A history of peptide science

184 milestones across 103 peptides and related compounds, from gland extracts to designed drugs. Select a name to read its full story.

Discovery era before 1950

The first hormones are found in crude gland extracts.

1. 1884

   Bivalirudin · Leech saliva anticoagulant discovered

2. 1895

   Vasopressin · Pressor effect of pituitary extract discovered

3. 1906

   NAD+ · Harden and Young discover “cozymase” in yeast

4. 1906

   Oxytocin · Uterus-contracting effect discovered

5. 1923

   Glucagon · Glucagon discovered

6. 1925

   Parathyroid hormone (PTH) · First active extract

7. 1928

   Oxytocin · Separated from vasopressin

8. 1929

   NAD+ · Nobel Prize to Harden and von Euler-Chelpin

9. 1931

   Substance P · Substance P discovered

10. 1937

    NAD+ · Niacin shown to cure pellagra

The chemistry era 1950–1979

Peptides are sequenced and synthesized; the brain’s hormones are found.

1. 1950s

   Bivalirudin · Hirudin isolated

2. 1950s

   Vasopressin · Sequenced and synthesized

3. 1953

   Oxytocin · Sequenced and synthesized

4. 1955

   Oxytocin · Nobel Prize to du Vigneaud

5. 1956

   Glucagon · Amino acid sequence determined

6. 1957

   KPV · α-MSH sequenced

7. 1962

   Calcitonin · Calcitonin discovered

8. 1964

   Calcitonin · Traced to the thyroid

9. 1966

   Thymosin beta-4 · Thymosin first described

10. 1967

    Desmopressin · Desmopressin synthesized

11. 1970s

    Parathyroid hormone (PTH) · Amino acid sequence determined

12. 1970

    Selank · Tuftsin discovered

13. 1970

    Tirzepatide · GIP discovered

14. 1970

    VIP · VIP isolated

15. 1970s

    VIP · Linked to VIP-secreting tumors

16. 1971

    Gonadorelin · Structure of GnRH reported by Schally’s team

17. 1971

    Substance P · Sequenced

18. 1973

    GHK-Cu · GHK identified in human plasma

19. 1973

    Octreotide · Somatostatin discovered

20. 1974

    Leuprolide · Leuprolide described

21. 1975

    Glucagon · “Bihormonal” theory of diabetes

22. 1977

    DSIP · DSIP isolated from sleeping rabbits

23. 1977

    Desmopressin · Use in bleeding disorders shown

24. 1977–80

    GHK-Cu · Its strong copper binding is described

25. 1977

    Gonadorelin · Nobel Prize to Schally and Guillemin

26. 1977

    Thymosin alpha-1 · Isolated and sequenced from thymosin fraction 5

27. 1978

    Desmopressin · Approved in the U.S.

28. 1978

    Gonadorelin · Pulsatile release shown to be essential

The molecular era 1980–1999

Genes, receptors and the first designed peptide drugs.

1. 1980s

   DSIP · Mixed results in human sleep studies

2. 1980s

   Epitalon · Pineal extract epithalamin studied

3. 1980s–90s

   KPV · Anti-inflammatory effects of α-MSH and its tail described

4. 1980s

   Melanotan II · Melanotan program begins in Arizona

5. 1980

   Neuropeptide Y · Related peptide YY discovered

6. 1980s–90s

   Neuropeptide Y · Role in appetite established

7. 1980s

   Semax · Developed in Moscow from an ACTH fragment

8. 1981

   LL-37 · Cecropins discovered in silk moths

9. 1981

   TB-500 · Thymosin beta-4 is isolated and sequenced

10. 1981

    Thymosin beta-4 · Thymosin beta-4 isolated and sequenced

11. 1982

    CJC-1295 · GHRH is discovered (see Sermorelin)

