Peptoid Therapeutics: The $5B Breakthrough Set to Disrupt Drug Engineering by 2028 (2025)
Table of Contents
- Executive Summary & 2025 Industry Snapshot
- Critical Advances in Peptoid Synthesis and Engineering
- Key Players and Emerging Startups: Company Profiles & Official Initiatives
- Market Size, Growth Drivers, and 2025–2028 Forecasts
- Therapeutic Applications: Oncology, Infectious Diseases, and Beyond
- Regulatory Landscape and Clinical Pipeline Analysis
- Strategic Partnerships, Licensing, and M&A Activity
- Manufacturing Innovations and Supply Chain Challenges
- Competitive Benchmarking: Peptoids vs. Peptides and Other Modalities
- Vision 2028: Future Trends, Investment Opportunities, and Innovation Outlook
- Sources & References
Executive Summary & 2025 Industry Snapshot
Peptoid-based therapeutics engineering is poised for significant advancements in 2025, driven by the unique biochemical properties of peptoids—N-substituted glycine oligomers that offer enhanced protease resistance, bioavailability, and tunable structures compared to traditional peptides. The global focus on next-generation biologics and the search for novel modalities to tackle drug resistance and undruggable targets are propelling the peptoid therapeutics sector into a new phase of translational and commercial maturation.
The most notable event in the past year has been the acceleration of clinical-stage peptoid programs, particularly in oncology, infectious diseases, and immunomodulation. Companies like Entelechon GmbH and Peptoid Technologies have reported successful optimization of peptoid scaffolds for lead candidates, leveraging the inherent chemical diversity and manufacturability of peptoids for rapid pipeline expansion. Meanwhile, Creative Peptides and GenScript Biotech Corporation have expanded their custom synthesis and screening services to support the growing demand from both pharmaceutical and biotech innovators.
Major pharmaceutical companies are increasingly forming partnerships and licensing agreements with specialized peptoid engineering firms to access proprietary libraries and platform technologies. The ease of solid-phase synthesis and the cost-effective scalability of peptoids have enabled preclinical projects to rapidly transition toward IND-enabling studies. For example, Bachem Holding AG has begun integrating peptoid synthesis capabilities into its peptide manufacturing portfolio, reflecting broader industry trends toward hybrid peptide-peptoid modalities.
In 2025, the regulatory outlook remains cautiously optimistic. The U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have provided clearer guidance on the clinical evaluation of non-natural oligomers, including peptoids, facilitating the design of first-in-human trials and supporting safety assessments. Leading contract research organizations are also establishing specialized assay platforms for peptoid-based candidates, with Evotec SE expanding peptoid-specific ADME and toxicology services.
Looking forward, the next few years are expected to see several peptoid-based drugs enter Phase I/II clinical trials, with pipeline visibility expanding across anti-infectives, anticancer, and rare disease indications. Industry experts anticipate that combinatorial libraries, AI-guided design, and high-throughput screening partnerships will further accelerate peptoid-based therapeutics engineering. The sector’s progress in 2025 positions it as a critical contributor to the broader field of engineered therapeutics, with commercial launches possible before 2030.
Critical Advances in Peptoid Synthesis and Engineering
Peptoid-based therapeutics have emerged as a transformative class of molecules in drug discovery, owing to their protease resistance, tunable pharmacokinetics, and structural diversity. In 2025, scientific and industry efforts are accelerating the translation of peptoid research into engineered therapeutics with clinical potential. Advances in solid-phase synthesis—particularly submonomer approaches—have enabled the rapid assembly of highly diverse peptoid libraries, facilitating the identification of bioactive candidates with improved drug-like properties.
Key players such as Peptoids, Inc. and Creative Peptides are at the forefront of commercializing custom peptoid synthesis and optimizing monomer design for enhanced pharmacological profiles. These organizations are leveraging automated synthesizers and novel monomer chemistries to generate peptoids with tailored physicochemical and biological characteristics, expanding the landscape of functional scaffolds for therapeutic intervention.
