Table 1.
Summary of the small peptide (less than 50 amino acids) therapeutics approved by the FDA between January 1999 and December 2019. Raw data (submission classification: Type 1—New Molecular Entity) were collected from Drugs@FDA (http://www.fda.gov/drugsatfda) and the data were further confirmed by DrugBank [50]. “MAP” is defined as “membrane-active peptide”.
| DRUG NAME | APPROVAL DATE | NDA NUMBER | ACTIVE INGREDIENTS | COMPANY | MW | PEPTIDE | APPLICATIONS | CATEGORY | ELIMINATION HALF-LIFE |
|---|---|---|---|---|---|---|---|---|---|
| SCENESSE | 10/8/2019 | 210797 | AFAMELANOTIDE | CLINUVEL INC | 1646.85 | Synthetic peptide | Prevents skin damage from the sun in patients with erythropoietic protoporphyria | Receptor binding | 30 min |
| GALLIUM DOTATOC GA68 | 8/21/2019 | 210828 | GALLIUM DOTATOC GA-68 | UNIV IOWA HOSPS AND CLINICS PET IMAGING CENTER | 1489.65 | Cyclic octapeptide | Neuroendocrine tumors (NETs) diagnosis | Receptor binding | 2–4 h |
| VYLEESI (AUTOINJECTOR) | 6/21/2019 | 210557 | BREMELANOTIDE ACETATE | AMAG PHARMS INC | 1025.2 | Cyclic heptapeptide | Hypoactive sexual desire disorder (HSDD) treatment | Receptor binding | 1.9–4 h |
| LUTATHERA | 1/26/2018 | 208700 | LUTETIUM DOTATATE LU-177 | AAA USA INC | 1609.6 | Cyclic peptide-radionuclide conjugate | Gastroenteropan-creatic neuroendocrine tumors (GEP-NETs) treatment | Receptor binding | 3.5–71 h |
| GIAPREZA | 12/21/2017 | 209360 | ANGIOTENSIN II ACETATE | LA JOLLA PHARMA | 1046.2 | Synthetic peptide | Treatment of sepsis, septic shock, diabetes mellitus, and acute renal failure | Receptor binding | <1 min |
| OZEMPIC | 12/5/2017 | 209637 | SEMAGLUTIDE | NOVO NORDISK INC | 4113.58 | Chemically modified peptide | Improving glycemic control in patients with type 2 diabetes mellitus | Receptor binding | 7 days |
| TYMLOS | 4/28/2017 | 208743 | ABALOPARATIDE | RADIUS HEALTH INC | 3961 | Synthetic peptide | Osteoporosis treatment | Receptor binding | 1.7 h |
| PARSABIV | 2/7/2017 | 208325 | ETELCALCETIDE | KAI PHARMS INC | 1047.5 | Synthetic peptide | Treatment of secondary hyperparathyroidism | Receptor binding | 3–4 days |
| TRULANCE | 1/19/2017 | 208745 | PLECANATIDE | SALIX | 1682 | Cyclic peptide | Chronic idiopathic constipation (CIC) treatment | Receptor binding | N/A |
| ADLYXIN | 7/27/2016 | 208471 | LIXISENATIDE | SANOFI-AVENTIS US | 4858.5 | Synthetic peptide | Type 2 diabetes mellitus (T2DM) treatment | Receptor binding | 1–3.5 h |
| NETSPOT | 6/1/2016 | 208547 | GALLIUM DOTATATE GA-68 | AAA USA INC | 1435.6 | Cyclic peptide-radionuclide conjugate | Neuroendocrine tumors (NETs) diagnosis | Receptor binding | 1 h |
| ORBACTIV | 8/6/2014 | 206334 | ORITAVANCIN DIPHOSPHATE | MELINTA THERAP | 1989.09 | Lipoglycopeptide | Treatment of complicated skin and skin structure infections (cSSSI) caused by gram-positive bacteria | MAP | 195.4 h |
| DALVANCE | 5/23/2014 | 021883 | DALBAVANCIN HYDROCHLORIDE | ALLERGAN SALES LLC | ~1800 | Lipoglycopeptide | Treatment of complicated skin and skin structure infections (cSSSI) caused by gram-positive bacteria | Inhibitor | 346 h |
| GATTEX KIT | 12/21/2012 | 203441 | TEDUGLUTIDE RECOMBINANT | NPS PHARMS INC | 3752 | Glucagon-like peptide-2 | Short bowel syndrome (SBS) treatment | Receptor binding | 1.3–2 h |
| SIGNIFOR | 12/14/2012 | 200677 | PASIREOTIDE DIASPARTATE | NOVARTIS | 1313.41 | Cyclohexapeptide | Treatment of Cushing’s disease | Receptor binding | 10–13 h |
| LINZESS | 8/30/2012 | 202811 | LINACLOTIDE | ALLERGAN SALES LLC | 1526.8 | Cyclic peptide | Treatment of irritable bowel syndrome | Receptor binding | N/A |
| KYPROLIS | 7/20/2012 | 202714 | CARFILZOMIB | ONYX THERAP | 719.9 | Modified tetrapeptidyl epoxide | Multiple myeloma treatment | Inhibitor | ≤1 h |
