Table 1.
List of selected FDA approved peptides, their sequence, type of counter-ion used, classification, and target [75,79,80,81].
| Name | Sequence | Counter-Ion | Chain Length | Brand Names | Company | Route of Administration | Target/Application |
|---|---|---|---|---|---|---|---|
| Eptifibatide | c(Mpa-hRGDWPC)NH2 | Acetate | 8 | INTEGRILIN® | Schering-Plough/Essex | Intravenous injection | Lutropin-choriogonadotropic hormone receptor, follicle-stimulating hormone receptor |
| Leuprolide | PHWSYLLR-NH2 | Acetate | 8 | Eligard®, Enantone®, Lupron®, Memryte® | Atrix Labs, Takeda, Abott, Curaxis | Subcutaneous injection | Analogue of gonadotropin releasing hormone (GnRH) |
| Desmopressin | c(Mpa-YFQNC)PrG-NH2 | Acetate | 8 | Nocdurna® | Ferring Pharmaceuticals, Inc. | Sublingual tablets | Agonist of vasopressin V1a, V1b V2 receptors |
| Vasopressin | c(CYFQNC)PRG-NH2 | Acetate | 9 | Pitressin® | JHP Pharmaceuticals | Intramuscular, subcutaneous injection | Agonist of vasopressin V1a, V1b V2 receptors |
| Oxytocin | c(CYIQNC)PRG-NH2 | Acetate | 9 | Pitocin® | JHP Pharmaceuticals | Intravenous infusion | Agonist of interferon alpha/beta receptor 1 and 2 |
| Buserelin | pEHWSYs(tBu)LRP-NHEt | Acetate | 9 | Suprecur® | Sanofi-Aventis | Subcutaneous injection | Agonist of lutropin-choriogonadotropic hormone receptor and GnRH receptor |
| Abarelix | Ac-d-2Nal-d-4-chloroPhe-d -3-(3′ -pyridyl)AS-N(Me)YLK(iPr)Pa-NH2 | Acetate | 10 | PlenaxisT® | Praecis Pharms | Intramuscular injection | Palliative treatment of men with advanced prostate cancer. GnRH antagonist that reduces the serum testosterone. |
| Cetrorelix | Ac-d-2Nal-d-4-chloroPhe-d-3-(3’ -pyridyl)Ala-SY-d-Cit-LRPa-NH2 | Acetate | 10 | Cetrotide® | Merck Serono | Subcutaneous injection | GnRH antagonistic activity. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner |
| Goserelin | pEHWSYs(tBu)LRP-NHNHCONH2 | Acetate | 10 | ZOLADEX® | AstraZeneca | Subcutaneus administration | GnRH agonist for the management of locally confined carcinoma of the prostate or palliative treatment of advanced carcinoma |
| Histrelin | pEHWSYh(1-Bn)LRP-NHEt | Acetate | 10 | Vantas® | Endo Pharmaceuticals | Subcutaneus administration | LH-RH agonist, acts as a potent inhibitor of gonadotropin secretion, implant consists of a 50-mg histrelin acetate drug core inside a nonbiodegradable, 3 cm by 3.5 mm cylindrically shaped hydrogel reservoir |
| Icatibant | rRP-Hyp-G-Thi-S-d-Tic-Oic-R | Acetate | 10 | Firazyr® | Jerini AG | Subcutaneous injection | Treatment of hereditary angioedema |
| Triporelin | pEHWSYwLRPG-NH2 | Pamoate | 10 | Trelstar Depot® | Debio Recherche Pharmaceutique | Intramuscular injection | GnRH agonist that causes a transient increase in serum testosterone levels. As a result, isolated cases of worsening of signs and symptoms of prostate cancer during the first weeks of treatment |
| Gramicidin D | XGALAVVVWLWLWLWY X–V or I Y–W, F or Y |
Chloride | 16 | Neosporin®/Sofradex® | Pfizer/Sanofi | External use only, occular use | Short term treatment of steroid responsive conditions of the eye when prophylactic antibiotic treatment is also required; Otitis externa |
| Bivalirudin | fPRPGGGGNGDFEEIPEEYL | Trifluoroacetate | 20 | Angiomax®/Angiox® | The Medicines Company UK | Intravenous infusion/injection | Prothrombin inhibitor |
| Lucinactant | KLLLLKLLLLKLLLKLLLLK | Acetate | 21 | Surfaxin® | Discovery Laboratories, Inc. | Intratracheal administration | Lung function improvement, pulmonary surfactant |
