Current Trends in Therapeutic Peptide Drug Discovery

June 13, 2025

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Peptides are changing the way we approach health and fitness. These small chains of amino acids mimic natural proteins in the body, targeting specific biological pathways. Unlike traditional drugs, they’re highly effective for treating chronic diseases and metabolic disorders.

In India, the prevalence of obesity is rising at an alarming rate. A 2025 World Heart Federation report shows 10% of women and 5% of men over 20 are obese, affecting around 44 million women and 26 million men. This trend is concerning, as obesity leads to diseases like type 2 diabetes, cardiovascular disorders, and fatty liver disease.

This article explores how peptides provide targeted treatments for chronic diseases, cancer, and metabolic disorders, with real-world examples and advantages over conventional drugs.

Recent advances in peptide therapeutics

Recent advances in peptide therapeutics showcase their growing importance in treating various diseases. Newly approved peptide drugs and ongoing clinical trials demonstrate this trend.

Recent approvals of peptide drugs and active clinical trials

Peptide drugs are steadily gaining ground, with more approvals and clinical trials paving the way for their broader use.

New Peptide Drugs: Approvals and Pending Reviews

Liraglutide: Approved in June 2025 for the treatment of insufficiently controlled Type 2 Diabetes Mellitus in adults, adolescents, and children aged 10 years and above.
Tirzepatide: Under review in India for chronic weight management and Type 2 Diabetes, with SEC approval in June 2024. Launch expected after final regulatory clearance and local trials.
Semaglutide: Under review in India for expanded use in diabetes and obesity. Expected broader approval due to rising demand for GLP-1 therapies.

Peptides in clinical trials:

MET-097i (Metsera Inc.): Now in Phase 2b, this oral peptide shows promise for obesity treatment by reducing fat while preserving muscle.
ANG1005 (Angiochem): ANG1005 is a paclitaxel-peptide conjugate designed to cross the blood-brain barrier and treat brain cancers like high-grade glioma and breast cancer brain metastases.

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Also read: Peptide hormones list: overview, functions, and examples

Key trends driving new applications in disease treatment

Peptides are not just a novel treatment option today. They’re becoming a central focus in the fight against several challenging diseases. Here’s how!

1. Autoimmune diseases:
Peptides offer a targeted way to treat autoimmune conditions like lupus and multiple sclerosis. Unlike traditional drugs that suppress the entire immune system, peptides can selectively modulate specific immune cells, thereby improving safety and reducing side effects.

2. Oncology:
Peptides are being used as both standalone therapies and in peptide-drug conjugates (PDCs) in cancer treatment. PDCs enhance precision by delivering chemotherapy directly to tumour cells, minimising harm to healthy tissue.

3. Neurological diseases:
Peptides show promise in treating neurological conditions like Alzheimer’s and Parkinson’s. To overcome the blood-brain barrier, researchers are combining peptides with nanoparticle carriers for better brain delivery.

4. Peptide-based vaccines and immune modulators:
Interest in peptide-based vaccines has surged post-pandemic. By targeting specific pathogen components, they offer precise immune activation with fewer side effects, making them ideal for infectious diseases and cancer.

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As peptide therapeutics evolve, discovery and optimisation methods are becoming more sophisticated, enabling targeted treatments.

Peptide discovery and optimization techniques

Peptide discovery has advanced with tools like phage and mRNA display, enabling rapid generation of diverse, high-affinity peptide libraries. However, despite these advancements, screening and optimisation remain complex.

Cutting-edge techniques: phage and mRNA display technologies

Phage and mRNA display technologies have transformed peptide research by enabling rapid screening of vast libraries to identify high-affinity binders, driving major advances in drug discovery.

The table below outlines the core principles, advantages, and applications of these two leading peptide discovery platforms.

Feature/ aspect	Phage display technology	mRNA display technology
Basic principle	Peptides are displayed on the surface of bacteriophages (viruses that infect bacteria).	Peptides here are encoded by mRNA and displayed in vitro on ribosomes.
How it works	Gene encoding a peptide inserted into the phage genome Phage infects bacteria and expresses a peptide on its surface Phages are screened against targets to identify high-affinity binders	mRNA is translated into a peptide in vitro Peptide remains attached to its mRNA via the ribosome Peptides are screened for binding to target molecules
Library size	Large, diverse peptide libraries	Even larger and more complex libraries are possible
Specificity/Affinity	Identifies peptides with high specificity and affinity	Identifies high-affinity binders, including novel structures
Advantages	High diversity Well-established Useful for drug development and antibody discovery	Greater library complexity Better control over peptide folding Useful for novel peptide discovery
Applications	Drug development, protein/antibody interaction studies	Drug discovery, especially for complex or novel peptide structures
Notable uses	Discovery of peptides binding to proteins, antibodies, or other molecules	Identification of peptides for treating cancer, autoimmune disorders, and other diseases

Overcoming challenges in high-throughput screening and library development

While peptide discovery technologies have made huge strides, challenges remain in efficiently screening large peptide libraries and optimising them for specific therapeutic targets.

