Bicycle Therapeutics Announces First Patient Dosed in Phase IIa Trial of Bicycle Toxin Conjugate BT1718

Bicycle Therapeutics plc (NASDAQ: BCYC), a biotechnology company pioneering a new and differentiated class of therapeutics based on its proprietary bicyclic peptide (Bicycle) technology, today announced that the first patient has been dosed in the Phase IIa expansion portion of the Phase I/IIa trial sponsored by Cancer Research UK, the world’s leading cancer charity dedicated to saving lives through research. The trial is evaluating BT1718 in patients with MT1-MMP-positive squamous non-small cell lung cancer (NSCLC) and a basket of other MT1-MMP-positive solid tumors.

“With the Phase IIa expansion, we look forward to building on the encouraging data generated through the Phase I dose escalation, in which BT1718 appeared tolerable with manageable adverse events and preliminary signs of anti-tumor activity were observed,” said Kevin Lee, Ph.D., Chief Executive Officer of Bicycle Therapeutics. “BT1718 is a Bicycle Toxin Conjugate, or BTC, that targets the antigen MT1-MMP, which was observed in our translational research to be highly expressed on the membrane of tumors of a squamous cell origin. Squamous NSCLC represents a key patient segment where there is a high unmet need for new treatment options, given the limitations of current therapies. We believe BT1718 represents a potential first-in-class therapy that could have significant potential in the treatment of squamous NSCLC, as well as more broadly across other MT1-MMP-expressing cancers with high unmet need.”

BT1718 is a BTC targeting MT1-MMP and is comprised of a mono-hindered disulfide cleavable linker and a cytotoxic DM1 payload. The Phase IIa expansion will evaluate BT1718 administered once weekly at the recommended Phase II dose (RP2D) of 20 mg/m² in an MT1-MMP-positive squamous NSCLC cohort, as well as in an MT1-MMP-positive solid tumor “basket” cohort. For the first time in the Phase I/IIa trial, patients will be preselected based on levels of antigen expression in target lesions, as determined by the Company’s proprietary clinical-grade MT1-MMP immunohistochemistry (IHC) assay. The primary objectives of the Phase IIa expansion portion are to evaluate the safety and tolerability profiles of BT1718. One of the secondary objectives is to assess anti-tumor response, as measured by RECIST criteria. The trial is sponsored by Cancer Research UK’s Centre for Drug Development and will be conducted at sites in the UK.