FDA-approved peptide drugs: a list by INN, approval year, target and length

Peptide drugs sit between small molecules and biologics: large enough to bind receptors with high selectivity, small enough to make by chemical synthesis. They include some of the oldest medicines in the US database and some of the newest. This page lists FDA-approved peptide drugs by International Nonproprietary Name (INN), with the year of the earliest original approval recorded in Drugs@FDA, the target or class, and the chain length, and then looks at the trends behind recent approvals.

Two rules apply throughout. Counts are given only as the cited sources state them; the table is a curated list, not an official census. And the data cut-off is 26 October 2026, with FDA’s 2026 novel approvals page current to 20 October 2026 [1]. Brand names are not used; molecules are identified by INN.

What counts as a peptide drug?

There is no single regulatory definition of “peptide drug”, but there is a regulatory definition of a protein. Under 21 CFR 600.3, “a protein is any alpha amino acid polymer with a specific, defined sequence that is greater than 40 amino acids in size”; for chains that associate as they do in nature, the count is the total across the chains [2]. Molecules of 40 amino acids or fewer therefore fall outside the protein definition and are generally developed as drugs under new drug applications.

Consequences are visible in Drugs@FDA. Lixisenatide and tesamorelin, both 44-residue peptides, are now listed under BLA application numbers [3] [4] [5]. Insulin, with a 30-residue B chain and a 21-residue A chain [6], is a protein under this rule because the chains are counted together, even though reviews count it as the first peptide therapeutic [7] [2]. In 2026, the 47-amino-acid lipopeptide bulevirtide was approved under a biologics licence [3] [1].

Literature reviews use broader definitions. The annual FDA TIDES reviews define peptide-based drugs as “compounds that carry at least two amino acids in their structure, that are synthesized mainly by chemical methods, and whose purity has been assessed by analytical methods” [8]. Under that definition, imaging agents and radioligands built on short peptides count as peptides. The background chemistry is covered in what is a peptide API.

How many FDA-approved peptide drugs are there?

The sources give different counts because they use different scopes:

Source	Scope	Count as stated	Ref
Muttenthaler et al., 2021	Worldwide, since insulin	”more than 80 peptide drugs have reached the market”	[7]
Wang et al., 2022	Worldwide	”more than 80 peptide drugs worldwide”; “more than 170 peptides are in active clinical development”	[9]
TIDES review, 2020 approvals	FDA, peptides and oligonucleotides	Six TIDES among 53 approvals in 2020; 23 TIDES in 2016 to 2020	[10]
TIDES review, 2021 approvals	FDA	Eight peptides, two oligonucleotides and two ADCs with peptide fragments, “the best TIDES harvest to date”	[11]
TIDES review, 2022 approvals	FDA	TIDES were 14% of 37 new drug entities	[8]
TIDES review, 2023 approvals	FDA	Five peptides and four oligonucleotides	[12]
TIDES review, 2024 approvals	FDA	Two peptides and two oligonucleotides among 50 novel drugs	[13]
TIDES review, 2025 approvals	FDA	One peptide, three oligonucleotides and one ADC with a peptide payload, among 46 novel drugs	[14]

None of these sources gives a current total for FDA alone, so this page does not claim one. The tables below list 55 approved peptides that we verified individually in Drugs@FDA, with lengths taken from FDA labels or KEGG.

List of FDA-approved peptide drugs by INN

How to read the table. “First FDA approval” is the year of the earliest original application approval recorded in Drugs@FDA for that active ingredient, retrieved through openFDA on 26 October 2026 [3]; for long-established molecules this can postdate first clinical use. Length is the number of amino acid residues as stated in the FDA label [4] or counted from the KEGG sequence [5]. Targets come from the label mechanism-of-action section or the KEGG target field [4] [5]. Marketing status is not tracked; some products have since been discontinued.