Screening bottlenecks:

Generating large peptide libraries is just the first step; screening for high-affinity peptides is the real challenge.
Advanced technologies like phage and mRNA display still result in time-consuming and resource-intensive screening.
Identifying peptides with desired specificity requires multiple selection rounds and complex assays.

Innovations in automation and AI:

To overcome these challenges, automation and AI are being increasingly integrated into the peptide discovery process.

Automation:

Robotic systems have automated parts of the screening process, speeding up sample handling.
Automated liquid handling reduces human error, increases throughput, and allows for hundreds or thousands of assays to run simultaneously.

AI and machine learning:

AI predicts peptide-target interactions, identifying promising candidates early.
Machine learning analyses screening datasets, uncovering patterns humans may miss.
AI integration with peptide display technologies predicts peptides likely to bind specific targets, reducing manual screening.

Also read: Understanding the gut microbiome: An introduction

Once peptides are discovered, the next focus is on strategies to enhance their stability and bioactivity, ensuring their long-term effectiveness as therapeutic agents.

Strategies to enhance peptide stability and bioactivity

Peptides are effective at targeting specific biological pathways but often face challenges related to stability and rapid degradation. To overcome these limitations, researchers use various chemical modifications that enhance peptide efficacy, bioactivity, and pharmacokinetics.

These strategies ensure peptides remain active in the body for extended periods.

1. Chemical modifications to improve efficacy

Cyclisation involves forming a covalent bond between the peptide's ends, creating a circular structure. This modification improves peptide stability by making it resistant to enzymatic breakdown. Cyclised peptides often exhibit:

Increased half-life in the bloodstream.
Better tissue penetration.
Enhanced resistance to degradation by enzymes.

D-amino acid substitution:
Peptides made of L-amino acids are susceptible to proteolytic degradation. Replacing L-amino acids with D-enantiomers (D-amino acids) increases resistance to enzymatic breakdown. This substitution results in:

More stable peptides with prolonged activity.
Improved bioactivity as peptides bind more effectively to their targets.

For example, D-penicillamine uses D-cysteine to reduce enzyme breakdown and improve pharmacokinetics in Wilson’s disease treatment.

2. Peptoids and N-methylation

Peptoids are synthetic polymers that resemble peptides but differ in structure. The side chains in peptoids are attached to the nitrogen atom of the backbone, making them more resistant to enzymatic degradation compared to peptides. Peptoids offer:

Enhanced stability and resistance to breakdown.
Better suitability for oral administration, unlike peptides that often require injections.
Potential applications in cancer treatment and antimicrobial therapies.

An example of this is cyclic peptoid-chemotherapy conjugates, which target cancer cells and deliver chemotherapy drugs with fewer side effects.

3. How N-methylation boosts peptide drug performance?

N-methylation adds a methyl group to the nitrogen atom in the peptide backbone. This small modification increases peptide stability and bioactivity.

Key benefits of N-methylation include:

Increased stability: Reduces susceptibility to proteolytic cleavage, allowing peptides to remain active in the body.
Enhanced blood-brain barrier penetration: Helps peptides cross barriers, making them suitable for neurological treatments.
Improved pharmacokinetics: Provides longer-lasting therapeutic effects and reduces dosing frequency, improving patient compliance.

For instance, N-methylated peptides used in Alzheimer’s treatment show enhanced stability and better targeting of amyloid plaques, with improved bioactivity and resistance to breakdown.

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To further improve peptide performance, computational and rational design methods are being employed to predict and refine peptide structures.

Computational and rational design in peptide discovery

Computational tools and rational design have enhanced peptide drug discovery by predicting peptide structures, optimising properties, and improving clinical trial success.

Artificial intelligence and machine learning in peptide design

Artificial intelligence (AI) and machine learning (ML) are key in peptide discovery, providing tools to predict peptide structures, functions, and binding affinities. AI algorithms analyse large datasets to identify patterns and predict which peptide sequences will bind effectively to their targets.

For example, in cancer research, AI models have identified peptides that bind to cancer cell markers, leading to the development of a peptide with high binding affinity. This helps researchers identify promising candidates early, saving time and costs in the drug development process.

The advantages of rational design methodologies in peptide drug development

Rational design employs a knowledge-based approach, utilising target protein data and peptide structure to inform the development process. Computational models and bioinformatics tools help optimize sequence properties, such as length, charge, and structure, for better binding and bioactivity.

Benefits of integrating computational models and bioinformatics tools include:

Faster identification of drug candidates: Computational models simulate peptide-target interactions, reducing the trial-and-error testing process
Improved targeting: Rational design enables more specific and compelling peptide therapeutics by understanding the molecular interactions between peptides and their targets
Cost efficiency: Predicting peptide behaviour before physical synthesis helps lower experimental costs and speeds up drug development

With peptides becoming more precisely designed, attention is shifting to innovative delivery systems that ensure these therapeutic peptides are efficiently transported to their targets.

