Peptide Database
265 therapeutic peptides with research summaries, clinical findings, and regulatory status.
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.
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.
Buserelin (Suprefact)
Buserelin is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH) that acts as a potent GnRH agonist. It binds with high affinity to pituitary GnRH receptors, initially stimulating gonadotropin release before inducing receptor desensitization and downregulation, ultimately suppressing sex hormone production. The peptide is used primarily in the management of hormone-dependent prostate cancer and endometriosis. Structural modifications include substitution of glycine at position 6 with D-serine and replacement of the C-terminal glycine amide with an ethylamide group to enhance potency and duration of action.
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.
Vapreotide
Vapreotide is a synthetic octapeptide analog of somatostatin with enhanced selectivity for somatostatin receptor subtypes 2 and 5. It exerts antisecretory and antiproliferative effects by binding to these receptors on neuroendocrine tumor cells and inhibiting hormone release. The therapeutic rationale centers on control of symptoms associated with vasoactive intestinal peptide secreting tumors and other neuroendocrine malignancies. Its longer half-life compared to native somatostatin allows for sustained receptor occupancy.
Vantictumab
Vantictumab is a fully human monoclonal antibody that targets multiple Frizzled receptors involved in the Wnt signaling pathway. By blocking Frizzled receptors 1, 2, 5, 7, and 8, it inhibits Wnt-driven tumor growth and is designed to target cancer stem cells. The therapeutic rationale is based on dysregulated Wnt signaling in various solid tumors, particularly breast and pancreatic cancers. Inhibition of this pathway may reduce tumor recurrence and metastatic potential.
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.
Plitidepsin (Aplidin)
Plitidepsin is a cyclic depsipeptide originally isolated from the Mediterranean tunicate Aplidium albicans and now produced synthetically. It targets the eukaryotic elongation factor 1A2 (eEF1A2), leading to oxidative stress, cell cycle arrest, and apoptosis in malignant cells. The compound has demonstrated activity against multiple myeloma and other hematologic malignancies in preclinical models. Its unique mechanism distinguishes it from conventional chemotherapeutic agents.
Melphalan Flufenamide (Pepaxto)
Melphalan flufenamide is a first-in-class peptide-drug conjugate that links the alkylating agent melphalan to a dipeptide carrier. The dipeptide facilitates cellular uptake via aminopeptidases that are overexpressed in myeloma cells, where intracellular cleavage releases active melphalan. This targeted delivery aims to enhance tumor exposure while reducing systemic toxicity. The compound represents a prodrug strategy to improve the therapeutic index of cytotoxic chemotherapy.