12. 1982

    Neuropeptide Y · Neuropeptide Y isolated

13. 1982

    Octreotide · Octreotide designed

14. 1982

    Sermorelin · GHRH isolated from pancreatic tumors

15. 1982

    Tesamorelin · Natural GHRH is discovered

16. 1984

    GHRP-2 · GHRP-6 published

17. 1984

    GHRP-6 · GHRP-6 published

18. 1985

    Leuprolide · Lupron approved for prostate cancer

19. 1987

    Amylin · Amylin identified from diabetic pancreatic amyloid

20. 1987

    Amylin · Amylin Pharmaceuticals founded

21. 1987

    Pramlintide · Amylin discovered

22. 1987

    Semaglutide · GLP-1 shown to stimulate insulin

23. 1988

    GHK-Cu · Shown to stimulate collagen synthesis in fibroblasts

24. 1988

    Octreotide · Sandostatin approved

25. 1989

    Leuprolide · Monthly depot approved

26. 1989

    PACAP-38 · PACAP isolated

27. 1990s

    AOD-9604 · Monash University develops the hGH 176–191 fragment

28. 1990

    Bivalirudin · Bivalirudin designed

29. 1990s

    Bremelanotide · Sexual effects of melanotan II observed

30. Late 1990s

    Epitalon · Synthetic epitalon developed

31. 1990s

    GHK-Cu · Copper peptides enter skincare

32. Early 1990s

    GHRP-2 · GHRP-2 developed

33. 1990s

    Oxytocin · Social bonding research

34. 1990s

    Selank · Selank developed in Moscow

35. 1990s–2000s

    Semax · Registered and used in Russia

36. 1990s

    Sermorelin · Sermorelin (Geref) approved in the U.S.

37. 1990s

    Thymosin alpha-1 · Approved outside the U.S. as Zadaxin

38. 1991

    Thymosin beta-4 · Shown to be the main actin-sequestering molecule in cells

39. 1992

    Exenatide · Exendin-4 isolated from Gila monster venom

40. 1993

    BPC-157 · First papers on BPC 157 from the Zagreb group

41. 1994

    Hexarelin · Hexarelin described

42. 1995

    Calcitonin · Nasal salmon calcitonin approved for osteoporosis

43. 1995

    LL-37 · Human cathelicidin gene identified

44. 1996

    Exenatide · Licensed to Amylin Pharmaceuticals

45. 1996

    GHRP-6 · Its receptor (GHS-R) cloned at Merck

46. 1996

    Kisspeptin-10 · KiSS-1 discovered as a melanoma metastasis suppressor

47. 1996

    LL-37 · LL-37 named and characterized

48. 1996

    Melanotan II · First human study of melanotan II

49. 1998

    Ipamorelin · Novo Nordisk publishes ipamorelin as a selective GH secretagogue

50. 1998

    Melanotan II · Erectile effects reported

51. 1999

    GHRP-6 · Ghrelin discovered as the natural hormone for the receptor

The drug-design era 2000–2014

Longer-lasting analogues and new classes of peptides.