Innovative delivery systems for peptide drugs

Peptide drugs face challenges like poor solubility, rapid degradation, and difficulty targeting specific tissues. Innovative delivery systems are being developed to improve peptide targeting and effectiveness.

1. Revolutionary chemical and biological delivery systems

Revolutionary delivery systems, such as nanoparticles and liposomes, help protect peptides from degradation, improve their stability, and ensure targeted delivery to specific tissues.

Nanoparticles: Their small size helps encapsulate peptides, improving solubility, protecting against degradation, and delivering them to specific tissues for longer-lasting effects.
Liposomes: These lipid-based spheres encapsulate peptides, enhancing solubility and stability while efficiently delivering both hydrophilic and hydrophobic peptides.

Addressing delivery challenges:

Poor solubility: Nanoparticles and liposomes improve the solubility of hydrophobic peptides, enhancing their effectiveness when administered orally or via injection.
Targeted tissue delivery: Both nanoparticles and liposomes can be engineered to target specific tissues, maximising therapeutic effects while minimising side effects on healthy tissues.
Protection from degradation: Encapsulation in nanoparticles or liposomes shields peptides from enzymatic degradation, allowing them to remain active in the body for longer periods.

2. Next-generation delivery methods

Next-generation methods, like microneedles and self-assembled peptide systems, offer innovative ways to improve peptide drug delivery. These approaches aim to enhance drug stability, simplify administration, and improve patient compliance.

Microneedles:

Microneedles provide a minimally invasive way to deliver peptides through the skin by creating microchannels for absorption. Ideal for peptides poorly suited to oral or IV routes, they’re being explored for conditions like diabetes that require continuous delivery.

Self-assembled peptide systems:

Self-assembling peptides represent a novel class of delivery systems that spontaneously form ordered structures under specific conditions. These systems can encapsulate peptides and gradually release them over time. The benefits include:

Improved drug stability: Self-assembly enhances peptide stability, helping maintain its effectiveness during storage and administration.
Controlled release: These systems offer the ability to control the release rate of peptides, providing sustained therapeutic effects and reducing the frequency of administration.
Enhanced patient compliance: With a slower release rate, patients can benefit from fewer doses, improving treatment adherence.

Also read: The science behind gut microbiome testing

While these innovative delivery methods are advancing peptide therapies, the field still faces challenges.

Challenges and opportunities in therapeutic peptide development

The peptide therapeutics market presents both opportunities and challenges. Success hinges on understanding market dynamics and effectively managing competition, costs, regulations, and access barriers.

1. Market dynamics and competitiveness in peptide therapeutics

Advances in peptide discovery, delivery, and biology are driving rapid market expansion. This growth intensifies competition among pharma giants and biotech startups developing next-gen peptide therapies.

Key players and partnerships:

Big pharmaceutical companies: Ipsen, Eli Lilly, and Novartis are investing heavily in peptide drug development, using their pipelines and financial strength to lead the market.
Biotech start-ups: Companies like Protagonist Therapeutics and Bachem drive innovation in peptide discovery, often partnering with larger firms for synthesis and scale.
Strategic partnerships: Collaborations between biotech firms and academic institutions, such as Novo Nordisk with UCL for diabetes research and Merck with Biosceptre for cancer research, are accelerating progress.

2. Pharmacoeconomic considerations in peptide therapy development

While peptide drugs offer several therapeutic advantages, there are huge financial and market-related challenges that need to be addressed for their widespread adoption.

Cost-effectiveness
Peptides are costlier to produce than small-molecule drugs due to complex synthesis, limiting their use in low-resource settings. Their precision and fewer side effects may lower overall healthcare costs by reducing hospitalisations and unnecessary treatments.
Market access and regulatory hurdles
Peptide drugs face strict regulatory demands that can delay market entry. Unlike small molecules, peptides must demonstrate safety, efficacy, stability, and scalability. Despite updated guidelines from the FDA and EMA, the process remains complex and costly.
Pricing and reimbursement
High production costs often result in higher drug prices, limiting access. To improve affordability and reach, companies must develop pricing and reimbursement strategies that balance development costs with accessibility, especially in underserved regions.

Also read: Gut Health and Diabetes: Could Your Microbiome Be the Key?

Peptide therapeutics are redefining what's possible in modern medicine by offering targeted, precise solutions for everything from chronic conditions to complex diseases. As technologies like AI, gene editing, and next-gen sequencing push discovery forward, peptides are becoming smarter, more stable, and more impactful than ever before.

The secret to utilising their complete potential lies in bridging innovation with accessibility, ensuring that the future of medicine is not just promising, but practical.

Curious about what’s next in peptide drug development?

Explore The Good Bug’s latest insights into therapeutic peptides, backed by science and curated by experts. Whether you’re tracking clinical advancements, exploring novel delivery systems, or are interested in how peptides are transforming disease treatment, we’re here to keep you informed.

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