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α4β7 integrin inhibitors: a patent review
Hao Li1, Shi-Ying Huang1, Fang-Hong Shi2
1a Department of Pharmacy , Shanghai Children's Medical Center, Shanghai Jiao Tong University School of Medicine , Shanghai , China.
Expert Opinion on Therapeutic Patents
|November 17, 2018
Summary
Alpha4beta7 integrin inhibitors show promise for treating various inflammatory diseases. Approved monoclonal antibodies like Natalizumab and Vedolizumab, alongside emerging small molecules and peptides, offer new therapeutic avenues.
Area of Science:
- Immunology
- Pharmacology
- Gastroenterology
Background:
- Alpha4beta7 integrin is a leukocyte cell surface receptor.
- Mucosal Addressing Cell Adhesion Molecule 1 (MAdCAM-1) is its exclusive ligand.
- This interaction is crucial in inflammatory processes.
Purpose of the Study:
- To review the discovery and development of alpha4beta7 integrin inhibitors.
- To explore their therapeutic applications in various immune-mediated diseases.
- To provide expert opinion on current and future treatments.
Main Methods:
- Review of scientific literature on alpha4beta7 integrin inhibitors.
- Analysis of clinical trial data for approved and investigational drugs.
- Synthesis of expert opinion on therapeutic potential.
Main Results:
- Monoclonal antibodies Natalizumab and Vedolizumab are clinically approved.
- Etrolizumab and AMG-181 are promising investigational antibodies targeting alpha4beta7.
- Small molecules (e.g., AJM300, CDP323) and peptide inhibitors show therapeutic potential.
Conclusions:
- Alpha4beta7 integrin inhibitors represent a significant therapeutic class.
- Diverse drug modalities are under investigation for inflammatory conditions.
- Targeting alpha4beta7 offers a promising strategy for immune-mediated diseases.
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