Pituitary, hypothalamic and reproductive hormone analogues

INN	First FDA approval	Target / class	Length (residues)	Notes
Glucagon	1960 [3]	Glucagon receptor; antihypoglycaemic [4]	29 [5]	Earliest record in this list
Desmopressin	1978 [3]	Vasopressin V2 receptor agonist [4]	9 [4]	1-(3-mercaptopropionic acid)-8-D-arginine vasopressin [4]
Calcitonin salmon	1978 [3]	Calcitonin analogue [4]	32 [4]
Oxytocin	1980 [3]	Oxytocin receptor agonist [5]	9, disulfide 1-6 [5]	Earliest Drugs@FDA record shown; see note above
Leuprolide	1985 [3]	GnRH receptor agonist [4]	9 [4]	Nonapeptide [4]
Octreotide	1988 [3]	Somatostatin receptor agonist [4]	8, cyclic [4]	Oral delayed-release capsule approved 2020 [3]
Goserelin	1989 [3]	GnRH analogue, inhibits gonadotropin secretion [4]	10 [4]
Ganirelix	1999 [3]	GnRH receptor antagonist [4]	10 [4]
Triptorelin	2000 [3]	GnRH receptor agonist [4]	10 [4]
Cetrorelix	2000 [3]	GnRH receptor antagonist [4]	10 [4]
Teriparatide	2002 [3]	Parathyroid hormone analogue, PTH(1-34) [4] [5]	34 [5]
Lanreotide	2007 [3]	Somatostatin analogue [4]	8, cyclic [4]
Degarelix	2008 [3]	GnRH receptor antagonist [4]	10 [4]	Seven unnatural amino acids, five D-amino acids [4]
Tesamorelin	2010 [3]	GHRH (GRF) receptor [4]	44 plus hexenoyl group [4]	Above 40 residues; listed with a BLA number [3]
Pasireotide	2012 [3]	Somatostatin receptor agonist [4]	6, cyclic [4]	Cyclohexapeptide [4]
Vasopressin	2014 [3]	V1 and V2 receptors [4]	9, cyclic 1-6 [4]	First NDA record in Drugs@FDA; see note above
Abaloparatide	2017 [3]	PTH-related peptide analogue [4]	34 [5]
Palopegteriparatide	2024 [3]	Releases PTH(1-34) [4]	34 (peptide moiety) [4]	PEGylated prodrug

Metabolic and gastrointestinal peptides

INN	First FDA approval	Target / class	Length (residues)	Notes
Exenatide	2005 [3]	GLP-1 receptor agonist [4]	39 [5]
Pramlintide	2005 [3]	Amylin analogue [4]	37 [5]
Liraglutide	2010 [3]	GLP-1 receptor agonist [4]	31 [5]	Fatty-acid acylated
Linaclotide	2012 [3]	Guanylate cyclase-C agonist [5]	14, three disulfides [4]	Oral
Teduglutide	2012 [3]	GLP-2 analogue [4]	33 [5]
Lixisenatide	2016 [3]	GLP-1 receptor agonist [4]	44 [5]	Above 40 residues; listed with a BLA number [3]
Plecanatide	2017 [3]	Guanylate cyclase-C agonist [4]	16 [5]	Oral
Semaglutide	2017 [3]	GLP-1 receptor agonist [4]	31 [5]	Oral tablet approved 2019 [3]
Setmelanotide	2020 [3]	MC4 receptor agonist [4]	8, cyclic [4]
Dasiglucagon	2021 [3]	Glucagon receptor agonist [4]	29 [5]
Tirzepatide	2022 [3]	GIP and GLP-1 receptor agonist [4]	39 [5]	Fatty-acid acylated
Enlicitide decanoate	2026 [3]	PCSK9 inhibitor [5]	Macrocyclic peptide [15]	Oral tablet [3]

Cardiovascular, haematology and bone growth

INN	First FDA approval	Target / class	Length (residues)	Notes
Eptifibatide	1998 [3]	GP IIb/IIIa; platelet aggregation inhibitor [4]	7, cyclic (6 amino acids plus mercaptopropionyl) [4]	Made by solution-phase synthesis [4]
Bivalirudin	2000 [3]	Direct thrombin inhibitor [4]	20 [5]
Nesiritide	2001 [3]	Natriuretic peptide receptor A agonist [5]	32, disulfide 10-26 [5]
Vosoritide	2021 [3]	Natriuretic peptide receptor B [4]	39, disulfide 23-39 [5]
Navepegritide	2026 [3]	Releases CNP; NPR-B [4]	38 (CNP moiety) [4]	PEGylated prodrug
Rusfertide	2026 [3]	Hepcidin mimetic; blocks ferroportin [4]	17, cyclic disulfide, palmitoylated [4] [5]
Lutetium Lu 177 dotatate	2018 [3]	Somatostatin receptor (SSTR2) radioligand [4]	8, cyclic, with DOTA chelator [4]

