Cancer Research UK and Bicycle Therapeutics, a biotechnology company pioneering a new class of therapeutics based on its proprietary bicyclic peptide (Bicycle) product platform, announced today that the first patient has been dosed in their phase I/IIa trial evaluating BT1718 in patients with advanced solid tumours. BT1718 is a first-in-class Bicycle Toxin Conjugate being developed by Bicycle Therapeutics that targets Membrane Type 1 Matrix Metalloproteinase (MT1-MMP/MMP-14), which has been shown to be highly expressed in solid tumours.

“The initiation of this study is a landmark event for the company and for our technology,” said Maria Koehler, M.D., Ph.D., chief medical officer of Bicycle Therapeutics. “BT1718 is the first clinical candidate from our pipeline of Bicycles, a brand-new class of chemically synthesized medicines. We believe that Bicycles, because of their small size and exquisite selectivity, could provide meaningful efficacy to patients suffering from cancer and avoid the toxicities associated with other classes of highly potent anti-cancer drugs. We are delighted to be exploring its potential in collaboration with Cancer Research UK.”

The approximately 120-patient phase I/IIa trial is designed to evaluate the safety and preliminary efficacy of BT1718 in patients with high expression of tumour MT1, as measured by a proprietary MT1 immunochemistry assay. Following a rapid dose escalation phase, the phase I/IIa trial will evaluate two schedules of BT1718.

“We are excited to initiate this clinical study of BT1718, the first in a promising new class of potent anticancer agents with strong potential to deliver a meaningful therapeutic impact,” said Dr. Udai Banaji, Principal Investigator for the phase I/IIa trial. “Our team is eager to evaluate this important new therapeutic in patients with advanced solid tumours.”

Dr. Nigel Blackburn, Cancer Research UK’s director of drug development, said: “BT1718 is a potentially transformative treatment that has shown great promise in preclinical studies, and trials like this are a big step towards helping more patients survive their cancer.  We urgently need new, safe and effective therapies for patients with hard to treat cancers such as non-small cell lung cancer and triple negative breast cancer that this drug will tested on. Supporting this type of innovative clinical research is a key priority for Cancer Research UK.”

BT1718 is a first-in-class Bicycle Toxin Conjugate being developed by Bicycle Therapeutics that targets Membrane Type 1 Matrix Metalloproteinase (MT1-MMP), also known as MMP-14, which has an established role in cell invasion and metastasis, is linked to poor outcomes and is over expressed in many solid tumours. BT1718 has demonstrated promising target-dependent efficacy in preclinical models, including both cell- and patient-derived xenografts that are resistant to treatment with standards of care. In addition, it shows only a subset of the toxicities typically associated with other highly potent cancer treatments.

Cancer Research UK’s Centre for Drug Development (CDD) is sponsoring a phase I/IIa study of BT1718. The trial is co-managed by Cancer Research UK and Bicycle Therapeutics. Under the terms of the agreement, Bicycle retains the right to further advance the BT1718 program, at which point an undisclosed payment split between cash and equity, success based milestones and royalty payments would be made to Cancer Research UK.