Table 3.
FDA-approved peptides between 2016 and 2020.
| # | Active Ingredient (Trade Name) | Company | Structure | Indication | Target | FDA Approval |
|---|---|---|---|---|---|---|
| Free Peptides | ||||||
| 1 | Lixisenatide (AdlyxinTM) |
Sanofi-Aventis (Paris, France) |
44 AAs | Diabetes type (II) | Glucagon-like peptide 1 receptor | July 2016 |
| 2 | Plecanatide (TrulanceTM) |
Synergy Pharmaceuticals (New York, NY, USA) |
16 AAs 2 disulfides | Chronic idiopathic constipation | Guanylate cyclase-C | January 2017 |
| 3 | Etelcalcetide (ParsabivTM) |
KAI Pharmaceuticals (South of San Francisco, CA, USA) Amgen (Thousand Oaks, CA, USA) |
7 AAs (all D) 1 disulfide intermolecular L-Cys | Secondary hyperparathyroidism in adult chronic kidney disease | Calcium-sensing receptor |
February 2017 |
| 4 | Abaloparatide (TymloTM) |
Radius Health (Boston, MA, USA) |
34 AAs | Anabolic agent | Parathyroid hormone 1 receptor | April 2017 |
| 5 | Semaglutide (OzempicTM) |
Novo Nordisk (Måløv, Denmark) |
31 AAs branched PEG-fatty acid | Diabetes type (II) | Glucagon-like peptide 1 receptor | December 2017 |
| 6 | Macimorelin (MacrilenTM) |
Aeterna Zentaris (Frankfurt, Germany) |
3 residues pseudopeptide | Diagnosis of adult growth hormone deficiency | Growth hormone secretagogue receptor type 1 |
December 2017 |
| 7 | Angiotensin II (GiaprezaTM) |
La Jolla Pharmaceutical (San Diego, CA, USA) |
8 AAs | Septic shock, diabetes mellitus, and acute renal failure | Type-1 angiotensin II receptor | December 2017 |
| 8 | Afamelanotide (ScenesseTM) |
University of Arizona (Tucson, Arizona, USA) Clinuvel Inc. (Menlo Park, CA, USA) |
13 AAs | Erythropoietic protoporphyria | Melanocortin 1 receptor | October 2019 |
| 9 | Bremelanotide (VyleesiTM) |
Palatin Technology (East Windsor, NJ, USA) AMAG Pharmaceuticals (Waltham, MA, USA) |
7AAs cyclic sidechain to tail | Hypoactive sexual desire disorder | Melanocortin receptors | June 2019 |
| 10 | Setmelanotide (ImcivreeTM) |
Rhythm Pharmaceuticals (Boston, MA, USA) |
8AAs Cyclic disulfide | Obesity | Melanocortin-4 receptor | November 2020 |
| Peptide-Chelator-radionuclide conjugates | ||||||
| 11 | [177Lu]-DOTA-TATE (LutatheraTM) | Advanced Accelerator Applications (Millburn, NJ, USA) |
7AAs Cyclic disulfide | Gastroenteropancreatic neuroendocrine tumors | Somatostatin receptor | January 2018 |
| 12 | [68Ga]-DOTATOC | University of Iowa Health Care (Iowa City, IA, USA) |
A 7AAs Cyclic disulfide | PET imaging | Somatostatin receptor | August 2019 |
| 13 | [64Cu]-DOTATATE (DetectnetTM) | Radiomedix Inc. (Housten, TX, USA) |
A 7AAs Cyclic disulfide | PET imaging | Somatostatin receptor | September 2020 |
| 14 | [68Ga]-PSMA-11 | University of California (Oakland, CA, USA) |
Peptidomemitic 2AAs urea linked | Diagnosis of recurrent prostate carcinoma by PET | Prostate-specific membrane antigen | December 2020 |
| Peptides in ADC’s | ||||||
| 15 | Enfortumab vedotin-ejfv (PadcevTM) |
Astellas Pharma (Northbrook, IL, USA) |
5 residues with γ-AA | Urothelial cancers | Nectin-4 receptor | December 2019 |
| 16 | Polatuzumab vedotin-piiq (PolivyTM) |
Roche (South of San Francisco, CA, USA) |
5 residues with γ-AA | Refractory diffuse large B-cell lymphoma | CD79b receptor expressed in mature Bcells | June 2019 |
| 17 | Belantamab mafodotin-blmf (BlenrepTM) |
GlaxoSmithKline (Brentford, UK) |
5 residues with γ-AA | Relapsed or refractory multiple myeloma | B-cell maturation antigen |
August 2020 |