Immunology, complement and inflammation

INN	First FDA approval	Target / class	Length (residues)	Notes
Cyclosporine	1983 [3]	Calcineurin inhibitor [4]	11, cyclic [5]	Non-ribosomal peptide [5]; oral capsules and solution [3]
Icatibant	2011 [3]	Bradykinin B2 receptor antagonist [4]	10 [4]	Five non-proteinogenic amino acids [4]
Voclosporin	2021 [3]	Calcineurin inhibitor [4]	11, cyclic [4]	Oral capsule
Pegcetacoplan	2021 [3]	Complement inhibitor [4]	Two 15-residue peptides on a 40 kDa PEG [4]
Zilucoplan	2023 [3]	Complement inhibitor [4]	15, macrocyclic [4]
Icotrokinra	2026 [3]	IL-23 receptor antagonist [4] [5]	13 [4]	Oral tablet [3]

Infectious disease, oncology, pain and other

INN	First FDA approval	Target / class	Length (residues)	Notes
Enfuvirtide	2003 [3]	HIV-1 gp41 fusion inhibitor [5]	36 [5]
Daptomycin	2003 [3]	Lipopeptide antibacterial [4]	13, cyclic, with fatty acid [5]
Ziconotide	2004 [3]	N-type calcium channel [4]	25, three disulfides [5]	Cone snail toxin sequence [9]
Romidepsin	2009 [3]	Histone deacetylase inhibitor [4]	Bicyclic depsipeptide [4]
Motixafortide	2023 [3]	CXCR4 inhibitor [4]	14, cyclic disulfide [4]
Rezafungin	2023 [3]	Echinocandin antifungal [4]	Semisynthetic cyclic lipopeptide [4]
Trofinetide	2023 [3]	Mechanism unknown [4]	3 (Gly-2-methyl-Pro-Glu) [4]	Oral solution
Elamipretide	2025 [3]	Mitochondrial cardiolipin binder [4]	4 (D-Arg-2,6-dimethyl-Tyr-Lys-Phe-NH2) [4]

Dermatology, CNS and receptor agonists with mixed indications

INN	First FDA approval	Target / class	Length (residues)	Notes
Etelcalcetide	2017 [3]	Calcium-sensing receptor agonist [4]	7 D-amino acids plus a disulfide-linked L-cysteine [4]
Afamelanotide	2019 [3]	MC1 receptor agonist [5]	13 [4]
Bremelanotide	2019 [3]	Melanocortin receptor agonist (non-selective) [4]	7, cyclic [4]
Difelikefalin	2021 [3]	Kappa opioid receptor agonist [4]	4 D-amino acids plus an aminopiperidine carboxylic acid [4]

That is 55 molecules across the six tables. It is not exhaustive: diagnostic radiotracers, antibody-drug conjugates with peptide linkers and several older hormone products are omitted. The incretin molecules in the metabolic table are compared in detail in GLP-1 agonists explained.

Peptide approvals by year, 2020 to 2026

Year	Peptides named in the source	Source and its own count	Ref
2020	Setmelanotide, copper Cu 64 dotatate, gallium Ga 68 PSMA-11; belantamab mafodotin listed with a peptide component	Six TIDES among 53 approvals	[10]
2021	Vosoritide, melphalan flufenamide, voclosporin, pegcetacoplan, dasiglucagon, piflufolastat F 18, difelikefalin, odevixibat	Eight peptides plus two ADCs with peptide fragments	[11]
2022	Tirzepatide, terlipressin, lutetium Lu 177 vipivotide tetraxetan (and gadopiclenol in the same review section)	TIDES 14% of 37 new drug entities	[8]
2023	Flotufolastat F 18, motixafortide, rezafungin, trofinetide, zilucoplan	Five peptides	[12] [16]
2024	Palopegteriparatide, pegulicianine; the review also covers levacetylleucine, which its authors state is not a peptide	Two peptides	[13] [17]
2025	Elamipretide; telisotuzumab vedotin, an ADC incorporating a peptide payload	One peptide plus one ADC	[14] [18]
2026 (to 20 Oct)	Navepegritide, icotrokinra, enlicitide decanoate, rusfertide; bulevirtide (47 residues, biologic)	No published TIDES review yet; molecules identified from FDA’s list and Drugs@FDA	[1] [3]

Two cautions apply. The TIDES series uses its own broad definition, so it includes amino acid derivatives and imaging agents that a stricter reader might not call peptide drugs; the 2024 review, for example, includes levacetylleucine, an acetylated amino acid that its authors state is not a peptide [13]. And the 2026 row is our own reading of FDA’s novel approvals list against Drugs@FDA and label descriptions, not a count published by FDA [1] [3] [4].

