Express bicyclic peptide-coupled immunotherapy, a new solid tumor targeting model has entered the clinic

▎Editor of WuXi AppTec's content team Today, Bicycle Therapeutics announced that its tumor-targeted immune cell agonist BT7480, designed based on bicyclic peptides, has completed the first patient administration in a phase 1/2 clinical trial
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BT7480 is an immune cell agonist targeting Nectin-4.
On the one hand, it can bind to Nectin-4 expressed on the surface of solid tumors, and it can also activate the costimulatory receptor CD137 expressed on the surface of immune cells
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Bicycle company uses bicyclic peptide technology 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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BT7480 is a potential "first-in-class" tumor-targeted immune cell agonist
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It is composed of three bicyclic peptides coupled, one bicyclic peptide can bind to Nectin-4, and the other two bicyclic peptides bind to CD137
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▲Schematic diagram of the structure of BT7480 (picture source: Reference [2]) In preclinical research, BT7480 can significantly change the tumor microenvironment, stimulate the infiltration of immune cells, and eliminate Nectin-4 expressing tumors in animals without continuous administration.

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▲BT7480 significantly reduces tumor size in animals (picture source: reference [2]) This phase 1/2 open-label clinical trial will be divided into two parts.
The first part will test the safety and tolerability of BT7480 and establish The recommended dose for phase 2 clinical trials
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Then the company plans to evaluate the effect of BT7480 as a single agent and in combination with the anti-PD-1 antibody nivolumab in the phase 2 clinical trial to treat patients with Nectin-4 positive cancer
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"BT7480 is our first bicyclic peptide tumor-targeted immune cell agonist that has entered the clinical development stage.
It represents a new type of tumor-targeting drug
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" said Dr.
Kevin Lee, CEO of Bicycle Therapeutics, "Nectin-4 is in It is highly expressed in a variety of common tumors and is associated with poor prognosis
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Activation of the costimulatory receptor CD137 can drive anti-tumor immune responses, but activation outside the tumor leads to toxicity
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Our preclinical studies have shown encouraging results We look forward to studying the safety and effectiveness of this unique therapy in clinical trials
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"References: [1] Bicycle Therapeutics Announces First Patient Dosed in Phase I/II Trial of Bicycle® Tumor-targeted Immune Cell Agonist™ BT7480 in Patients with Advanced Solid Tumors Associated with Nectin-4 Expression.
Retrieved November 4, 2021, from https://investors.
bicycletherapeutics.
com/news-releases/news-release-details/bicycle-therapeutics-announces-first-patient-dosed-phase-iii-1[2] Hurov et al.
, (2021).
BT7480 , a novel fully synthetic Bicycle tumor-targeted immune cell agonist™ (Bicycle TICA™) induces tumor localized CD137 agonism.
Journal of ImmunoTherapy of Cancer, http://dx.
doi.
org/10.
1136/jitc-2021-002883 The WuXi AppTec content team focuses on introducing global biomedical health research progress
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