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Updated: Oct 16, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Bicyclic Peptide Makes Targeting EphA2 Possible

    Cancer Discovery
    |October 20, 2021
    PubMed

    Insights

    A novel bicyclic peptide, BT5528, shows promise for cancer treatment by targeting EphA2. Early trials indicate clinical responses in ovarian and urothelial cancers without significant toxicity.

    Area of Science:

    • Oncology
    • Molecular Biology
    • Drug Development

    Background:

    • EphA2 receptor tyrosine kinase is a promising cancer target.
    • Previous EphA2-directed therapies faced toxicity challenges.
    • Tumor-penetrating peptides offer a novel delivery mechanism.

    Purpose of the Study:

    • To evaluate the safety and efficacy of BT5528, a novel bicyclic peptide targeting EphA2.
    • To assess the therapeutic potential of BT5528 in patients with advanced cancers.

    Main Methods:

    • Phase I clinical trial.
    • Administration of BT5528 to patients with ovarian and urothelial cancers.
    • Monitoring for clinical responses and toxicity.

    Main Results:

    • BT5528 demonstrated clinical responses in three patients.
    • The therapeutic candidate showed an acceptable safety profile.
    • No significant toxicity issues were observed, unlike previous EphA2-directed agents.

    Conclusions:

    • BT5528 represents a potential breakthrough in targeting EphA2 for cancer therapy.
    • The drug's tumor-penetrating capabilities and favorable safety profile warrant further investigation.

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