Bicycle Therapeutics Announces the Publication of an Article Highlighting Preclinical Data for the BT7480 Program in the Journal of Medicinal Chemistry

CAMBRIDGE, England & BOSTON, July 12, 2022–(BUSINESS WIRE)–Bicycle Therapeutics plc (NASDAQ: BCYC), a biotechnology company pioneering a new, differentiated class of therapeutics based on its proprietary bicyclic peptide (Bike®) technology, today announced that a paper highlighting preclinical data for BT7480, a Bike Tumor Targeted Immune Cell Agonist® (Bike TICA™) targeting Nectin-4 and the agonizing CD137 (4-1BB), was published in the Journal of Medicinal Chemistry. The article, titled “Discovery and Optimization of a Synthetic Class of Nectin-4-Targeted CD137 Agonists for Immuno-oncology” is available in the publications section of Bicycle’s website at this address link.

“CD137 is a co-stimulatory receptor on immune cells that can drive anti-tumor immunity and Nectin-4 is a cell adhesion molecule that is overexpressed in a wide range of solid tumors. We discovered BT7480 using a series of new Bikes targeting CD137, which were conjugated to new Bikes targeting Nectin-4,” said Nicholas Keen, Ph.D., Chief Scientific Officer of Bicycle Therapeutics. unique – small size, reliance on binding to Nectin-4-bearing tumor cells for activity and very potent CD137 agonism. In addition, we have designed the molecule so that it can be dosed once a week in the clinic. We deployed a multi-pronged approach to optimize the molecule’s affinity for the two targets, linker length, linker stoichiometry, solubility, and pharmacokinetic properties. By exploring the valence of Bikes in rodent studies, the 1:2 Nectin-4/CD137 format has been shown to lead to a promising immune response in solid tumors. BT7480 is currently in Phase I development with dose escalation underway.”

About Bicycle Therapeutics

Bicycle Therapeutics (NASDAQ: BCYC) is a clinical-stage biopharmaceutical company developing a new class of drugs, called Bikesfor diseases underserved by existing therapies. Bikes are fully synthetic short peptides constrained by small molecule scaffolds to form two loops that stabilize their structural geometry. This constraint facilitates binding to the target with high affinity and selectivity, making Bikes attractive candidates for drug development. Bicycle is currently evaluating BT5528, a second-generation Bicycle Toxin Conjugate (BTC™) targeting EphA2; BT8009, a second-generation BTC targeting Nectin-4, a well-validated tumor antigen; and BT7480, a Bicycle TICA™ targeting Nectin-4 and stressful CD137, in company-sponsored Phase I/II trials. Additionally, BT1718, a BTC that targets MT1-MMP, is being studied in an ongoing Phase I/IIa clinical trial sponsored by the Cancer Research UK Center for Drug Development. Bicycle is headquartered in Cambridge, UK, with many key functions and members of its management team located in Lexington, Massachusetts. For more information, visit

Forward-looking statements

This press release may contain forward-looking statements made pursuant to the safe harbor provisions of the Private Securities Litigation Reform Act of 1995. Such statements may be identified by words such as “aims”, “anticipates”, “believes”, ” could, “estimate”, “expect”, “plan”, “goal”, “intend”, “may”, “plan”, “possible”, “potential”, “seek”, “will” and variations of these words or similar expressions intended to identify forward-looking statements, although not all forward-looking statements contain these words. Forward-looking statements in this press release include, but are not limited to, statements regarding Bicycle’s planned advancement of its product candidates, including BT7480; the progress of Bicycle’s product candidate pipeline; Bicycle’s planned design, initiation, enrollment and progress in clinical trials; the availability of clinical trial data; and the therapeutic potential of Bicycle’s product candidates. Bicycle may not achieve the plans, intentions or expectations disclosed in such forward-looking statements, and you should not place undue reliance on such forward-looking statements. Actual results or events could differ materially from the plans, intentions and expectations disclosed in these forward-looking statements due to a variety of factors, including: risks relating to the opening of the site, the start of the clinical trial, recruitment and follow-up patients, as well as Bicycle’s ability to meet other anticipated timelines and milestones presented by the ongoing COVID-19 pandemic; the uncertainties inherent in the initiation and completion of clinical trials and clinical development of Bicycle’s product candidates; the risk that Bicycle will not realize the anticipated benefits of its technology; availability and timing of clinical trial results; whether the results of preclinical studies will be predictive of the results of clinical trials; the risk that testing will be delayed and not yield satisfactory results; potential adverse effects resulting from testing or use of Bicycle’s product candidates; and other important factors, each of which could cause our actual results to differ from those contained in the forward-looking statements, are more fully described in the section titled “Risk Factors” in Bicycle’s Quarterly Report on Form 10- Q filed with the Securities and Exchange Commission (SEC) on May 5, 2022, as well as in other filings Bicycle may make with the SEC in the future. All forward-looking statements contained in this press release speak only as of the date hereof, and Bicycle expressly disclaims any obligation to update any forward-looking statements contained herein, whether as a result of new information, future events, changed circumstances or otherwise, except as otherwise required by law.

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