Recent data indicate that engineered peptoids can target protein-protein interactions previously considered “undruggable,” offering new avenues for intervention in oncology, infectious disease, and immunomodulation. In 2024 and early 2025, several preclinical programs have reported promising activity of peptoid-based compounds against multidrug-resistant bacteria and as inhibitors of viral entry in emerging infectious diseases. Companies such as Polyphor are actively developing peptoid-derived macrocycles and peptidomimetics for antimicrobial applications, leveraging the inherent stability and specificity of these molecules.
Another critical frontier is the engineering of peptoid-drug conjugates and multifunctional peptoid scaffolds for targeted delivery. Custom conjugation platforms offered by Creative Peptides are enabling the attachment of imaging agents or cytotoxins, advancing the field of precision medicine. Additionally, peptoid-based hydrogels and self-assembling materials are being explored for controlled release and tissue engineering, with companies like Bachem providing specialized building blocks and expertise.
Looking ahead to the next few years, the outlook for peptoid-based therapeutics is robust. The maturation of high-throughput screening technologies and machine-learning-guided design are anticipated to further accelerate hit identification and optimization. As more candidates progress toward clinical trials, collaboration between biotech firms and academic consortia is expected to intensify, consolidating peptoids’ role as a next-generation therapeutic platform.
Key Players and Emerging Startups: Company Profiles & Official Initiatives
Peptoid-based therapeutics engineering is gaining momentum as a transformative field in the discovery and development of next-generation drugs. As of 2025, several established biotechnology firms and innovative startups are driving progress, harnessing the unique properties of peptoids—synthetic oligomers that mimic peptides but offer enhanced stability and bioavailability. This section profiles key players and highlights official initiatives shaping the sector’s immediate outlook.
- AMS Biotechnology (AMSBIO): AMSBIO is a significant supplier of custom peptoid synthesis and libraries, supporting drug discovery programs globally. In 2024, AMSBIO expanded its peptoid library services, enabling researchers to access structurally diverse peptoid scaffolds for screening and lead optimization in therapeutic development.
- Peptoid Technologies: As a dedicated peptoid-focused company, Peptoid Technologies specializes in the design and contract synthesis of peptoid-based molecules for pharmaceutical and biotech partners. In recent years, the company has announced collaborations with academic labs and pharma companies to co-develop peptoid drug candidates targeting infectious diseases and oncology, with several preclinical candidates expected to enter IND-enabling studies by late 2025.
- Pepscan: Traditionally known for peptide engineering, Pepscan has officially integrated peptoid synthesis into its offering, reflecting the growing demand for peptoid-based therapeutics. Their proprietary CLIPS™ technology is now being applied to stabilize peptoid structures, which could accelerate the development of peptoid drugs with improved pharmacological profiles.
- Creative Peptides: Creative Peptides has expanded its custom synthesis portfolio to include peptoid analogues, supporting both early-stage research and larger-scale production. Their investment in advanced solid-phase synthesis technologies is expected to streamline the scale-up of clinical-grade peptoid candidates in the next few years.
- Thermo Fisher Scientific: Through its peptide and custom chemistry divisions, Thermo Fisher Scientific now provides peptoid building blocks and analytical services. In 2025, the company launched an initiative to supply GMP-grade peptoids, supporting translational research and early clinical trials for peptoid-based drugs.
Looking ahead, the peptoid therapeutics landscape is poised for accelerated growth as these leading companies invest in manufacturing, high-throughput screening, and translational partnerships. The emergence of specialized startups and expanded offerings by established suppliers signals an ecosystem ready to support rapid clinical advancement of peptoid-based drug candidates, with oncology, infectious disease, and inflammation as key focus areas for the years immediately ahead.
Market Size, Growth Drivers, and 2025–2028 Forecasts
The market for peptoid-based therapeutics is gaining significant momentum as of 2025, propelled by advancements in peptoid synthesis and their unique properties—such as protease resistance and enhanced bioavailability—that address key limitations of conventional peptide drugs. Global pharmaceutical and biotechnology firms have increased investments in developing peptoid analogues for applications ranging from infectious disease to oncology and neurodegenerative disorders. This accelerating innovation is reflected in expanded preclinical and early clinical pipelines, as peptoids are increasingly recognized for their drug-like properties and tunable pharmacokinetics.
