Peptide Database
265 therapeutic peptides with research summaries, clinical findings, and regulatory status.
Pentosan Polysulfate (Elmiron)
A semi-synthetic sulfated polysaccharide derived from beechwood hemicellulose with structural similarities to glycosaminoglycans. Pentosan polysulfate replenishes the defective glycosaminoglycan layer of the bladder urothelium in interstitial cystitis, reducing urothelial permeability to irritants. It also exhibits anti-inflammatory, anticoagulant, and fibrinolytic properties through inhibition of complement activation and mast cell histamine release.
Semaglutide (Ozempic/Wegovy)
A glucagon-like peptide-1 receptor agonist (GLP-1 RA) with 94% amino acid homology to native GLP-1. Semaglutide enhances glucose-dependent insulin secretion, suppresses glucagon, delays gastric emptying, and acts on hypothalamic GLP-1 receptors to reduce appetite. Its fatty acid side chain enables albumin binding, extending its half-life to approximately 7 days.
Tirzepatide (Mounjaro/Zepbound)
A first-in-class dual glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptor agonist. Tirzepatide activates both incretin pathways simultaneously, producing superior glycemic control and weight loss compared to selective GLP-1 RAs. The dual mechanism enhances insulin sensitivity and lipid metabolism beyond what either pathway achieves alone.
Liraglutide (Saxenda/Victoza)
A GLP-1 receptor agonist with 97% homology to native GLP-1, modified with a fatty acid side chain (C-16 palmitoyl) enabling albumin binding and a half-life of approximately 13 hours. Liraglutide enhances glucose-dependent insulin secretion, suppresses glucagon, delays gastric emptying, and promotes satiety through hypothalamic GLP-1R activation. It was the first GLP-1 RA approved for chronic weight management.
Exenatide (Byetta/Bydureon)
A synthetic version of exendin-4, a 39-amino acid peptide originally isolated from the saliva of the Gila monster lizard (Heloderma suspectum). Exenatide shares 53% homology with human GLP-1 and is resistant to DPP-4 degradation. It activates GLP-1 receptors to enhance insulin secretion, suppress glucagon, slow gastric emptying, and promote beta-cell preservation.
Glucagon
A 29-amino acid peptide hormone produced by alpha cells of the pancreatic islets of Langerhans. Glucagon acts primarily on hepatocytes via the glucagon receptor (GCGR), a G-protein-coupled receptor that activates adenylyl cyclase, increasing cAMP and triggering glycogenolysis and gluconeogenesis to raise blood glucose. It also relaxes smooth muscle of the GI tract and has positive inotropic and chronotropic cardiac effects.
Pramlintide (Symlin)
A synthetic analog of amylin (islet amyloid polypeptide), a 37-amino acid peptide hormone co-secreted with insulin from pancreatic beta cells. Pramlintide has three proline substitutions that prevent amyloid fibril formation while retaining amylin receptor activity. It slows gastric emptying, suppresses postprandial glucagon secretion, and promotes satiety via area postrema activation, complementing insulin therapy in diabetes management.
Dulaglutide (Trulicity)
A long-acting GLP-1 receptor agonist consisting of a GLP-1 analog covalently linked to a modified human IgG4 Fc fragment via a peptide linker. This fusion protein design increases molecular size to reduce renal clearance and enables FcRn-mediated recycling, producing a half-life of approximately 5 days suitable for once-weekly dosing. Dulaglutide activates pancreatic GLP-1 receptors to enhance glucose-dependent insulin secretion and suppress glucagon.
Lixisenatide (Adlyxin)
A selective GLP-1 receptor agonist derived from exendin-4 with a modified C-terminal tail containing six lysine residues. Lixisenatide has a half-life of approximately 3 hours and primarily reduces postprandial glucose through potent delay of gastric emptying rather than fasting glucose reduction. It is designed for once-daily use as an add-on to basal insulin therapy in type 2 diabetes.
Setmelanotide (Imcivree)
A cyclic peptide melanocortin-4 receptor (MC4R) agonist designed to restore MC4R signaling in patients with obesity caused by genetic deficiencies in the leptin-melanocortin pathway. Setmelanotide bypasses upstream defects in POMC, PCSK1, or LEPR genes by directly activating MC4R, reducing hunger and increasing energy expenditure. It represents one of the first precision medicines for genetically defined obesity.
Sermorelin
A synthetic 29-amino acid analog of GHRH representing the shortest fully functional fragment of the native 44-amino acid hormone. Sermorelin stimulates the pituitary to produce and release growth hormone through the natural GHRH receptor pathway, preserving the hypothalamic-pituitary feedback axis. It maintains physiological pulsatile GH secretion patterns.
Tesamorelin (Egrifta)
A synthetic GHRH analog consisting of the 44-amino acid sequence of human GHRH with a trans-3-hexenoic acid modification at the N-terminus to improve stability. Tesamorelin specifically targets visceral adipose tissue reduction by stimulating lipolysis through GH-mediated pathways. It is the only FDA-approved treatment for HIV-associated lipodystrophy.
