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1. Definition of Peptide Drugs

Peptides are compounds composed of multiple amino acids linked together by peptide bonds, typically consisting of 2 to 50 amino acid residues. Their linkage pattern is identical to that of proteins, and their molecular weight generally falls below 10,000 Daltons. Peptides are widely involved in regulating the physiological functions of various systems, organs, tissues, and cells within the human body, playing essential roles in biological processes.

Peptide drugs, synthesized through modern biological or chemical technologies, represent a unique class of therapeutics situated between large-molecule protein drugs and small-molecule chemical drugs. They possess the ability to modulate cellular biological functions and are applicable in disease prevention, diagnosis, and treatment. A detailed comparison of their properties is provided in the table below.

Table 1. Comparison of Peptide Drugs with Traditional Small-Molecule Chemical Drugs and Protein-Based Biologics

2. Market Size Analysis of Peptide Drugs

According to data from Nature, peptide drugs accounted for approximately 5% of the global pharmaceutical market as of 2019 (Figure 1). Primarily used for the treatment of chronic diseases, peptide therapeutics are currently concentrated in seven major therapeutic areas: rare diseases, oncology, diabetes (endocrinology and metabolic disorders), gastrointestinal diseases, orthopedics, immunology, and cardiovascular diseases. Among these, rare diseases, oncology, and diabetes serve as the “three key drivers” of peptide drug market growth (Figure 2).

Data from Frost & Sullivan projects that the global peptide therapeutics market will reach USD 210.8 billion by 2030, with the Chinese market maintaining a roughly 15% share of the global total (Figure 3).

3. Synthesis Methods and Characteristics of Peptide Drugs

Peptide drugs are generally synthesized through either biological methods or chemical synthesis. Among these, solid-phase peptide synthesis (SPPS) has become the mainstream approach for peptide drug manufacturing.

4. Chemical Modification Strategies for Peptide Drugs

Peptide drug discovery suffers limitations, including:

• Metabolically unstable because of cleavage by proteolytic enzymes

• Rapid clearance because of metabolism by enzymes

• Poor oral bioavailability because of metabolic instability

• Poor solubility of few peptides because of high hydrophobic character

• Poor membrane permeability owing to presence of charge and hydrophilic or polar amino acids

These constitutional physicochemical properties affected the progression of peptide therapeutics, and major challenges include the development of orally administered analogs. Consequently, research focusing on the development of peptide carriers or delivery systems and novel dosage forms has expedited the introduction of more peptide-based drugs to the market. Furthermore, pharmacokinetic characteristics, including absorption, half-life, metabolism, and bioavailability of the peptides, can be modulated by using various structural modifications. Frequently used approaches for peptide structural modulation include: (i) backbone modifications, such as depsipeptide, azapeptide, endothiopeptide, retro-inverso peptide, fluoroalkene, and replacement of amide bonds with triazole or oxetane; (ii) modification of the N or C terminus by N-alkylation, N-heterocyclic conjugation, Cesterification or amidation; and (iii) macrocyclization of the peptide using head to tail, side chain to side chain, head to side chain, and side chain to tail via ring-closing metathesis, cross-coupling reactions, ligation strategies, and stapling. Additionally, techniques such as replacement of natural amino acids with unnatural or modified amino acids, synthesis of peptidomimetics, and peptide conjugates via PEGylation and lipidation are also frequently used.

The permeability and bioavailability of peptides can be increased by substituting them with groups such as glycosyl or lipids (Figure 4). Thus, such progress in synthetic chemistry tools has expedited peptide-based investigations.

5. FDA-Approved Therapeutic Peptides in Recent Years

6. Peptide-Related Transactions

In recent years, major transactions and acquisitions in the peptide field—including peptide–drug conjugates (PDCs)—have primarily occurred between MNCs (or large pharmaceutical companies) and biotechs. Key players involved include Novo Nordisk, AstraZeneca, Roche, AbbVie, and Hengrui Pharma, with deal values exceeding USD 2 billion.

7. Chemexpress Peptide Capability

ChemExpress is a full-service CRO & CDMO offering end-to-end solutions from R&D to commercialization, providing flexible peptide service models including FTE/FFS, Process development, CMC and CDMO . Our peptide services include high-throughput solid-phase synthesis, solid-phase synthesis, liquid-phase synthesis, custom synthesis, peptide modification, and GMP manufacturing. With 10+ years of experience and facilities meeting FDA, EMA, and NMPA standards, we support projects from milligram-scale research to kilogram-scale commercial manufacturing. Leveraging our integrated payload-linker capabilities, we have extended our services to the R&D and production of PDC (Peptide-Drug Conjugate).

1 2023 Overview of China's Peptide Drug Industry – Frost & Sullivan & LeadLeo

2 https://doi.org/10.1038/s41573-020-00135-8

3 https://doi.org/10.1007/s00726-025-03454-5

4 Company Press Release