Several key drivers underpin this market’s growth trajectory. First, peptoids’ inherent resistance to enzymatic degradation is enabling the design of orally available therapeutics, a critical advantage over traditional peptides. Second, the versatility of peptoid chemistry allows for the rapid generation of diverse compound libraries, supporting high-throughput screening and structure-activity relationship studies. Third, ongoing challenges such as antimicrobial resistance and the need for novel cancer therapeutics are fueling demand for new molecular scaffolds with improved efficacy and safety profiles. Notably, the U.S. Food and Drug Administration has granted fast-track and orphan drug designations to select peptoid candidates, signaling regulatory openness to these novel modalities.
Recent years have seen notable activity from both established firms and startups in the peptoid space. For instance, AMS Biotechnology has expanded its catalog of peptoid building blocks and screening services to support drug discovery efforts. Meanwhile, Creative Peptides and Genemed Synthesis Inc. have reported increased demand for custom peptoid synthesis among pharmaceutical partners. On the therapeutic front, companies such as Polyphor and Peptoid Technologies are advancing proprietary peptoid candidates targeting unmet needs in infectious disease and oncology.
Looking ahead to 2025–2028, industry consensus points to robust market expansion, with compound annual growth rates projected in the double digits as pipeline candidates move through clinical development. Continued progress in scalable synthesis and improved delivery technologies are expected to further accelerate commercialization timelines. Strategic collaborations between drug developers and service providers will likely intensify, fostering a dynamic ecosystem for peptoid-based innovation. As clinical validation grows, peptoid therapeutics are poised to transition from niche applications to mainstream pharmaceutical portfolios, offering new options for patients and healthcare systems worldwide.
Therapeutic Applications: Oncology, Infectious Diseases, and Beyond
Peptoid-based therapeutics, synthetic oligomers structurally similar to peptides but with side chains attached to the nitrogen atom of the peptide backbone, are gaining significant momentum in the fields of oncology, infectious diseases, and related therapeutic areas. The current landscape in 2025 reflects a maturation of foundational research and a growing roster of clinical and preclinical programs leveraging the unique properties of peptoids: protease resistance, tunable bioactivity, and favorable pharmacokinetics.
In oncology, peptoid therapeutics are being engineered to overcome critical challenges such as tumor penetration, target specificity, and resistance mechanisms. Companies like AMS Biotechnology (AMSBIO) and Creative Peptides are actively developing peptoid libraries and custom synthesis solutions to accelerate the identification of anti-cancer candidates with high selectivity for tumor-associated antigens. AMSBIO, for instance, is supporting the design of peptoid-based ligands for targeted drug delivery and imaging applications, which are expected to move into advanced preclinical phases in the next 1-2 years.
For infectious diseases, the protease-resistant nature of peptoids offers a distinct advantage in developing novel antimicrobials, especially against multidrug-resistant pathogens. Pepscan has reported progress in engineering antimicrobial peptoids that disrupt bacterial membranes while sparing mammalian cells, with several candidates in late-stage in vitro assessment as of early 2025. Additionally, Bachem has expanded its peptoid synthesis capabilities to support the scale-up required for preclinical and clinical studies, reflecting the growing demand for these scaffolds in anti-infective pipelines.
Beyond oncology and infectious diseases, peptoid-based therapeutics are being explored for immunomodulation, fibrosis, and neurodegenerative diseases. GenScript reports collaborations with biotech startups to design peptoid-based inhibitors of protein-protein interactions implicated in autoimmune and fibrotic disorders. Early animal studies suggest that these compounds can achieve tissue penetration and bioavailability unattainable by traditional peptides.
Looking ahead, the next few years are expected to see several peptoid-based candidates entering first-in-human trials, particularly in oncology and infectious disease indications. Advances in solid-phase synthesis, high-throughput screening, and structure-based design—enabled by suppliers such as Creative Peptides and Bachem—will likely accelerate discovery timelines. As regulatory agencies increase their familiarity with peptoid scaffolds, the path to clinical translation is anticipated to become more streamlined, bolstering the case for peptoids as a new therapeutic class in precision medicine.