PT-141 (Bremelanotide / Vyleesi)
A synthetic cyclic heptapeptide melanocortin receptor agonist that activates MC3R and MC4R in the central nervous system. Unlike PDE5 inhibitors that act peripherally on vascular smooth muscle, PT-141 works centrally through hypothalamic melanocortin pathways that modulate sexual arousal and desire. It is a metabolite of Melanotan II without significant melanogenic activity.
Oxytocin
A nine-amino acid cyclic neuropeptide produced in the hypothalamus and released from the posterior pituitary. Oxytocin mediates uterine contractions during labor, milk ejection during lactation, and social bonding behaviors. It modulates the HPA stress axis, reduces cortisol, and has anxiolytic properties. Intranasal administration reaches the CNS through olfactory and trigeminal nerve pathways.
Macimorelin (Macrilen)
An orally bioavailable growth hormone secretagogue approved as a diagnostic agent for adult growth hormone deficiency (AGHD). Macimorelin stimulates GH release via GHS-R1a agonism, and the GH response to a standardized oral dose is used to confirm or exclude AGHD. It offers a simpler, better-tolerated alternative to the insulin tolerance test and GHRH-arginine test for GH deficiency diagnosis.
Cosyntropin (Cortrosyn)
A synthetic peptide consisting of the first 24 amino acids of the 39-amino acid adrenocorticotropic hormone (ACTH). Cosyntropin retains full biological activity of native ACTH for stimulating adrenal cortisol production and is used as a diagnostic agent in the ACTH stimulation test to evaluate adrenal gland function. It binds to the MC2R receptor on adrenocortical cells, activating steroidogenesis.
Gonadorelin (GnRH)
A synthetic decapeptide identical to endogenous gonadotropin-releasing hormone. Gonadorelin stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary when administered in a pulsatile fashion. Continuous or high-dose administration paradoxically downregulates GnRH receptors, suppressing gonadotropin secretion, a principle exploited by GnRH agonist therapeutics.
Leuprolide (Lupron)
A synthetic nonapeptide GnRH agonist approximately 15-fold more potent than native GnRH. After an initial stimulatory phase (flare effect) lasting 1-2 weeks, chronic leuprolide administration downregulates pituitary GnRH receptors, resulting in profound suppression of LH, FSH, and downstream sex steroids. This chemical castration effect is exploited in treating hormone-sensitive cancers, endometriosis, and precocious puberty.
Goserelin (Zoladex)
A synthetic decapeptide GnRH agonist administered as a biodegradable subcutaneous implant that provides sustained drug release over 1 or 3 months. Like other GnRH agonists, goserelin initially stimulates and then suppresses the HPG axis, reducing sex hormone production to castrate or postmenopausal levels. The implant formulation eliminates the need for repeated injections and ensures compliance.
Cetrorelix (Cetrotide)
A synthetic decapeptide GnRH antagonist that competitively blocks pituitary GnRH receptors, producing immediate and dose-dependent suppression of LH and FSH without the initial flare effect seen with GnRH agonists. Cetrorelix prevents premature LH surges during controlled ovarian stimulation in IVF, allowing precise timing of oocyte maturation and retrieval.
Ganirelix
A synthetic decapeptide GnRH antagonist that competitively and reversibly blocks GnRH receptors on pituitary gonadotroph cells. Ganirelix rapidly suppresses LH secretion within hours of administration, preventing premature ovulation during assisted reproductive technology (ART) cycles. Its mechanism provides immediate suppression without the flare phase associated with GnRH agonists.
Semax
A synthetic heptapeptide analog of the ACTH(4-7) fragment (Met-Glu-His-Phe-Pro-Gly-Pro) with nootropic and neuroprotective properties. Semax modulates BDNF and NGF expression, enhances monoaminergic neurotransmission, and provides neuroprotection through anti-oxidant and anti-inflammatory mechanisms. It crosses the blood-brain barrier via intranasal administration.
Enfuvirtide (Fuzeon)
A 36-amino acid synthetic peptide that inhibits HIV-1 entry into CD4+ T-cells by blocking the gp41-mediated membrane fusion step. Enfuvirtide binds to the first heptad repeat (HR1) region of gp41, preventing the conformational change required for viral-cell membrane fusion. It is the first and only FDA-approved fusion inhibitor and is active against HIV-1 strains resistant to other antiretroviral drug classes.
Teriparatide (Forteo)
A recombinant form of the first 34 amino acids of human parathyroid hormone (PTH 1-34). When administered intermittently via daily subcutaneous injection, teriparatide stimulates osteoblastic bone formation more than osteoclastic resorption, producing a net anabolic effect on bone. It activates the PTH1 receptor on osteoblasts, increasing Wnt signaling, osteoblast differentiation, and survival while reducing sclerostin expression.
Abaloparatide (Tymlos)
A synthetic 34-amino acid peptide analog of parathyroid hormone-related protein (PTHrP 1-34) that selectively activates the RG conformation of the PTH1 receptor. This receptor selectivity produces a more transient signaling response compared to teriparatide, favoring anabolic bone formation with less stimulation of bone resorption and calcium mobilization. Abaloparatide increases bone mineral density at both cortical and trabecular sites.
