The power of peptide therapeutics: Advancements and methods in peptide drug development

28th Jun 2024

As the pharmaceutical industry has heightened its focus on targeted therapies and personalised medicine, peptide therapeutics have emerged as a promising strategy.

While the earliest peptide therapeutics came from natural sources, limitations like low oral bioavailability and short half-lives have caused reluctance around peptide research in the past . Over the last several decades, however, advances in technology have enabled scientists to enhance peptide functionality and synthesise novel peptides for a particular purpose.

Now, the global peptide therapeutics market is valued at $43.45 billion , and this number continues to grow. With their high specificity, precise targeting capabilities, and opportunities for custom design, peptides have become a core focus for many pharmaceutical and biotechnology organisations.

In this whitepaper, we’ll cover the advantages and core use cases for peptides in the pharmaceutical space, then compare methods for peptide drug development.

Peptide advancements and use cases

Peptide therapeutics themselves are not a new discovery. Insulin, for example, was first used to treat diabetes in the 1920s . However, insulin and other peptide therapeutics at the time were derived from natural sources. Today, scientists are using technological advances to develop novel, targeted peptides.

Chemical synthesis of peptides first occurred in the 1950s, but peptide drugs still brought a number of challenges. As scientists began to apply strategies like the incorporation of non-natural amino acids and backbone modification, they have been able to extend half-life, improve solubility, and increase stability, making peptide therapeutics even more appealing . Today, more than 80 peptide drugs have been approved worldwide, with over 30 non-insulin peptide therapeutics entering the market since 2000 .

Here are some of the key reasons synthetic peptides have gained traction:

Scientists can design peptides to target specific receptors, maximising therapeutic efficiency while minimising side effects. This allows for more targeted therapies and supports the development of personalised medicines.

Tumour-homing peptides, such as the arginylglycylaspartic acid (RGD) peptide, are designed to improve internalisation of nanoparticles into cancerous cells.


Naturally occurring peptides play a role in numerous physiological processes. As a result, peptide drugs can be applied to a wide range of treatment areas, and administered in a variety of ways, including injections, oral formulations, and others.

Peptides have been developed to treat HIV, chronic pain, short bowel syndrome, and numerous other indications.

Synthesis and other biological methods for peptide development allow scientists to focus on and optimise certain properties, like stability and bioavailability. In addition, scientists can develop peptides for specific targets or pathways.

One example is CB1, a custom peptide derived from the naturally occurring Cecropin B to target lung cancer cells while avoiding healthy lung cells.

Examining methods of peptide development

Modern peptide therapeutics are generally developed in one of two ways; through peptide synthesis, or using biological routes. In peptide synthesis, amino acids are chemically assembled to create a peptide chain, while biological routes involve cell cultivation to express and then extract the desired peptide.

One of the most common methods of synthesis is solid-phase peptide synthesis (SPPS), which builds an amino acid sequence on a solid support. After synthesis, the product is purified to remove byproducts and isolate the active component, which is then dried using lyophilization to create the resulting peptide drug. Today, scientists can leverage automated synthesisers, such as microwave-assisted peptide synthesisers, to build peptides with greater efficiency than ever. Purification is then necessary to remove any byproducts and isolate the target peptide.

Both peptide synthesis and biological approaches to customisation can be beneficial in certain use cases. While biological routes deliver advantages like post-translational modifications and can support potentially more complex structures, chemical peptide synthesis can enable greater cost-effectiveness, more precise control, higher stability, and faster development.

Selecting the most appropriate method

When discerning whether to leverage peptide synthesis or biological methods in their programmes, scientists should consider several factors. Here are some of the potential advantages each approach can deliver:

Peptide synthesis

• Precise control over amino acid sequence

• Lower setup costs

• Rapid development

• Higher stability

• Access to non-natural peptides

Biological methods

• Support for complex structures

• Potential for post-translational modifications

• Higher specificity

• Environmental friendliness

Maximising peptide potential with the right partner

Now is a more exciting time than ever for peptide therapeutics, with over 170 peptide drugs in clinical development today and even more in the preclinical stage. As peptides remain a core area of research and progress in the life sciences space, pharmaceutical and biotechnology organisations require a partner with extensive expertise.

Sterling’s Cork, Ireland facility offers more than 20 years of expertise in peptide synthesis, analysis, manufacturing and purification, and we are authorised to supply peptides to all markets. Our facilities include a dedicated laboratory for peptide analysis and a multipurpose plant with a peptide synthesiser and stirred reactors. In addition, our purification plant consists of multiple chromatography columns, bioburden controls and cleanroom lyophilization capability, allowing us to support a full range of peptide synthesis requirements. We combine powerful capabilities with close collaboration to empower our customers and support industry-wide innovation.

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