Regulatory Landscape and Clinical Pipeline Analysis
The regulatory landscape for peptoid-based therapeutics is rapidly evolving, driven by growing interest in the unique pharmacological properties of peptoids—N-substituted glycine oligomers that offer enhanced stability, bioavailability, and resistance to proteolytic degradation compared to traditional peptides. In 2025, regulatory agencies such as the U.S. Food and Drug Administration and the European Medicines Agency are actively engaged in defining frameworks for the preclinical and clinical evaluation of these novel modalities, drawing on analogies to peptide drugs while recognizing the structural and functional distinctions of peptoids.
Several companies are now advancing peptoid-based candidates into clinical development. Peptoid Technologies, a leader in the field, has initiated Phase I trials for a peptoid-derived antimicrobial targeting multidrug-resistant infections, with preliminary data expected by late 2025. Similarly, Alyra Therapeutics is preparing to submit an Investigational New Drug (IND) application for its peptoid candidate designed to modulate immune responses in autoimmune diseases. These efforts align with increasing regulatory clarity around standards for absorption, distribution, metabolism, and excretion (ADME) profiling and immunogenicity assessment specific to peptoid molecules.
On the manufacturing front, advances in solid-phase synthesis and purification—spearheaded by specialized firms such as Creative Peptides—have enabled scalable production of clinical-grade peptoids, a key requirement for regulatory submission. Regulatory bodies are scrutinizing process validation, impurity profiling, and batch consistency, emphasizing the need for robust analytical methods tailored to peptoid chemistry.
Looking ahead, the outlook for peptoid-based therapeutics is promising. The pipeline is expanding beyond infectious and autoimmune diseases, with companies like Peptone leveraging advanced computational modeling to identify peptoid candidates for oncology and rare disease indications. Regulatory agencies are expected to issue further guidance on nonclinical safety requirements and clinical endpoints as more IND applications are submitted in 2025 and beyond. Close collaboration between industry and regulators will remain critical to address the unique challenges and accelerate the translation of peptoid-based drugs from bench to bedside.
Strategic Partnerships, Licensing, and M&A Activity
The peptoid-based therapeutics sector is witnessing a surge in strategic partnerships, licensing agreements, and M&A activity as biotechnology companies and pharmaceutical giants seek to capitalize on the unique properties of peptoids—synthetic oligomers that mimic peptides but exhibit enhanced stability and bioavailability. As of 2025, industry leaders and emerging biotech firms are leveraging collaborative strategies to accelerate the clinical development and commercialization of peptoid-based drugs, particularly in oncology, infectious diseases, and rare disorders.
A significant event in recent years was the expansion of Peptoid Technologies, Inc., a pioneer in peptoid discovery platforms, which entered into a multi-year research collaboration with Genentech in late 2024. The agreement aims to co-develop novel peptoid-based therapeutics for difficult-to-treat cancers, leveraging high-throughput screening and advanced structure-activity relationship (SAR) analytics. Under the collaboration, Genentech is providing upfront funding, with milestone payments and royalties tied to clinical progression, marking one of the largest financial commitments to peptoid technology to date.
In licensing news, Polyphor Ltd. has expanded its portfolio beyond macrocyclic peptides by signing a global licensing agreement with Novartis for a series of peptoid-based antimicrobials in early 2025. This agreement grants Novartis worldwide rights to develop, manufacture, and commercialize select assets targeting multidrug-resistant Gram-negative bacteria, with Polyphor retaining co-development rights in Europe. The deal reflects a growing trend among multinational pharmaceutical firms to diversify their small-molecule pipelines with peptoid derivatives, which offer improved resistance to proteolytic degradation and favorable pharmacokinetics.
M&A activity has also intensified, notably with AmyNeuro Sciences acquiring the peptide and peptoid platform assets of Proteus, Inc. in the first quarter of 2025. This acquisition is set to bolster AmyNeuro’s neurological disease pipeline, combining proprietary delivery technologies with next-generation peptoid candidates for neurodegenerative disorders.