Calcitonin
A 32-amino acid peptide hormone naturally produced by parafollicular C-cells of the thyroid gland. Calcitonin inhibits osteoclast-mediated bone resorption by binding to calcitonin receptors on osteoclasts, reducing their activity and number. Salmon calcitonin is approximately 40-50 times more potent than human calcitonin and has a longer half-life, making it the preferred therapeutic form.
Vosoritide (Voxzogo)
A C-type natriuretic peptide (CNP) analog that acts as an agonist at the natriuretic peptide receptor B (NPR-B) on growth plate chondrocytes. Vosoritide counteracts the constitutively activated FGFR3 signaling that suppresses endochondral ossification in achondroplasia. By stimulating the NPR-B/cGMP/MAPK pathway, it antagonizes the growth-inhibitory FGFR3 signal and restores more normal linear bone growth.
Vasopressin (ADH)
A nine-amino acid cyclic peptide hormone (arginine vasopressin) produced in the hypothalamus and released from the posterior pituitary. Vasopressin acts on V1a receptors (vascular smooth muscle vasoconstriction), V1b receptors (ACTH release from pituitary), and V2 receptors (aquaporin-2 insertion in renal collecting ducts for water reabsorption). It is essential for body water homeostasis and hemodynamic stability.
Desmopressin (DDAVP)
A synthetic analog of vasopressin with enhanced V2 receptor selectivity and minimal V1a vasopressor activity. Desmopressin has a deaminated cysteine at position 1 and D-arginine at position 8, increasing its antidiuretic potency 10-fold while largely eliminating the hypertensive effects of native vasopressin. Its prolonged half-life of 2-4 hours (vs. 10-20 minutes for vasopressin) allows convenient dosing for chronic conditions.
Terlipressin
A synthetic vasopressin analog and prodrug that is cleaved by endopeptidases to release lysine-vasopressin. Terlipressin has greater V1a receptor selectivity than vasopressin, producing splanchnic vasoconstriction that reduces portal pressure and redistributes blood flow to the kidneys. This mechanism addresses the pathophysiology of hepatorenal syndrome (HRS) by counteracting the splanchnic vasodilation that drives renal hypoperfusion.
Eptifibatide (Integrilin)
A synthetic cyclic heptapeptide modeled after the KGD (Lys-Gly-Asp) disintegrin sequence found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). Eptifibatide is a potent, reversible glycoprotein IIb/IIIa receptor antagonist that blocks the final common pathway of platelet aggregation by preventing fibrinogen and von Willebrand factor binding to activated platelets.
Nesiritide (Natrecor)
A recombinant form of human B-type natriuretic peptide (BNP), a 32-amino acid peptide naturally produced by ventricular cardiomyocytes in response to volume overload and wall stress. Nesiritide binds natriuretic peptide receptor A (NPR-A), activating guanylyl cyclase and increasing intracellular cGMP to produce venous, arterial, and coronary vasodilation, natriuresis, and suppression of the renin-angiotensin-aldosterone and sympathetic nervous systems.
Angiotensin II (Giapreza)
A synthetic form of the endogenous octapeptide angiotensin II, the primary effector of the renin-angiotensin system. Angiotensin II acts on AT1 receptors on vascular smooth muscle to produce potent vasoconstriction, and on the adrenal cortex to stimulate aldosterone release. Exogenous administration raises blood pressure in vasodilatory shock refractory to conventional vasopressors by restoring vascular tone through a mechanism complementary to catecholamine vasopressors.
Bivalirudin (Angiomax)
A synthetic 20-amino acid peptide that acts as a direct thrombin inhibitor by binding both the catalytic active site and anion-binding exosite 1 of thrombin. Bivalirudin inhibits both free and clot-bound thrombin, providing more predictable anticoagulation than heparin without requiring antithrombin III as a cofactor. It is enzymatically cleaved by thrombin itself, producing a self-limiting anticoagulant effect with a 25-minute half-life.
Romiplostim (Nplate)
A thrombopoietin (TPO) receptor agonist consisting of a peptide sequence that binds the TPO receptor (c-Mpl) fused to an IgG1 Fc domain (peptibody). Romiplostim activates JAK2/STAT5 signaling in megakaryocyte progenitors, promoting megakaryocyte proliferation, differentiation, and platelet production. It has no sequence homology to endogenous TPO, minimizing the risk of cross-reactive antibody formation.
Pegcetacoplan (Empaveli)
A pegylated cyclic peptide that inhibits complement component C3, the central node of all three complement activation pathways (classical, lectin, and alternative). By binding C3 and preventing its cleavage into C3a and C3b, pegcetacoplan blocks both intravascular hemolysis (mediated by membrane attack complex) and extravascular hemolysis (mediated by C3b opsonization and phagocytosis). This dual mechanism addresses the limitation of C5 inhibitors that only prevent intravascular hemolysis.
Carfilzomib (Kyprolis)
A tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds the chymotrypsin-like (beta5) subunit of the 20S proteasome. By blocking proteasomal degradation of ubiquitinated proteins, carfilzomib causes accumulation of misfolded proteins, endoplasmic reticulum stress, and activation of the unfolded protein response, leading to apoptosis preferentially in malignant plasma cells. Its irreversible binding confers greater proteasome inhibition than bortezomib.
