Jitsubo’s strategies for overcoming the fundamental issues involved in commercializing peptide therapeutics

1st generation
  :year 1920~

図解

Sequence containing natural amino acids
 

Special features

  • Structured with natural amino acids
  • Normally with no chemical modification
  • More than 50 products in the market

2nd generation
  :year 2000~

図解

Sequence containing unnatural amino acids and structure modifications

Special features

  • Including unnatural amino acids and chemically modified molecules
  • Structurally constrained peptides (e.g. bridged peptides)
  • Requirement for advanced control during manufacturing over 1st generation

Challenges involved in commercializing peptide therapeutics

  1. Pharmaceutical ingredient costs are higher than those for small molecules
  2. Administering methods are mainly restricted to injections
  3. Structural optimization options are limited compared to small molecules

Jitsubo’s strategy

1st generation peptides

  1. Provide high-quality active pharmaceutical ingredients with low manufacturing costs
  2. Develop non-injection administering methods in order to supply therapeutics that are less of a burden on patients

Jitsubo’s strategy

2nd generation peptides

Using our unrivalled molecular structure optimization technology, Jitsubo can provide the ‘best-in-class’ peptide therapeutics with improved pharmaceutical characteristics, such as target selectivity and stability, offering ways to satisfy unmet medical needs

The discovery of peptide therapeutics can be divided into two major historical stages. The 1st generation of peptide therapeutics were based on peptide hormone sequences with the regulation of functions controlled in vivo. The 2nd generation began when sequences were found using synthetic lead compound discovery techniques, particularly display technologies, without any relation to hormone sequences discovered in vivo. By 2015, most peptide therapeutics available on the market were 1st generation products, but the proportion of 2nd generation pharmaceuticals among new drugs is expected to increase in the future.

To commercialize peptide therapeutics, regardless of the product generation, businesses face the same challenge: the costs of pharmaceutical ingredients are higher than those for small molecule drugs, even though both can be produced by chemical synthesis. This is especially true for 2nd generation therapeutics, which are structurally more complex and tend to have higher compositions of unnatural amino acids.

Another common challenge is to develop new drug administration routes, which are now mainly restricted to injections. As protein fragments, peptides are easily broken down into amino acids when ingested, representing a challenge for unmodified peptides, making it difficult to deliver them through oral administration. Furthermore, even once inside the systemic circulation, peptides are readily degraded by a multitude of enzymes. Consequently, since their stability is so low, peptides are most effectively administered via injection, with intravenous injection and hypodermic injection.

To commercialize 1st generation peptide therapeutics, Jitsubo is working to develop generic drugs and products offering improved administering methods. To accomplish this, our strategy is to make the most of our core technologies, which enable us to manufacture peptides at a significantly lower cost compared to existing technologies.

To commercialize 2nd generation peptide therapeutics, we intend to utilize our molecular structure optimization technology, which is aided by our peptide manufacturing technology. In this way, the company will work to discover new drugs and launch them as ‘best-in-class’ peptide therapeutics on the market.