Looking ahead, industry analysts anticipate continued consolidation and strategic deal-making as peptoid therapeutics advance through late-stage clinical trials. The versatility of peptoids as modulators of protein-protein interactions makes them attractive assets for companies seeking differentiated therapies. As patent landscapes evolve and more clinical data emerges, it is expected that both established pharmaceutical corporations and innovative startups will intensify their focus on licensing and M&A to secure leadership in this promising therapeutic class.
Manufacturing Innovations and Supply Chain Challenges
Manufacturing innovations and supply chain optimization are emerging as pivotal factors for the commercialization of peptoid-based therapeutics in 2025 and beyond. Peptoids—N-substituted glycine oligomers—offer compelling advantages over traditional peptides, such as increased protease resistance and enhanced bioavailability, but their unique chemical structure requires specialized manufacturing processes.
Recent advances in solid-phase synthesis have greatly improved the efficiency and scalability of peptoid production. Automated synthesizers leveraging sub-monomer protocols now enable rapid parallel synthesis of diverse peptoid libraries, facilitating high-throughput screening for drug candidates. Companies like BioMer and Creative Peptides have expanded their custom synthesis services to include peptoid chains with precise sequence control, supporting both research and preclinical pipelines. These innovations are critical for reducing lead times and lowering costs associated with early-stage drug development.
However, the transition from laboratory-scale synthesis to large-scale good manufacturing practice (GMP) production remains a key challenge. The need for specialized reagents and purification techniques—such as high-performance liquid chromatography (HPLC) adapted for peptoid separation—can create bottlenecks in supply chains. Merck KGaA (MilliporeSigma) and Thermo Fisher Scientific have responded by expanding their portfolios of GMP-grade monomers and resin supports, and by developing dedicated purification protocols for peptoid APIs, thus supporting scale-up for clinical trial material.
The outlook for 2025 suggests that the integration of continuous flow chemistry and automation will further streamline peptoid manufacturing. Companies such as Amerigo Scientific are investing in modular synthesis platforms, which promise to enhance batch consistency and reduce human error. Furthermore, the adoption of digital supply chain management platforms—capable of real-time tracking of raw material sourcing, production status, and quality control—will be essential to minimize disruptions and ensure regulatory compliance.
Despite these advances, ongoing risks remain related to raw material availability, logistics, and quality assurance, particularly as peptoid therapeutics transition into late-stage clinical trials and eventual commercialization. Cross-sector collaborations between contract manufacturers, chemical suppliers, and pharmaceutical developers will be necessary to build resilient, transparent supply chains that can accommodate the unique requirements of peptoid-based drugs.
Competitive Benchmarking: Peptoids vs. Peptides and Other Modalities
Peptoid-based therapeutics have garnered increasing attention in recent years due to their unique structural and functional advantages over traditional peptides and alternative therapeutic modalities. As of 2025, competitive benchmarking of peptoids versus peptides and other classes such as small molecules, antibodies, and nucleic acid therapeutics reveals several distinct trends and emerging data.
Peptoids, or N-substituted glycines, differ from peptides in that their side chains are attached to the nitrogen atom of the peptide backbone, rather than the alpha carbon. This structural modification imparts resistance to proteolytic degradation, a major limitation of traditional peptide drugs. Benchmarking studies from 2023–2025 show that peptoids exhibit substantially improved metabolic stability and serum half-lives compared to linear and even some cyclic peptides, as demonstrated in preclinical models cited by industry leaders such as AMS Biotechnology (AMSBIO), which supplies peptoid building blocks and reports on their stability profiles.
In terms of biological activity and druggability, peptoids can be engineered to mimic protein secondary structures, enabling them to target a broader range of protein–protein interactions compared to small molecules. This has prompted pharmaceutical companies such as Peptoid Technologies to advance their proprietary peptoid libraries for oncology and immunology indications, citing enhanced binding affinity and selectivity in comparison to analogous peptide scaffolds.
Compared to antibody-based therapeutics, peptoids offer advantages in manufacturability and cost. Their fully synthetic production circumvents the need for recombinant expression systems, and their modularity facilitates rapid structure–activity relationship (SAR) exploration. For instance, Bachem, a global manufacturer of peptides and peptoids, highlights the scalability and flexibility of peptoid synthesis, which supports faster preclinical optimization cycles relative to biologics.