Bortezomib (Velcade)
A modified dipeptidyl boronic acid that reversibly inhibits the chymotrypsin-like activity of the 26S proteasome. Bortezomib disrupts the ubiquitin-proteasome pathway, stabilizing pro-apoptotic factors and inhibiting NF-kB activation, which is constitutively active in many hematologic malignancies. It was the first proteasome inhibitor approved for cancer treatment and fundamentally changed the treatment landscape of multiple myeloma.
Lutetium-177 dotatate (Lutathera)
A radiolabeled somatostatin analog consisting of the peptide DOTA-Tyr3-octreotate chelated to the beta-emitting radioisotope lutetium-177. Lutathera binds with high affinity to somatostatin receptor subtype 2 (SSTR2), which is overexpressed on neuroendocrine tumor cells, delivering targeted radiation therapy directly to tumor cells while sparing surrounding normal tissue. This peptide receptor radionuclide therapy (PRRT) approach combines receptor-targeted delivery with cytotoxic radiation.
Leuprolide (Lupron) - Oncology
A GnRH agonist used in oncology for androgen deprivation therapy (ADT) in prostate cancer and hormone suppression in premenopausal breast cancer. Chronic administration produces sustained downregulation of pituitary GnRH receptors, achieving medical castration with testosterone levels below 50 ng/dL. The initial testosterone flare can be mitigated by co-administration of an antiandrogen. Depot formulations provide sustained release for up to 6 months.
Octreotide (Sandostatin)
A synthetic octapeptide analog of somatostatin with a substantially longer half-life (90 minutes IV, 6 hours subcutaneous vs. 2 minutes for native somatostatin). Octreotide binds somatostatin receptors (primarily SSTR2 and SSTR5) to inhibit the secretion of GH, glucagon, insulin, gastrin, secretin, VIP, and other GI hormones. It reduces splanchnic blood flow, GI motility, and exocrine pancreatic secretion.
Lanreotide (Somatuline Depot)
A synthetic octapeptide analog of somatostatin with high affinity for SSTR2 and moderate affinity for SSTR5 receptors. Lanreotide is formulated as a supersaturated solution that forms a drug depot at the injection site, providing sustained release over 4 weeks. It inhibits GH secretion, GI hormone release, and has direct antiproliferative effects on neuroendocrine tumor cells through cell cycle arrest and apoptosis induction.
Pasireotide (Signifor)
A multireceptor-targeted somatostatin analog with high binding affinity for SSTR1, SSTR2, SSTR3, and SSTR5, particularly notable for its 40-fold greater affinity for SSTR5 compared to octreotide. This receptor profile makes pasireotide uniquely effective in Cushing's disease, where corticotroph adenomas predominantly express SSTR5. Pasireotide suppresses ACTH secretion from pituitary corticotroph tumors, reducing cortisol production.
Plecanatide (Trulance)
A synthetic 16-amino acid peptide structurally related to uroguanylin, an endogenous intestinal peptide that regulates fluid and electrolyte homeostasis in the GI tract. Plecanatide activates guanylate cyclase-C (GC-C) receptors on intestinal epithelial cells in a pH-dependent manner, preferentially in the proximal small intestine where pH is slightly acidic. GC-C activation increases intracellular and extracellular cGMP, stimulating chloride and bicarbonate secretion while reducing visceral pain signaling.
Linaclotide (Linzess)
A synthetic 14-amino acid peptide structurally related to the heat-stable enterotoxin of Escherichia coli and the endogenous peptide guanylin. Linaclotide activates guanylate cyclase-C (GC-C) on the luminal surface of intestinal epithelium, increasing intracellular cGMP to stimulate CFTR-mediated chloride and bicarbonate secretion, accelerating intestinal transit. Extracellular cGMP also reduces firing of visceral afferent pain fibers, providing analgesic effects in the gut.
Secretin
A 27-amino acid peptide hormone produced by S-cells of the duodenal and jejunal mucosa in response to acidic chyme entering the small intestine. Secretin stimulates pancreatic ductal cells to secrete bicarbonate-rich fluid, neutralizing duodenal acid, and promotes bile flow from hepatocytes. It was the first hormone ever identified (Bayliss and Starling, 1902) and serves as a key diagnostic tool in gastroenterology and endocrinology.
Ziconotide (Prialt)
A synthetic 25-amino acid peptide identical to omega-conotoxin MVIIA, a neurotoxin found in the venom of the marine cone snail Conus magus. Ziconotide selectively and reversibly blocks N-type voltage-gated calcium channels (Cav2.2) in the dorsal horn of the spinal cord, inhibiting neurotransmitter release from primary afferent nociceptive neurons. It provides analgesia without opioid receptor activation, tolerance development, or respiratory depression.
Difelikefalin (Korsuva)
A selective kappa-opioid receptor (KOR) agonist peptide that does not cross the blood-brain barrier, providing peripheral analgesia and anti-pruritic effects without central opioid side effects such as euphoria, dysphoria, sedation, or addiction. Difelikefalin activates kappa receptors on peripheral sensory neurons and immune cells to reduce itch signaling and inflammation. Its restricted CNS penetration is a deliberate design feature to avoid abuse potential.
