Express bicyclic peptides accurately deliver cytotoxic drugs and treat bladder cancer and ovarian cancer with positive clinical results

▎Bicycle Therapeutics, editor of WuXi AppTec's content team, announced today that two new-generation bicyclic peptide-conjugated toxins have shown positive anti-cancer activity in phase 1 clinical trials
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Among them, the bicyclic peptide-conjugated toxin BT5528 that targets EphA2 allowed two patients with urothelial cancer to obtain partial remission, reaching 80% disease control rate in ovarian cancer patients
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Bicycle company uses bicyclic peptide technology (named Bicycle) to develop differentiated therapies
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Bicyclic peptide molecules combine the characteristics of antibodies, small molecule drugs and peptides, and have similar affinity and specificity to antibodies; at the same time, they have a small molecular weight and can penetrate tissues quickly and deeply; their peptide properties provide The adjustable half-life of pharmacokinetics and renal clearance pathways avoid the common liver and gastrointestinal toxicity in other drug forms
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BT5528 is a bicyclic peptide-conjugated toxin targeting EphA2
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EphA2 is overexpressed in a variety of difficult-to-treat tumors and regulates cell migration, proliferation and differentiation
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Previously, the development of antibody-conjugated drugs for this target has not achieved ideal results
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▲Introduction to BT5528 (picture source: Bicycle Therapeutics company official website) In this phase 1 clinical trial, cancer patients who had received a variety of pre-treatments (median number of treatments were 7) received BT5528 treatment
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Preliminary anti-cancer activity was observed in patients with urothelial cancer and ovarian cancer: two patients with urothelial cancer received treatment, and they both achieved partial remission
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Eight patients with ovarian cancer received treatment, of which five patients were confirmed to be EphA2 positive by immunohistochemical tests
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Among these 5 patients, 4 patients (80%) observed anti-cancer activity, and one patient achieved partial remission
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The company's BT8009 is a bicyclic peptide-conjugated toxin targeting Nectin-4
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Preliminary clinical trial data showed that among 11 patients with urothelial cancer treated with two different doses of BT8009, 4 patients (36%) achieved partial remission, with tumor shrinkage between 37% and 89%
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▲Tumor changes in patients treated with BT8009 (picture source: Bicycle Therapeutics official website) "These data support the bicyclic peptide platform to provide a potential differential delivery of toxins
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" Bicycle Therapeutics CEO Dr.
Kevin Lee said
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▲Bicyclic peptide-based immuno-oncology therapy (picture source: Bicycle Therapeutics company official website) In addition to coupling toxins, the company’s R&D pipeline also includes bispecific bicyclic peptide molecules that can simultaneously bind to tumor antigens and CD137.
They are expected to become A new generation of immuno-oncology therapies
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Bicycle company has also reached cooperation with companies such as Roche and Ionis Pharmaceuticals to develop innovative bicyclic peptide coupling therapies
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Reference: [1] Bicycle Therapeutics Announces Interim BT5528 Phase I Clinical Trial Results and Preliminary Results from Ongoing BT8009 Phase I Clinical Trial.
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