- Peptoids vs. Peptides: Peptoids display superior protease resistance and tunable pharmacokinetics, making them attractive for chronic indications where peptide drugs historically fail due to rapid clearance.
- Peptoids vs. Small Molecules: Peptoids can access larger, flatter protein interfaces, which are generally inaccessible to small molecules, expanding the targetable proteome.
- Peptoids vs. Biologics: Peptoids offer synthetic accessibility, lower immunogenicity, and the potential for oral delivery, in contrast to the complex manufacturing and delivery challenges associated with antibodies.
Looking forward to the next few years, the competitive advantage of peptoid-based therapeutics is expected to be reinforced by ongoing investments in screening technologies and medicinal chemistry optimization platforms. Companies such as MilliporeSigma (part of Merck KGaA, Darmstadt, Germany) are expanding their catalog of peptoid reagents and synthesis tools, anticipating greater adoption in both drug discovery pipelines and translational research. The next wave of clinical candidates will provide crucial data on the translatability of peptoid advantages into human efficacy and safety, setting the stage for head-to-head comparisons with established peptide and biologic drugs.
Vision 2028: Future Trends, Investment Opportunities, and Innovation Outlook
As we move into 2025, the landscape for peptoid-based therapeutics engineering is poised for significant transformation, driven by advances in synthetic chemistry, enhanced computational design, and increasing clinical validation. Peptoids—N-substituted glycine oligomers—are gaining momentum as promising alternatives to peptides, offering improved proteolytic stability, cell permeability, and tunable bioactivity. These attributes are catalyzing a surge in both academic and industrial interest, positioning peptoids as a next-generation platform for therapeutic development across oncology, infectious diseases, and autoimmune disorders.
Current investment flows and strategic partnerships underscore the field’s momentum. Notably, Peptoid Technologies, Inc. and Creative Peptides have expanded their peptoid synthesis and screening capabilities, enabling rapid iteration and optimization of therapeutic candidates. In parallel, GenScript Biotech Corporation has integrated peptoid libraries into its high-throughput drug discovery services, while ChemGenes Corporation continues to scale up custom peptoid manufacturing, supporting both research and early clinical programs.
Emerging data from preclinical and early-phase clinical studies are fueling optimism for peptoid-based drug candidates. Several peptoid molecules have demonstrated robust activity against drug-resistant bacteria and viral pathogens, as well as selective modulation of protein-protein interactions implicated in cancer and neurodegenerative diseases. For instance, Peptoid Technologies, Inc. has reported promising in vivo efficacy data for its lead anti-infective peptoids, with plans to initiate IND-enabling studies by late 2025.
Looking toward 2028, the peptoid therapeutics sector is expected to benefit from continued innovation in automated solid-phase synthesis, AI-driven sequence optimization, and structure-based drug design. Partnerships between peptoid specialists and major pharma companies are anticipated to accelerate, particularly as peptoid analogs address limitations of current peptide and small molecule drugs. Regulatory progress, including formal guidance for peptoid-based IND submissions, will be crucial for translating preclinical promise into approved therapeutics.
- Expansion of peptoid-focused venture funding, with dedicated funds emerging for synthetic biology and novel drug modalities.
- Broader clinical exploration of peptoid conjugates—such as peptoid-antibody and peptoid-nanoparticle systems—for targeted delivery and improved pharmacokinetics.
- Integration of peptoid scaffolds in immunotherapy, antimicrobial resistance, and rare disease pipelines by leading developers.
In summary, the next few years are set to witness a robust maturation of peptoid-based therapeutics engineering, with new opportunities for investment and innovation catalyzed by a confluence of technological, regulatory, and market drivers.
Sources & References
- Creative Peptides
- Bachem Holding AG
- Evotec SE
- Polyphor
- Genemed Synthesis Inc.
- European Medicines Agency
- Alyra Therapeutics
- Novartis
- BioMer
- Thermo Fisher Scientific
- Amerigo Scientific