Afamelanotide (Scenesse)
A synthetic 13-amino acid analog of alpha-melanocyte-stimulating hormone (alpha-MSH) with a substitution of norleucine at position 4 that confers enhanced potency and enzymatic stability. Afamelanotide activates melanocortin-1 receptors (MC1R) on melanocytes, stimulating eumelanin production independent of UV exposure. The resulting increase in skin eumelanin provides photoprotection by absorbing UV radiation and scavenging reactive oxygen species.
Pentagastrin
A synthetic pentapeptide containing the C-terminal tetrapeptide sequence of gastrin (Trp-Met-Asp-Phe-NH2) linked to beta-alanine. Pentagastrin stimulates gastric acid secretion by binding to cholecystokinin-2 (CCK2) receptors on parietal cells, and stimulates calcitonin release from thyroid C-cells. It has been used as a diagnostic agent for both gastric acid secretory capacity testing and provocative testing for medullary thyroid carcinoma (MTC).
Icatibant (Firazyr)
A synthetic decapeptide bradykinin B2 receptor antagonist containing five non-natural amino acids for enhanced stability and receptor selectivity. Icatibant competitively blocks bradykinin, the primary mediator of swelling in hereditary angioedema (HAE) caused by C1 esterase inhibitor deficiency. By preventing bradykinin-induced vasodilation and increased vascular permeability, it rapidly reverses mucosal and subcutaneous edema.
Teduglutide (Gattex)
Teduglutide is a recombinant analogue of human glucagon-like peptide-2 (GLP-2) comprising 33 amino acids with a single amino acid substitution that confers resistance to enzymatic degradation by dipeptidyl peptidase-4. This GLP-2 receptor agonist enhances intestinal epithelial barrier function, promotes mucosal growth, and increases mesenteric blood flow, thereby improving nutrient and fluid absorption. The therapeutic rationale centers on reducing dependence on parenteral nutrition in patients with short bowel syndrome by augmenting remnant bowel adaptive capacity.
Beinaglutide
Beinaglutide is a recombinant glucagon-like peptide-1 (GLP-1) receptor agonist engineered with structural modifications to prolong plasma half-life and improve metabolic stability. The peptide activates GLP-1 receptors on pancreatic beta cells, stimulating glucose-dependent insulin secretion while suppressing glucagon release, delaying gastric emptying, and promoting satiety. Its mechanism targets multiple pathways involved in glycemic control, making it suitable for the treatment of type 2 diabetes mellitus.
Albiglutide (Tanzeum)
Albiglutide is a GLP-1 receptor agonist consisting of a tandem repeat of modified human GLP-1 sequences fused to human albumin, creating a protein of approximately 73 kilodaltons with extended pharmacokinetic properties. The albumin fusion technology allows for once-weekly dosing by delaying renal clearance and protecting the peptide from enzymatic degradation. By activating GLP-1 receptors, albiglutide enhances glucose-dependent insulin secretion and suppresses inappropriate glucagon release in patients with type 2 diabetes.
Capromorelin (Entyce)
Capromorelin is a selective ghrelin receptor agonist, or growth hormone secretagogue, that mimics the endogenous peptide hormone ghrelin by binding to the GHS-R1a receptor in the hypothalamus and pituitary. Activation of ghrelin receptors stimulates appetite, promotes growth hormone release, and modulates energy balance, providing a therapeutic rationale for conditions characterized by inappetence and weight loss. The compound is formulated as an oral solution, distinguishing it from injectable peptide therapies.
Anamorelin (Adlumiz)
Anamorelin is an orally active selective ghrelin receptor agonist designed to stimulate appetite and promote anabolic processes by mimicking endogenous ghrelin at the growth hormone secretagogue receptor (GHS-R1a). The small-molecule peptidomimetic increases growth hormone and IGF-1 secretion while enhancing food intake and lean body mass, targeting the muscle wasting and cachexia associated with chronic illness. Its oral bioavailability and receptor selectivity differentiate it from earlier injectable ghrelin analogues.
Somatropin (Genotropin)
Somatropin is recombinant human growth hormone (rhGH) consisting of 191 amino acids identical in sequence to endogenous pituitary growth hormone. It binds to growth hormone receptors on target tissues to stimulate linear growth, protein synthesis, lipolysis, and carbohydrate metabolism. Genotropin is one of several branded formulations of somatropin approved for multiple indications including pediatric growth hormone deficiency, Turner syndrome, and adult growth hormone deficiency.
Somapacitan (Sogroya)
Somapacitan is a long-acting growth hormone analogue engineered by attaching an albumin-binding moiety to recombinant human growth hormone. This modification extends the half-life to allow once-weekly subcutaneous administration, compared to daily injections required for standard somatropin. The peptide retains growth hormone receptor agonist activity with pharmacokinetic enhancement intended to improve treatment adherence.
Lonapegsomatropin (Skytrofa)
Lonapegsomatropin is a long-acting prodrug of somatropin created through site-specific PEGylation that releases active growth hormone after administration. The PEG moiety extends circulating half-life and enables once-weekly dosing for pediatric growth hormone deficiency. This represents a transient modification strategy in which the PEG is cleaved to yield native growth hormone.
