Bicycle Therapeutics and Cancer Research UK Announce Initiation of First Clinical Study of a Bicyclic Peptide (Bicycle®)

First patient dosed in Phase I/IIa clinical trial of BT1718 in
patients with advanced solid tumors

LONDON & CAMBRIDGE, United Kingdom & BOSTON–(BUSINESS WIRE)–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 tumors. 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
tumors.


“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 tumor 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
tumors.”

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, which this drug will be tested on. Supporting this type of
innovative clinical research is a key priority for Cancer Research UK.”

ABOUT BT1718

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 tumors. 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.

ABOUT BICYCLE THERAPEUTICS

Bicycle Therapeutics is developing a unique class of chemically
synthesized medicines based on its proprietary bicyclic peptide (Bicycle®)
product platform to address therapeutic needs unreachable with existing
treatment modalities. Bicycle’s internal focus is in oncology, where the
company is developing targeted cytotoxics (Bicycle Toxin Conjugates),
targeted innate immune activators and T-cell modulators for cancers of
high unmet medical need. Bicycles’ small size and exquisite
targeting deliver rapid tumor penetration and retention while clearance
rates and routes of elimination can be tuned to minimize exposure of
healthy tissue and bystander toxicities. The company’s lead program,
BT718, is being evaluated in a Phase I/IIa trial in collaboration with
Cancer Research, UK. The company’s unique intellectual property is based
on the work initiated at the MRC Laboratory of Molecular Biology in
Cambridge, U.K., by the scientific founders of the company, Sir Gregory
Winter and Professor Christian Heinis. Bicycle has its headquarters in
Cambridge, U.K., with many key functions and members of its leadership
team located in the biotech hub of Boston, Mass. For more information,
visit www.bicycletherapeutics.com or
follow us on Twitter at @Bicycle_tx.

ABOUT CANCER RESEARCH UK’S COMMERCIAL PARTNERSHIPS TEAM

Cancer Research UK is the world’s leading cancer charity dedicated to
saving lives through research. Our specialist Commercial Partnerships
Team work closely with leading international cancer scientists and their
institutes to protect intellectual property arising from their research
and to establish links with commercial partners. The team develop
promising ideas into successful cancer therapeutics, software, devices,
diagnostics and enabling technologies. This helps to accelerate progress
in exciting new discoveries in cancer research and bring new treatments
to patients sooner. http://commercial.cancerresearchuk.org/

Cancer Research UK’s commercial activity operates through Cancer
Research Technology Ltd. (CRT), a wholly owned subsidiary of Cancer
Research UK. It is the legal entity which pursues drug discovery
research in themed alliance partnerships and delivers varied commercial
partnering arrangements.

ABOUT CANCER RESEARCH UK’S CENTRE FOR DRUG DEVELOPMENT

Cancer Research UK has an impressive record of developing novel
treatments for cancer. The Cancer Research UK Centre for Drug
Development, formerly the Drug Development Office, has been pioneering
the development of new cancer treatments for 25 years, taking over 140
potential new anti-cancer agents into clinical trials in patients. It
currently has a portfolio of around 30 new anti-cancer agents in
preclinical development, Phase I or early Phase II clinical trials. Six
of these new agents have made it to market including temozolomide for
brain cancer, abiraterone for prostate cancer and rucaparib for ovarian
cancer. Two other drugs are in late development Phase III trials. This
rate of success is comparable to that of any pharmaceutical company.

ABOUT CANCER RESEARCH UK

  • Cancer Research UK is the world’s leading cancer charity dedicated to
    saving lives through research.
  • Cancer Research UK’s pioneering work into the prevention, diagnosis
    and treatment of cancer has helped save millions of lives.
  • Cancer Research UK receives no funding from the UK government for its
    life-saving research. Every step it makes towards beating cancer
    relies on vital donations from the public.
  • Cancer Research UK has been at the heart of the progress that has
    already seen survival in the UK double in the last 40 years.
  • Today, 2 in 4 people survive their cancer for at least 10 years.
    Cancer Research UK’s ambition is to accelerate progress so that by
    2034, 3 in 4 people will survive their cancer for at least 10 years.
  • Cancer Research UK supports research into all aspects of cancer
    through the work of over 4,000 scientists, doctors and nurses.
  • Together with its partners and supporters, Cancer Research UK’s vision
    is to bring forward the day when all cancers are cured.

For further information about Cancer Research UK’s work or to find
out how to support the charity, please call 0300 123 1022 or visit
www.cancerresearchuk.org.
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Contacts

Bicycle:
Media:
Ten Bridge Communications
Sarah
Sutton, +1-518-932-3680
Sarah@tenbridgecommunications.com
or
Investors:
Argot
Partners
Maeve Conneighton, +1-212-600-1902
maeve@argotpartners.com
or
Cancer
Research UK:

Kathryn Ingham in the Cancer Research UK press
office
0203 469 5475
Kathryn.ingham@cancer.org.uk