| FIRAZYR | 8/25/2011 | 022150 | ICATIBANT ACETATE | SHIRE ORPHAN THERAP | 1304.5 | Synthetic peptide | Treatment of angioedema, liver disease, burns, and burn infections | Receptor binding | 1.4 h |
| INCIVEK | 5/23/2011 | 201917 | TELAPREVIR | VERTEX PHARMS | 679.85 | Chemically modified peptide | Treatment of chronic Hepatitis C | Inhibitor | 4–11 h |
| EGRIFTA | 11/10/2010 | 022505 | TESAMORELIN ACETATE | THERATECHNOLOGIES | 5135.9 | Synthetic peptide | Human immunodeficiency virus (HIV) treatment | Receptor binding | 26–38 min |
| VICTOZA | 1/25/2010 | 022341 | LIRAGLUTIDE RECOMBINANT | NOVO NORDISK INC | 3751.2 | Synthetic peptide | Improving glycemic control in patients with type 2 diabetes mellitus | Receptor binding | 13 h |
| ISTODAX | 11/5/2009 | 022393 | ROMIDEPSIN | CELGENE | 540.71 | Bicyclic peptide | Treatment of cutaneous T-cell lymphoma (CTCL) and/or peripheral T-cell lymphoma (PTCL) | Inhibitor | 3 h |
| VIBATIV | 9/11/2009 | 022110 | TELAVANCIN HYDROCHLORIDE | CUMBERLAND PHARMS | 1755.6 | Lipoglycopeptide | Treatment of complicated skin and skin structure infections (cSSSI) caused by Gram-positive bacteria | MAP | 8 h |
| FIRMAGON | 12/24/2008 | 022201 | DEGARELIX ACETATE | FERRING | 1632.3 | Synthetic peptide | Prostate cancer treatment | Receptor binding | 53 h |
| SOMATULINE DEPOT | 30/08/2007 | 022074 | LANREOTIDE ACETATE | IPSEN PHARMA | 1096.34 | Cyclical octapeptide | Treatment of neuroendocrine tumors (NETs) and acromegaly | Receptor binding | 22 days |
| ERAXIS | 2/17/2006 | 021632 | ANIDULAFUNGIN | VICURON | 1140.3 | Lipopeptide | Anti-fungal drug | Inhibitor | 40–50 h |
| LEVEMIR | 6/16/2005 | 021536 | INSULIN DETEMIR RECOMBINANT | NOVO NORDISK INC | 5916.9 | A long-acting basal insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 57 h |
| LEVEMIR FLEXPEN | 6/16/2005 | 021536 | INSULIN DETEMIR RECOMBINANT | NOVO NORDISK INC | 5916.9 | A long-acting basal insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 5–7 h |
| LEVEMIR FLEXTOUCH | 6/16/2005 | 021536 | INSULIN DETEMIR RECOMBINANT | NOVO NORDISK INC | 5916.9 | A long-acting basal insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 5–7 h |
| LEVEMIR INNOLET | 6/16/2005 | 021536 | INSULIN DETEMIR RECOMBINANT | NOVO NORDISK INC | 5916.9 | A long-acting basal insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 5–7 h |
| LEVEMIR PENFILL | 6/16/2005 | 021536 | INSULIN DETEMIR RECOMBINANT | NOVO NORDISK INC | 5916.9 | A long-acting basal insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 5–7 h |
| BYETTA | 4/28/2005 | 021773 | EXENATIDE SYNTHETIC | ASTRAZENECA AB | 4186.6 | Synthetic peptide | Improving glycemic control in patients with type 2 diabetes mellitus | Receptor binding | 2.4 h |
| SYMLIN | 3/16/2005 | 021332 | PRAMLINTIDE ACETATE | ASTRAZENECA AB | 3949.4 | Peptide hormone | Treatment of type 1 and type 2 diabetes mellitus | Receptor binding | 48 min |
| PRIALT | 12/28/2004 | 021060 | ZICONOTIDE ACETATE | TERSERA THERAPS LLC | 2639 | Synthetic peptide | Chronic pain treatment | Inhibitor | 2.9–6.5 h |
| APIDRA | 4/16/2004 | 021629 | INSULIN GLULISINE RECOMBINANT | SANOFI AVENTIS US | 5823 | Human insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Inhibitor | 13–86 min |
| APIDRA SOLOSTAR | 4/16/2004 | 021629 | INSULIN GLULISINE RECOMBINANT | SANOFI AVENTIS US | 5823 | Human insulin analog | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Inhibitor | 13–86 min |