Pegvisomant (Somavert)
Pegvisomant is a PEGylated growth hormone receptor antagonist engineered from human growth hormone with nine amino acid substitutions that confer antagonist properties. The molecule binds to growth hormone receptors but does not activate downstream signaling, effectively blocking the action of endogenous growth hormone. It is used exclusively for the treatment of acromegaly in patients with inadequate response to surgery or other medical therapies.
Mecasermin (Increlex)
Mecasermin is recombinant human insulin-like growth factor 1 (IGF-1) consisting of 70 amino acids identical to the endogenous peptide hormone. It binds to IGF-1 receptors to promote growth and anabolic processes, bypassing the need for growth hormone receptor signaling. Mecasermin is indicated specifically for children with severe primary IGF-1 deficiency or growth hormone gene deletion who have developed neutralizing antibodies to growth hormone.
OP-1 / BMP-7
OP-1, or osteogenic protein-1, is the recombinant form of bone morphogenetic protein-7 (BMP-7), a member of the transforming growth factor-beta superfamily. This homodimeric protein induces differentiation of mesenchymal stem cells into osteoblasts and chondrocytes, stimulating new bone formation. It was developed primarily for spinal fusion procedures and long bone non-unions where autologous bone graft is not feasible.
Carperitide (h-ANP)
Carperitide is a recombinant form of human atrial natriuretic peptide consisting of 28 amino acids. It activates guanylyl cyclase A receptors, increasing intracellular cyclic GMP to promote vasodilation, natriuresis, and diuresis. The peptide reduces cardiac preload and afterload while inhibiting the renin-angiotensin-aldosterone system, providing therapeutic benefit in acute heart failure.
Brain Natriuretic Peptide (BNP)
Brain natriuretic peptide, despite its name, is a 32-amino acid hormone secreted predominantly by ventricular cardiomyocytes in response to ventricular stretch and pressure overload. It activates guanylyl cyclase A receptors to promote vasodilation, natriuresis, and suppression of the renin-angiotensin-aldosterone and sympathetic nervous systems. BNP and its N-terminal fragment (NT-proBNP) are widely used as diagnostic and prognostic biomarkers in heart failure.
Degarelix (Firmagon)
Degarelix is a synthetic decapeptide gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of advanced prostate cancer. Unlike GnRH agonists, degarelix competitively blocks GnRH receptors in the anterior pituitary without causing an initial testosterone surge, achieving rapid suppression of luteinizing hormone and testosterone. This immediate pharmacological castration provides therapeutic benefit in androgen-dependent malignancies. The peptide consists of unnatural amino acids to resist enzymatic degradation and prolong activity.
Triptorelin (Trelstar)
Triptorelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) that functions as a long-acting GnRH agonist. Following an initial stimulatory phase, chronic administration leads to downregulation of pituitary GnRH receptors, resulting in suppression of luteinizing hormone and follicle-stimulating hormone secretion and subsequent reduction in sex steroid production. This mechanism provides therapeutic benefit in hormone-sensitive conditions including advanced prostate cancer, endometriosis, and central precocious puberty. The peptide incorporates amino acid substitutions at positions 6 and 10 to enhance receptor affinity and metabolic stability.
Histrelin (Vantas)
Histrelin is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH) that functions as a GnRH agonist. The peptide is administered via a subcutaneous implant that delivers continuous drug release over 12 months, inducing initial gonadotropin stimulation followed by sustained receptor downregulation and suppression of testicular androgen production. It is indicated for palliative treatment of advanced prostate cancer and management of central precocious puberty. Amino acid modifications at positions 6 and 10 enhance receptor binding and resistance to peptidase degradation.
Abarelix (Plenaxis)
Abarelix is a synthetic decapeptide that functions as a gonadotropin-releasing hormone (GnRH) receptor antagonist. It competitively blocks pituitary GnRH receptors, producing immediate suppression of luteinizing hormone, follicle-stimulating hormone, and testosterone without the initial surge associated with GnRH agonists. The peptide was developed for treatment of advanced symptomatic prostate cancer in patients who refused surgical castration and were not candidates for GnRH agonist therapy. Its structure incorporates multiple unnatural amino acids to optimize receptor antagonism and pharmacokinetic properties.
Elagolix (Orilissa)
Elagolix is a small molecule non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist administered orally. While not a peptide itself, it mimics the antagonist action of peptide GnRH blockers by competitively inhibiting endogenous GnRH at pituitary receptors, resulting in dose-dependent suppression of luteinizing hormone, follicle-stimulating hormone, and ovarian sex steroids. It is indicated for management of moderate to severe endometriosis pain and heavy menstrual bleeding associated with uterine fibroids. The oral bioavailability distinguishes it from injectable peptide GnRH antagonists.
Relugolix (Orgovyx)
Relugolix is an orally bioavailable non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist. Although it is not a peptide, it exerts its therapeutic effect through the same mechanism as peptide GnRH antagonists, competitively blocking pituitary GnRH receptors to suppress gonadotropin and sex steroid production. It is indicated for advanced prostate cancer and, in combination formulation, for management of heavy menstrual bleeding associated with uterine fibroids and moderate to severe endometriosis pain. The oral route of administration offers a distinct advantage over depot peptide formulations.
