Naturally occurring peptides molecules serve as signaling agents in the body, regulating functions such as hormone activity, immune responses, and cellular communication. Over the last few decades, synthetic modified peptides have been developed to mimic or block these natural signals and have emerged as powerful tools in therapeutic applications, bridging the gap between small molecules and large biologics. These short chains of amino acids, typically comprising 2 to 50 amino acid residues, play a key role in a range of biological processes and are now being harnessed to treat a variety of diseases with high specificity and low toxicity.
Some advantages of peptide demonstrated in therapeutics include:
Because of these advantages, peptides have been applied in a number of therapeutic biotech, as well as in cosmetics industries (Ref 1). A couple of applications are highlighted here.
Peptides are being developed as both diagnostic tools and treatments in oncology. Peptide-drug conjugates and tumor-homing peptides can deliver cytotoxic agents directly to cancer cells, improving efficacy and minimizing damage to healthy tissue.
One Example is Lutetium-177-DOTATATE (Lutathera), a Peptide-Based drug for treating Neuroendocrine Tumors.
Lutathera (Lu-177 DOTATATE) is an FDA-approved peptide receptor radionuclide therapy (PRRT) to treat certain types of gastroenteropancreatic neuroendocrine tumors (GEP-NETs). It represents a powerful example of how peptides can be used to target tumors precisely, minimizing harm to surrounding healthy tissues (Ref 2).
The peptide used in Lutathera is DOTATATE, a synthetic analog of somatostatin, a hormone that binds specifically to somatostatin receptor subtype 2 (SSTR2). These receptors are overexpressed on the surface of many neuroendocrine tumor cells.
DOTATATE is a peptide molecule linked with a radioactive isotope, Lutetium-177 (Lu-177, see Figure 1), which emits beta particles capable of damaging and killing nearby cells.
Figure 1. Lutetium-177-DOTATATE (Lutathera)
DOTATATE can bind specifically to tumor cells expressing SSTR2. Once bound, the radioactive payload is internalized into the tumor cell, where localized radiation causes DNA damage, leading to tumor cell death. Lutathera significantly improved progression-free survival and overall tumor control compared to high-dose octreotide (another somatostatin analog).
Lutathera is a landmark example of peptide-drug conjugates used in oncology. It showcases how a small targeting peptide can deliver a therapeutic payload with incredible precision, embodying the ideals of personalized and targeted cancer therapy (Ref 2).
One of the most notable peptide drugs in managing diabetes is insulin, other examples include GLP-1 receptor agonists like semaglutide, which are used to control blood sugar and support weight loss.
Semaglutide is one example of GLP-1 Receptor Agonist for Type 2 Diabetes and Obesity. Semaglutide is a synthetic peptide molecule (Figure 2) that mimics the human hormone GLP-1 (glucagon-like peptide-1). Fatty acid chain for albumin binding and extends half-life (Ref 3).
Figure 2. Structure of Semaglutide
Semaglutide is used to treat type 2 diabetes and obesity by enhancing insulin secretion, suppressing appetite, and delaying gastric emptying. Semaglutide is considered a game-changer in metabolic medicine. It not only improves glycemic control but also contributes meaningfully to weight loss and cardiometabolic health. Its mechanism of action as below:
Another popular therapeutical peptide is Tirzepatide (known as LY 3298176), a dual GIP and GLP-1 receptor agonist developed by Eli Lilly, Tirzepatide is a gastric inhibitory polypeptide (GIP) analog with a peptide linked to a PEG lipid (Figure 3).
Figure 3. structure of Tirzepatide
Tirzepatide has a greater affinity to GIP receptors than to GLP-1 receptors, and this dual agonist behavior has been shown to produce greater reductions of hyperglycemia compared to a selective GLP-1 receptor agonist. It was used to treat type 2 diabetes and for weight loss. Brand name Mounjaro is for diabetes treatment and Zepbound for weight loss and treatment of obstructive sleep apnea (Ref 4).
A notable example of a peptide used in treating cardiovascular diseases is Nesiritide (brand name: Natrecor) - A Recombinant B-type Natriuretic Peptide (BNP).
Nesiritide is a recombinant form of human B-type natriuretic peptide (BNP) with 32 amino acids (Ref 5), as shown below in Figure 4.
Figure 4. Nesiritide
Brain natriuretic peptide (BNP), a natriuretic peptide synthesized in the cardiac ventricles, is secreted in response to ventricular volume expansion and pressure overload, commonly observed in heart failure. Nesiritide, a recombinant form of human BNP, contributes to cardiovascular fluid homeostasis by antagonizing the renin-angiotensin-aldosterone system and activating guanylate cyclase, thereby inducing smooth muscle cell relaxation (Ref 5).
Antimicrobial peptides (AMPs) show promise in combating antibiotic-resistant bacteria by disrupting microbial membranes. Peptides are also being studied as components of vaccines and antiviral therapies (Ref 6).
For example, Enfuvirtide is a synthetic 36-amino acid peptide (Figure 5) that targets HIV-1, the virus responsible for AIDS. It is the first and FDA-approved peptide-based fusion inhibitor used in antiretroviral therapy (Ref 7).
Figure 5. Enfuvirtide
Despite their promise of peptide utility, peptide therapeutics face several challenges:
However, advances in peptide engineering-such as PEGylation, cyclization, and nanocarrier systems-are helping to overcome these obstacles (Ref 1).
The global peptide therapeutics market is projected to grow significantly in the coming years, driven by increased demand for targeted treatments and innovations in drug delivery technologies. As our understanding of peptide biology deepens, we can expect a new wave of precision medicines that are safer, more effective, and customized to individual patient needs.
Peptides represent a versatile and powerful class of therapeutics with the potential to transform modern medicine. From managing chronic diseases to tackling drug-resistant infections and cancer, peptide-based drugs are paving the way for a new era of targeted and personalized treatment (Ref 2).
As a leading peptide supplier worldwide, BroadPharm offers a comprehensive portfolio of high-quality peptide building blocks and therapeutic peptide compounds to support pharmaceutical and biotech R&D. In addition to our extensive peptide catalog, BroadPharm also provides a broad selection of PEG lipids for peptide conjugation applications. We also offer custom peptide-drug conjugation services to help accelerate the development of targeted therapeutics and innovative drug delivery systems.