1. 2000

   AOD-9604 · Early metabolic studies published

2. 2000s

   BPC-157 · Pliva tests it as PL 14736 for inflammatory bowel disease

3. 2000

   Bivalirudin · Angiomax approved

4. 2000

   Liraglutide · Liraglutide described

5. 2000

   NAD+ · Sirtuins shown to depend on NAD+

6. 2000s

   SS-31 (Elamipretide) · Szeto–Schiller peptides designed and tested

7. Late 2000s

   Selank · Registered in Russia for anxiety

8. 2000s

   TB-500 · TB-500 products appear in the horse-racing world

9. 2001

   Degarelix · Degarelix described

10. 2001

    Humanin · Humanin discovered

11. 2001

    Kisspeptin-10 · Kisspeptin peptides identified

12. 2001

    Leuprolide · $875 million TAP settlement

13. 2001

    MOTS-c · Humanin, the first mitochondrial peptide, is found

14. 2001

    SHLP2 · Humanin discovered

15. 2001

    Teriparatide · Pivotal fracture trial published

16. 2002

    Hexarelin · CD36 identified as a heart receptor for hexarelin

17. 2002

    Parathyroid hormone (PTH) · Teriparatide approved

18. 2002

    Teriparatide · FDA approves Forteo

19. 2003

    Epitalon · Telomerase activation reported in cell culture

20. 2003

    Humanin · Independent discoveries of its binding partners

21. 2003

    Kisspeptin-10 · Receptor mutations shown to block puberty

22. 2003

    Substance P · First receptor-blocking drug, aprepitant, approved

23. 2004

    NAD+ · Nicotinamide riboside identified as an NAD+ precursor

24. 2005

    Amylin · Pramlintide approved

25. 2005

    CJC-1295 · First animal studies of the albumin-binding GHRH analogue

26. 2005

    Exenatide · Byetta approved

27. 2005

    Kisspeptin-10 · First human studies

28. 2005

    Pramlintide · FDA approves Symlin

29. 2006

    CJC-1295 · Human study shows days-long rises in GH and IGF-1

30. 2006

    CJC-1295 · Phase 2 trial halted after a participant’s death

31. 2006

    LL-37 · Vitamin D shown to induce LL-37

32. 2007

    AOD-9604 · Phase 2b obesity trial fails; development stops

33. 2007

    Lanreotide · U.S. approval for acromegaly

34. 2007

    Tesamorelin · Phase 3 results in the New England Journal of Medicine

35. 2008

    ARA-290 / Cibinetide · EPO-derived protective peptides described

36. 2008

    Bremelanotide · Nasal version dropped

37. 2008

    Degarelix · Firmagon approved

38. 2008–2011

    Ipamorelin · Helsinn runs trials for postoperative ileus

39. 2008

    KPV · KPV shown to reduce colitis in mice via PepT1

40. 2008

    Sermorelin · Withdrawn from the U.S. market by the maker

41. 2009

    PACAP-38 · Shown to trigger migraine attacks

42. 2010s

    ARA-290 / Cibinetide · Trials in small-fiber neuropathy

43. 2010s

    BPC-157 · Spreads through online fitness and biohacking communities

44. 2010

    Liraglutide · Victoza approved

45. 2010s

    SS-31 (Elamipretide) · Stealth BioTherapeutics runs clinical trials

46. 2010

    Tesamorelin · FDA approves Egrifta for HIV-associated abdominal fat

47. 2010s

    Thymosin beta-4 · Eye-drop trials for dry eye and corneal damage

48. 2012

    Exenatide · Once-weekly Bydureon approved

49. 2012

    TB-500 · Essendon supplement program begins in Australian football

50. 2013

    AOD-9604 · Named in the Essendon doping investigation

51. 2014

    Dulaglutide · Trulicity approved

52. 2014

    Ipamorelin · Trial finds no significant benefit; development stops

53. 2014

    Lanreotide · CLARINET trial in neuroendocrine tumors

54. 2014

    Liraglutide · Saxenda approved for weight

55. 2014

    Vasopressin · Vasostrict approved for low blood pressure in shock

The modern era 2015–today

Mitochondrial peptides and the GLP-1 revolution.

1. 2015–16

   Humanin · Related mitochondrial peptides (MOTS-c, SHLPs) found

2. 2015

   MOTS-c · MOTS-c reported in Cell Metabolism

3. 2016

   Liraglutide · LEADER cardiovascular trial

4. 2016

   SHLP2 · SHLP1–6 described

5. 2016

   TB-500 · Court of Arbitration for Sport bans 34 Essendon players

6. 2017

   Semaglutide · FDA approves Ozempic

7. 2018 on

   Tesamorelin · Updated formulations approved

8. 2018

   Tirzepatide · Tirzepatide first described

9. 2019

   Bremelanotide · Vyleesi approved

10. 2019

    Dulaglutide · REWIND trial shows cardiovascular benefit

11. 2019

    Glucagon · Nasal glucagon approved

12. 2019

    Melanotan II · Related melanotan I approved as Scenesse

13. 2019

    Semaglutide · Oral Rybelsus approved

14. 2020s

    Amylin · Long-acting amylin analogues in trials

15. 2020s

    MOTS-c · Early human studies begin

16. 2020

    Octreotide · Oral octreotide approved

17. 2020s

    PACAP-38 · Anti-PACAP migraine drugs in trials

18. 2020

    Teriparatide · Boxed warning removed

19. 2020

    Thymosin alpha-1 · Used in China during COVID-19

20. 2021

    Semaglutide · Wegovy approved for weight management

21. 2022

    BPC-157 · WADA lists BPC-157 by name as a prohibited substance

22. 2022

    Retatrutide · First human (Phase 1) results

23. 2022

    Tirzepatide · FDA approves Mounjaro; SURMOUNT-1 results

24. 2023

    BPC-157 · FDA places it in Category 2 for compounding over safety concerns

25. 2023

    Retatrutide · Phase 2: 24% weight loss at 48 weeks

26. 2023

    Semaglutide · SELECT trial; Science Breakthrough of the Year

27. 2023

    Tirzepatide · Zepbound approved for weight management

28. 2024

    Liraglutide · Generic versions arrive

29. 2024

    Parathyroid hormone (PTH) · Yorvipath approved for hypoparathyroidism

30. 2024

    Semaglutide · Lasker Award for GLP-1 discovery

31. 2024

    Tirzepatide · Approved for obstructive sleep apnea

32. 2025

    SS-31 (Elamipretide) · FDA accelerated approval as Forzinity for Barth syndrome

33. 2025

    Semaglutide · Oral Wegovy pill approved

34. 2026

    BPC-157 · FDA allows 503A compounding under enforcement discretion

35. 2026

    Epitalon · FDA allows 503A compounding under enforcement discretion

36. 2026

    KPV · FDA allows 503A compounding under enforcement discretion

37. 2026

    MOTS-c · FDA allows 503A compounding under enforcement discretion

38. 2026

    Retatrutide · Phase 3 TRIUMPH-1: 28.3% weight loss at 80 weeks

39. 2026

    Semax · FDA allows 503A compounding under enforcement discretion

40. 2026

    TB-500 · FDA allows 503A compounding of TB-500 under enforcement discretion