177Lu-PSMA-617 (Pluvicto)
177Lu-PSMA-617 is a radioligand therapeutic consisting of a small peptide-based ligand targeting prostate-specific membrane antigen (PSMA) conjugated to the beta-emitting radioisotope lutetium-177. The peptide component binds selectively to PSMA, a transmembrane protein highly expressed on prostate cancer cells, enabling targeted delivery of cytotoxic radiation to tumor sites while sparing normal tissues. It is indicated for treatment of metastatic castration-resistant prostate cancer in patients previously treated with androgen receptor pathway inhibition and taxane-based chemotherapy. The targeting moiety is derived from a urea-based peptidomimetic scaffold optimized for PSMA affinity.
Somatostatin (Native)
Somatostatin is a naturally occurring cyclic tetradecapeptide hormone produced by neuroendocrine cells throughout the body, including the hypothalamus, pancreas, and gastrointestinal tract. It functions as a potent inhibitor of growth hormone, insulin, glucagon, and various gastrointestinal hormones by binding to five subtypes of somatostatin receptors (SSTR1-5), which are G protein-coupled receptors. The therapeutic rationale in oncology derives from the expression of somatostatin receptors on neuroendocrine tumors and the peptide's ability to inhibit tumor cell proliferation and hormone secretion. Native somatostatin has an extremely short plasma half-life of 2 to 3 minutes, limiting its clinical utility and necessitating the development of longer-acting synthetic analogues.
Tirbanibulin (Klisyri)
Tirbanibulin is a small molecule synthetic peptide mimetic that inhibits tubulin polymerization and disrupts Src kinase signaling pathways. It is applied topically as a 1% ointment to treat actinic keratosis, a precancerous skin condition caused by chronic sun exposure. The dual mechanism targets both the cytoskeleton and oncogenic signaling in hyperproliferative keratinocytes. Its localized application minimizes systemic exposure while achieving targeted antiproliferative effects.
Cholecystokinin (CCK)
Cholecystokinin is an endogenous peptide hormone existing in multiple forms, most commonly as CCK-8 and CCK-33, secreted by I-cells in the duodenum and jejunum. It binds to CCK-1 and CCK-2 receptors to stimulate gallbladder contraction, pancreatic enzyme secretion, and satiety signaling. Therapeutic interest centers on diagnostic imaging applications and potential treatments for obesity and functional gastrointestinal disorders. The peptide also plays neuromodulatory roles in the central nervous system.
Polymyxin B
Polymyxin B is a cyclic lipopeptide antibiotic derived from Bacillus polymyxa, consisting of a heptapeptide ring and a tripeptide side chain acylated with a fatty acid tail. The molecule binds to lipopolysaccharide in the outer membrane of Gram-negative bacteria, causing membrane permeabilization and cell death. Its cationic residues interact electrostatically with anionic phosphate groups on lipid A. Polymyxin B is reserved for serious infections caused by multidrug-resistant Gram-negative pathogens when other options are unavailable.
Colistin (Polymyxin E)
Colistin, also known as polymyxin E, is a cyclic polypeptide antibiotic structurally similar to polymyxin B, produced by Paenibacillus polymyxa. It disrupts the bacterial cell membrane by binding to lipopolysaccharide and displacing divalent cations, leading to increased permeability and cell lysis. The compound is administered as colistimethate sodium, an inactive prodrug that is hydrolyzed in vivo to the active colistin base. Its spectrum targets Gram-negative bacteria, particularly Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumoniae.
PTH (1-34) Analogs
PTH (1-34) analogs, including teriparatide and abaloparatide, are synthetic peptides corresponding to the 34 N-terminal amino acids of human parathyroid hormone. These agents bind to the PTH1 receptor on osteoblasts and osteocytes, stimulating bone formation through activation of intracellular signaling pathways including cyclic AMP and protein kinase A. Intermittent administration preferentially stimulates osteoblastic bone formation over osteoclastic resorption, increasing bone mass and reducing fracture risk. The anabolic effect distinguishes these agents from antiresorptive therapies such as bisphosphonates.
Sclerostin Antibodies (Romosozumab)
Romosozumab is a humanized monoclonal antibody that binds and inhibits sclerostin, a glycoprotein produced by osteocytes that negatively regulates the Wnt signaling pathway. By blocking sclerostin, romosozumab increases Wnt pathway activity in osteoblasts, simultaneously promoting bone formation and reducing bone resorption. This dual mechanism produces rapid and substantial increases in bone mineral density. The antibody is composed of two heavy and two light immunoglobulin chains in a standard IgG2 configuration.
BMP-2 (Bone Morphogenetic Protein-2)
BMP-2 is a member of the transforming growth factor-beta superfamily, consisting of a homodimeric protein with each monomer containing approximately 114 amino acids in its mature form. The protein binds to type I and type II serine/threonine kinase receptors on mesenchymal stem cells, activating SMAD-dependent signaling pathways that induce osteoblastic differentiation and bone formation. Recombinant human BMP-2 is delivered on an absorbable collagen sponge carrier to provide sustained local release at the site of intended bone growth. The molecule is a potent osteoinductive agent capable of inducing ectopic bone formation when implanted in soft tissue.
