Phase I results provide additional clinical activity data for Bicycles

Bicycle Therapeutics, a biotechnology company pioneering a new class of therapeutics based on its proprietary bicyclic peptide (Bicycle®) technology, today announced the successful completion of Oxurion’s Phase I clinical trial evaluating the safety and tolerability of a single intravitreal injection of THR-149, a novel Bicycle-based plasma kallikrein (PKal) inhibitor, in patients with diabetic macular edema (DME). No dose-limiting toxicities or drug-related adverse events were reported. Activation of the PKal enzyme has been shown to increase retinal vascular permeability, microaneurysm and inflammation in DME.

This Phase I open-label, multi-center, non-randomized trial evaluated the safety of a single intravitreal injection of THR-149 at three ascending dose levels in 12 subjects with visual impairment due to center-involved DME. The study also investigated changes to patients’ best corrected visual acuity (BCVA). A rapid onset of action was observed from Day 1, with an increasing average improvement in BCVA of up to 7.5 letters at Day 14. This activity was maintained with an average improvement in BCVA of 6.5 letters at Day 90 following a single injection of THR-149.

“These trial results represent additional human clinical data generated using Bicycles, a new therapeutic modality developed using our proprietary technology. It is impressive to see sustained activity out to 90 days in patients after a single injection, providing further support for the use of Bicycles in the ophthalmic setting. The safety and tolerability of THR-149 provides evidence of the clinical potential of this modality as we advance BT1718, our proprietary Bicycle Toxin Conjugate, which is currently in a Phase I/IIa clinical trial,” said Kevin Lee, Ph.D., Chief Executive Officer of Bicycle Therapeutics. “Beyond our oncology programs, we are excited about the potential role that THR-149 may play for patients with DME. We look forward to building on our strong collaboration with Oxurion as the program moves into more advanced clinical development.”

“With these favorable safety and tolerability results and initial data illustrating the long duration of action that can be obtained following a single injection of THR-149, we will continue our innovative, Bicycle-based approach to potential treatments for DME,” said Patrik De Haes, M.D., Chief Executive Officer of Oxurion.

In 2013, Bicycle entered into a research collaboration and license agreement with Oxurion (OXUR.NX) related to the discovery and development of novel human plasma kallikrein inhibitors for use in ophthalmic indications.

About Bicycle Therapeutics

Bicycle Therapeutics (BCYC) is a clinical-stage biopharmaceutical company developing a novel class of medicines, referred to as Bicycles®, for diseases that are underserved by existing therapeutics. Bicycles are fully synthetic short peptides constrained with small molecule scaffolds to form two loops that stabilize their structural geometry. This constraint facilitates target binding with high affinity and selectivity, making Bicycles attractive candidates for drug development. Bicycle’s lead product candidate, BT1718, is a BicycleToxin Conjugate being investigated in an ongoing Phase I/IIa clinical trial in collaboration with the Centre for Drug Development of Cancer Research UK. Bicycle is headquartered in Cambridge, U.K. with many key functions and members of its leadership team located in Lexington, MA. For more information, visit BicycleTherapeutics.com, connect with us on LinkedIn and follow us on Twitter at @Bicycle_tx.

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. These statements may be identified by words such as “aims,” “anticipates,” “believes,” “could,” “estimates,” “expects,” “forecasts”, “goal,” “intends,” “may” “plans,” “possible,” “potential,” “seeks,” “will,” and variations of these words or similar expressions that are intended to identify forward-looking statements. All statements other than statements of historical facts contained in this presentation are forward-looking statements, including statements regarding our collaboration with Oxurion; the therapeutic potential for Bicycles in ophthalmology and oncology; the discovery of potential product candidates using our technology; and the development of potential product candidates.