| Cosyntropin | SYSMEHFRWGKPVGKKRRPVKVYP | Acetate | 24 | Cortrosyn® | Amphastar Pharmaceuticals | Intravenous injection, intravenous infusion, intramuscular injection | Agonist of adrenocorticotropic hormone receptor |
| Secretin | HSDGTFTSELSRLRDSARLQRLLQGLV | Acetate | 27 | SecreFlo®, Secremax® | Repligen Corp | Intravenous infusion | Agonist of secretin receptor |
| Thymalfasin | SDAAVDTSSEITTKDLKEKKEVVEEAEN | Acetate | 28 | Zadaxin® | SciClone Pharmaceuticals (SCLN) | Subcutaneous injection | Synthetic analogue of thymosin-alpha-1 for the treatment of malignant melanoma |
| Glucagon recombinant | HSQGTFTSDYSKYLDSRRAQDFVQWLMNT | Chloride | 29 | GlucaGen®/Glucagon® | Novo Nordisk/Eli Lilly | Subcutaneous, intramuscular, or intravenous infusion | Agonist of glucagon, glucagon-like peptide 1, and glucagon-like peptide 2 receptors |
| Sermorelin | YADAIFTNSYRKVLGQLSARKLLQDIMSRQ | Acetate | 30 | Sermorelin acetate® | Emd serono inc | Subcutaneous injection | Agonist of growth hormone-releasing hormone receptor |
| Nesiritide | SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH | Acetate | 32 | NATRECOR® | Scios unit of Johnson and Johnson, | Intravenous injection | Recombinant form of the B-type natriuretic peptide |
| Liraglutide | HAEGTFTSDVSSYLEGQAAKEEFIIAWLVKGRG | Acetate | 33 | Saxenda®, Victoza® | Novo Nordisk | Subcutaneous injection | Agonist of glucagon-like peptide 1 receptor |
| Enfuvirtide | Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2 | Acetate | 36 | FUZEON® | Roche | Subcutaneous injection | HIV fusion inhibitor, antiretroviral drug used in combinational therapy in the treatment of HIV-1 |
| Pramlintide | Kc(CNTATC)ATQRLANFLVHSSNNFGPILPPTNVGSNTY-NH2 | Acetate | 37 | Symlin® | AstraZeneca | Subcutaneous injection | Calcitonin receptor, receptor activity-modifying protein 1, receptor activity-modifying protein 2, receptor activity-modifying protein 3 |
| Acthar | SYSMEHFRWGKPVGKKRRPVKVYPDGAEDQLAEAFPLEF | Acetate | 39 | H.P. Acthar® | Questcor Pharmaceutical Inc. | Intramuscular or subcutaneous injection, | Adrenocorticotropic hormone (ACTH) analogue indicated as monotherapy for the treatment of infantile spasms in infants and children under 2 years of age |
| Corticorelin | SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA-NH2, | Trifluoroacetate | 41 | Acthrel® | Ferring Pharmaceuticals, Inc. | Intravenous injection | Analogue of the human CRH (hCRH) peptide. Stimulates ACTH release and further cortisol production |
| Tesamorelin | X-YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL-NH2 X-trans-3-hexenoic acid |
Acetate | 44 | Egrifta® | Theratechnologies | Subcutaneous injection | Agonist of growth hormone-releasing hormone receptor |
| Aprotinin | RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA | Acetate | 58 | Trasylol® | Bayer Pharmaceuticals | Intravenous administration | Broad spectrum protease inhibitor which modulates systemic inflammatory response |
| Lepirudin | LXYTDC(1)TESGQNLC(1)LC(2)EGSNVC(3)GQGNKC(2)ILGSDGEKNQC(3)VTGEGTPKPQSHNDGDFEEIPEEYLQ X–V or T Dissulfide bridges 1-1; 2-2 and 3-3 |
Acetate | 65 | Refludan® | Berlex Labs | Intravenous infusion | Thrombin inhibitor, analogue of hirudin, used as anticoagulant |
| Mecasermin | GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | Acetate | 70 | Increlex® | Tercica, Inc. | Subcutaneous Injection | Human insulin-like growth factor-1 (rhIGF-1, rDNA origin) |
c—cyclization through dissulfide bridge.