| CHIRHOSTIM | 4/9/2004 | 021256 | SECRETIN SYNTHETIC HUMAN | CHIRHOCLIN | 3039.44 | Gastrointestinal peptide hormone | (1) Pancreatic secretions to aid in the diagnosis of pancreatic exocrine dysfunction(2) Gastrin secretion to aid in the diagnosis of gastrinoma(3) Pancreatic secretions to facilitate the identification of the ampulla of Vater and accessory papilla during ERCP | Inhibitor | 45 min |
| PLENAXIS | 11/25/2003 | 021320 | ABARELIX | SPECIALTY EUROPEAN | 1416.06 | Synthetic peptide | Prostate cancer treatment | Inhibitor | 13.2 days |
| CUBICIN | 9/12/2003 | 021572 | DAPTOMYCIN | CUBIST PHARMS LLC | 1620.67 | Cyclic lipopeptide | Treatment of complicated skin and skin structure infections (cSSSI) caused by Gram-positive bacteria | MAP | 8.1–9 h |
| CUBICIN RF | 9/12/2003 | 021572 | DAPTOMYCIN | CUBIST PHARMS LLC | 1620.67 | Cyclic lipopeptide | Treatment of complicated skin and skin structure infections (cSSSI) caused by Gram-positive bacteria | MAP | 8.1–9 h |
| REYATAZ | 6/20/2003 | 021567 | ATAZANAVIR SULFATE | BRISTOL MYERS | 704.9 | Azapeptide | Human immunodeficiency virus (HIV) treatment | Inhibitor | 6.5–7.9 h |
| VELCADE | 5/13/2003 | 021602 | BORTEZOMIB | MILLENNIUM PHARMS | 384.24 | Chemically modified peptide | Multiple myeloma treatment | Inhibitor | 9–15 h |
| FUZEON | 3/13/2003 | 021481 | ENFUVIRTIDE | ROCHE | 4492 | Synthetic peptide | Human immunodeficiency virus (HIV) treatment | Inhibitor | 3.8 h |
| NATRECOR | 8/10/2001 | 020920 | NESIRITIDE RECOMBINANT | SCIOS LLC | 3464 | Cyclic peptide | Acute decompensated heart failure (ADHF) treatment | Receptor binding | 18 min |
| CANCIDAS | 1/26/2001 | 021227 | CASPOFUNGIN ACETATE | MERCK | 1213.42 | Cyclic lipopeptide | Anti-fungal drug | Inhibitor | 9–11 h |
| ANGIOMAX | 12/15/2000 | 020873 | BIVALIRUDIN | SANDOZ INC | 2180 | Synthetic peptide | Treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis | Inhibitor | 22 min–3.5 h |
| CETROTIDE | 8/11/2000 | 021197 | CETRORELIX | EMD SERONO INC | 1431.06 | Synthetic peptide | For prevention of premature ovulation in women undergoing fertility treatments with controlled ovulation | Receptor binding | ~62.8 h |
| TRELSTAR | 6/15/2000 | 020715 | TRIPTORELIN PAMOATE | ALLERGAN SALES LLC | 1699.9 | Synthetic peptide | Prostate cancer treatment | Receptor binding | 6 min–3 h |
| NOVOLOG | 6/7/2000 | 020986 | INSULIN ASPART RECOMBINANT | NOVO NORDISK INC | 5825.8 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 81 min |
| NOVOLOG FLEXPEN | 6/7/2000 | 020986 | INSULIN ASPART RECOMBINANT | NOVO NORDISK INC | 5825.8 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 81 min |
| NOVOLOG FLEXTOUCH | 6/7/2000 | 020986 | INSULIN ASPART RECOMBINANT | NOVO NORDISK INC | 5825.8 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 81 min |
| NOVOLOG INNOLET | 6/7/2000 | 020986 | INSULIN ASPART RECOMBINANT | NOVO NORDISK INC | 5825.8 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 81 min |
| NOVOLOG PENFILL | 6/7/2000 | 020986 | INSULIN ASPART RECOMBINANT | NOVO NORDISK INC | 5825.8 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | 81 min |
| LANTUS | 4/20/2000 | 021081 | INSULIN GLARGINE RECOMBINANT | SANOFI AVENTIS US | 6063 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | N/A |
| LANTUS SOLOSTAR | 4/20/2000 | 021081 | INSULIN GLARGINE RECOMBINANT | SANOFI AVENTIS US | 6063 | Peptide hormone | Treatment of hyperglycemia caused by type 1 and type 2 diabetes | Receptor binding | N/A |
| NEO TECT KIT | 8/3/1999 | 021012 | TECHNETIUM TC-99M DEPREOTIDE | CIS BIO INTL SA | 486.14 | Cyclic peptide | (1) Detecting coronary artery disease(2) Evaluating myocardial function | Others | 6.02 h |
| GANIRELIX ACETATE | 7/29/1999 | 021057 | GANIRELIX ACETATE | ORGANON USA INC | 1570.35 | Peptide hormone | For inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation | Receptor binding | 16.2 h |