contraction and milk ejection, and studied extensively for central roles in bonding and social behaviour. Du Vigneaud's 1953 sequencing and synthesis won the Nobel Prize.
CYIQNCPLG-NH2 (Cys1-Cys6 disulfide)
FDA and EMA approved for labour induction and postpartum haemorrhage. Behavioural and psychiatric uses remain off-label and investigational.
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Vasopressin & desmopressin
Approved drugAVP · ADH · DDAVP
Vasopressin controls renal water reabsorption through V2 receptors and vascular tone through V1. Desmopressin is the long-acting, V2-selective analogue used clinically since the mid-1970s.
CYFQNCPRG-NH2 (AVP); deamino-Cys1/D-Arg8 analogue (desmopressin)
Both FDA and EMA approved: vasopressin for vasodilatory shock, desmopressin for central diabetes insipidus, nocturnal enuresis and some bleeding disorders.
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ACTH / cosyntropin
Approved drugCorticotropin · tetracosactide · Cortrosyn · Synacthen
The standard provocative agent for assessing adrenal reserve. Cosyntropin stimulates cortisol synthesis through MC2R and underpins the widely used ACTH stimulation test.
ACTH(1-24) synthetic fragment of the 39-residue hormone
FDA and EMA approved as a diagnostic agent for adrenal insufficiency testing.
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Gonadorelin
Approved drugGnRH · LHRH · gonadoliberin
The native hypothalamic decapeptide that drives pituitary LH and FSH release. Pulsatile delivery restores reproductive signalling; continuous exposure shuts it down, which is the basis of the whole GnRH-analogue drug class.
pyroGlu-HWSYGLRPG-NH2
Approved for diagnostic and fertility use (e.g. Lutrepulse). Manipulating the hormonal axis in sport falls under WADA scrutiny.
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Kisspeptin-10
Human trials (limited)Metastin(45-54) · KP-10
The active C-terminal fragment of kisspeptin, the upstream switch for GnRH release. Human infusion studies show reliable reproductive-hormone responses, and it is being tested as a fertility and diagnostic tool.
YNWNSFGLRF-NH2
Investigational only; not approved. Active academic trials in hypothalamic amenorrhoea and hypogonadism.
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Leuprolide
Approved drugLeuprorelin · Lupron
A GnRH superagonist that suppresses sex-steroid production after an initial surge, used in prostate cancer, endometriosis and central precocious puberty. Depot forms cover one to six months per injection.
pyroGlu-HWSY-(D-Leu)-LRP-NHEt
FDA-approved 1985 and EMA-approved. Restricted in sport as a hormone and metabolic modulator.
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Triptorelin
Approved drugDecapeptyl · Trelstar · Pamorelin
A long-established decapeptide with decades of randomised evidence across oncology, paediatric endocrinology and gynaecology. Included as a well-documented reference point for how a peptide hormone analogue is actually validated.
pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
FDA- and EMA-approved for prostate cancer, central precocious puberty and endometriosis. GnRH analogues generally require a therapeutic-use exemption in sport.
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Cetrorelix
Approved drugCetrotide · SB-075
Cetrorelix prevents premature luteinising hormone surges during IVF and is supported by multiple randomised trials in assisted reproduction. It is the clearest clinical example of GnRH antagonism as distinct from agonist downregulation.
Ac-D-Nal-D-Cpa-D-Pal-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2
FDA-approved in 2000 and EMA-approved in 1999 for controlled ovarian stimulation.
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Ganirelix
Approved drugOrgalutran · Antagon
Ganirelix has a long clinical track record in IVF, established by the European Orgalutran Study Group trials and confirmed in later randomised work in other populations.
Modified GnRH decapeptide antagonist (see FDA label for full residue structure)
FDA- and EMA-approved for controlled ovarian stimulation.
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Octreotide
Approved drugSandostatin
Beyond decades of symptomatic use in acromegaly and carcinoid syndrome, the placebo-controlled PROMID trial showed an antiproliferative effect in midgut neuroendocrine tumours. It also underpins the peptide-receptor radionuclide therapy field.
Cyclic D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr(ol)
FDA-approved in 1988 and EMA-approved; long-acting depot forms are widely used.
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Lanreotide
Approved drugSomatuline Depot · Somatuline Autogel
The CLARINET trial was a large placebo-controlled study showing prolonged progression-free survival in non-functioning enteropancreatic neuroendocrine tumours, establishing an antitumour rather than purely symptomatic role for somatostatin analogues.
Cyclic D-2Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2
FDA- and EMA-approved for acromegaly and gastroenteropancreatic neuroendocrine tumours.
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Pasireotide
Approved drugSignifor · SOM230
Phase 3 trials showed meaningful reductions in urinary free cortisol in Cushing's disease, a condition with few medical options. Hyperglycaemia is a frequent and clinically important adverse effect requiring monitoring.
Cyclic hexapeptide with non-natural residues; not expressible in one-letter code
FDA-approved in 2012 and EMA-approved for Cushing's disease, with a depot form for acromegaly.
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Goserelin
Approved drugZoladex
Randomised trials including EORTC 22863 showed improved survival when goserelin was added to radiotherapy in locally advanced prostate cancer, and it has a long track record across several hormone-sensitive conditions.
pGlu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH2
FDA- and EMA-approved for prostate cancer, breast cancer and endometriosis.
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Degarelix
Approved drugFirmagon
Phase 3 work showed faster castration than goserelin without a testosterone surge, which matters for patients at risk of spinal cord compression or urinary obstruction at the start of therapy.
Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(Hor)-D-4Aph(Cbm)-Leu-ILys-Pro-D-Ala-NH2
FDA-approved in 2008 and EMA-approved for advanced prostate cancer.
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