BMP-7 (Osteogenic Protein-1)
BMP-7, also known as osteogenic protein-1 (OP-1), is a member of the bone morphogenetic protein family with a mature homodimeric structure of approximately 139 amino acids per monomer. Like other BMPs, it signals through serine/threonine kinase receptors to activate SMAD transcription factors, promoting differentiation of mesenchymal cells into osteoblasts and chondrocytes. The recombinant form is delivered on a bovine collagen matrix to provide localized, sustained release. BMP-7 also exhibits renoprotective effects in preclinical models, though clinical development in nephrology has not advanced.
Gonadotropin Releasing Hormone (GnRH) Agonists
Gonadotropin-releasing hormone agonists are synthetic decapeptide analogues of native GnRH that initially stimulate and then suppress gonadotropin secretion from the pituitary gland. Following initial receptor activation, continuous GnRH agonist exposure leads to receptor downregulation and reversible suppression of the hypothalamic-pituitary-gonadal axis, reducing sex steroid production. Approved formulations include leuprolide, goserelin, and triptorelin, used primarily in hormone-sensitive cancers and reproductive medicine. The longevity rationale derives from theoretical models linking reduced reproductive signaling to extended lifespan observed in model organisms, though this remains speculative in humans.
Nafarelin (Synarel)
Nafarelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) with substitutions at positions 6 and 10 that enhance receptor affinity and metabolic stability. Chronic administration leads to downregulation of pituitary GnRH receptors and suppression of gonadotropin secretion, resulting in a hypoestrogenic state. This mechanism is therapeutically exploited in conditions requiring ovarian suppression, including endometriosis and central precocious puberty.
Choriogonadotropin Alfa (Ovidrel)
Choriogonadotropin alfa is a recombinant human chorionic gonadotropin produced in Chinese hamster ovary cells with identical amino acid sequence to endogenous hCG. The 237-amino acid heterodimeric glycoprotein binds the LH/hCG receptor on ovarian granulosa and theca cells to trigger final oocyte maturation and ovulation. It is used in assisted reproductive technology protocols to time oocyte retrieval and support luteal phase progesterone production.
Follitropin Alfa (Gonal-F)
Follitropin alfa is a recombinant human follicle-stimulating hormone produced in Chinese hamster ovary cells, consisting of a heterodimeric glycoprotein with 92-amino acid alpha and 111-amino acid beta subunits. The peptide binds FSH receptors on ovarian granulosa cells to stimulate follicular development, estradiol synthesis, and oocyte maturation. It is employed in ovulation induction and controlled ovarian stimulation for assisted reproductive technologies.
Menotropin (Menopur)
Menotropin is a purified preparation of human menopausal gonadotropins extracted from the urine of postmenopausal women, containing both follicle-stimulating hormone and luteinizing hormone activity in approximately equal proportions. The combination of FSH and LH bioactivity stimulates follicular recruitment, granulosa cell proliferation, and steroidogenesis in ovarian theca cells. It is indicated for ovulation induction in anovulatory infertility and controlled ovarian hyperstimulation in assisted reproduction.
Corifollitropin Alfa (Elonva)
Corifollitropin alfa is a recombinant long-acting FSH analogue created by fusing the C-terminal peptide of the hCG beta subunit to the FSH beta chain. This structural modification extends the elimination half-life to approximately 70 hours, enabling a single injection to sustain follicular stimulation for seven days. The agent is designed to simplify controlled ovarian stimulation protocols by replacing the first week of daily FSH injections in IVF cycles.
Cetrorelix (Cetrotide) Analog
Cetrorelix is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) that acts as a competitive GnRH receptor antagonist. By binding to pituitary GnRH receptors, it rapidly suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion without the initial agonist flare seen with GnRH agonists. This property makes it valuable for controlled ovarian stimulation protocols, where prevention of premature LH surges is critical for optimizing oocyte retrieval timing.
Peginesatide (Omontys)
Peginesatide is a synthetic pegylated peptide-based erythropoiesis-stimulating agent (ESA) consisting of two 21-amino acid chains linked to polyethylene glycol. Unlike recombinant erythropoietin, it contains no erythropoietin sequence homology yet activates the erythropoietin receptor to stimulate red blood cell production. The pegylation confers a prolonged half-life, enabling once-monthly dosing in dialysis-dependent chronic kidney disease.
Eltrombopag Peptide Mimetics
Eltrombopag is a small-molecule, non-peptide thrombopoietin receptor agonist that binds to the transmembrane domain of the thrombopoietin receptor, distinct from the natural ligand binding site. While not itself a peptide, it mimics thrombopoietin signaling to stimulate megakaryocyte proliferation and platelet production. The oral bioavailability of this synthetic agent addresses limitations of recombinant thrombopoietin peptides, which face immunogenicity challenges.
DOTATATE (Ga-68)
Gallium-68 DOTATATE is a radiolabeled somatostatin analog consisting of an octapeptide (Tyr3-octreotate) conjugated to the macrocyclic chelator DOTA, which binds the positron-emitting radioisotope gallium-68. It exhibits high affinity for somatostatin receptor subtype 2, which is overexpressed on neuroendocrine tumor cells, enabling PET imaging of these malignancies. The 68-minute half-life of gallium-68 and the rapid pharmacokinetics of the peptide provide excellent tumor-to-background ratios within 1 to 2 hours post-injection.