Trends in peptide therapeutics

1. The incretin class and fatty-acid half-life extension

Native GLP-1 lasts minutes, so the approved GLP-1 receptor agonists are all engineered for longer exposure. Exenatide (2005) was followed by liraglutide (2010), lixisenatide (2016), semaglutide (2017) and the dual GIP and GLP-1 receptor agonist tirzepatide (2022) [3]. Liraglutide, semaglutide and tirzepatide use fatty-acid acylation for albumin binding [9] [4]. The TIDES review of 2024 approvals notes a global shortage of GLP-1 molecules alongside their expanding uses [13]. Investigational successors, such as the triple agonist retatrutide, are covered in the library.

2. Cyclic and macrocyclic peptides

Cyclisation is now common. Of the 2023 to 2026 peptide approvals in the tables above, motixafortide (cyclic disulfide), zilucoplan (15-residue macrocycle), rusfertide (cyclic disulfide) and enlicitide (macrocycle) are cyclic, as are earlier molecules such as octreotide, pasireotide, setmelanotide and cyclosporine [4] [5]. The 2023 TIDES review describes linear, cyclic and lipopeptides among that year’s approvals and credits chemical modification for improving peptide pharmacokinetics [12].

3. Oral peptides

Oral delivery has been the classic limitation. The 2021 TIDES review counted “a total of four orally available peptides” authorised in the preceding five years [11], and the 2023 review highlighted the oral tripeptide trofinetide “given the scarcity of the orally available peptides” [12]. Drugs@FDA records oral semaglutide tablets from 20 September 2019 and octreotide delayed-release capsules from 26 June 2020 [3]. In 2026 FDA approved two oral peptide tablets: icotrokinra, a 13-amino-acid IL-23 receptor antagonist, on 17 March, and enlicitide decanoate, a macrocyclic PCSK9 inhibitor formulated with permeation enhancers, on 15 July [3] [4] [15].

4. PEGylated prodrugs and releasable carriers

Three recent approvals attach a peptide to polyethylene glycol. Pegcetacoplan links two 15-residue peptides to a 40 kDa PEG [4]. Palopegteriparatide (2024) releases PTH(1-34) to maintain continuous exposure, and navepegritide (2026) releases a 38-residue CNP that binds NPR-B [4].

5. Radioligands and imaging peptides

Peptides are also delivery vehicles for radionuclides. Lutetium Lu 177 dotatate binds SSTR2 and is internalised by receptor-positive tumour cells [4], and the TIDES reviews list several PSMA- and somatostatin-targeted imaging peptides among recent approvals [10] [11] [12].

6. Peptides crossing the 40-residue line

Longer designs blur the regulatory boundary. Lixisenatide and tesamorelin (44 residues) now carry BLA numbers [3], and bulevirtide (47 residues, myristoylated) was approved in 2026 as a biologic [4] [1]. Investigational molecules such as the 68-residue amycretin are synthesised chemically yet exceed the protein threshold [2].

What the list means for peptide API research and sourcing

Chemical synthesis is central to the TIDES definition of a peptide drug [8], which is why solid-phase and liquid-phase synthesis, purification and impurity control dominate peptide API development. Eptifibatide’s label, for example, states that it “is produced by solution-phase peptide synthesis, and is purified by preparative reverse-phase liquid chromatography and lyophilized” [4]. Route choices are compared in SPPS vs LPPS, and impurity specifications for approved and generic peptide APIs in peptide API impurities and specifications. For laboratories, the INN, sequence and length in the tables are the starting point for identity testing by LC-MS and purity by HPLC.

How Winhycare Pharma supplies peptide APIs and research peptides

Winhycare Pharma supplies semaglutide and tirzepatide, among other molecules, as research-use-only material for laboratories and, separately, as API to licensed pharmaceutical manufacturers, at a purity of at least 99% as stated in our brochure. US-DMF and CTD Module 3 support is available for semaglutide. Custom synthesis of other peptide sequences is available. See our peptide API supply page, or contact the pharma team about peptide API supply or custom synthesis.

For laboratory research use only. Not for human or veterinary use.