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iTeos Therapeutics SA Files Patent for Immunomodulators in Cancer Immunotherapy

February 10, 2014

GOSSELIES, Belgium, February 10, 2014 /PRNewswire/ –

iTeos Therapeutics SA today announced the filing of the Company’s first patent
applications protecting proprietary inhibitors of the intracellular enzyme TDO2, which is
expressed at high levels in specific cancers. iTeos Therapeutics has collaborated with
Ludwig Cancer Research over the last year to identify small molecule inhibitors of the
enzyme that display nanomolar potency, good selectivity, favorable pharmacokinetics
profiles in rodents and activity in pharmacodynamic models.

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“We are excited about realizing the potential of our small molecule immunomodulator
discovery platform to create a new class of anti-cancer therapies in order to enhance the
benefits of conventional chemotherapy, immune checkpoint inhibition and/or therapeutic
vaccination,” said Michel Detheux, Ph.D., CEO of iTeos Therapeutics. “We plan to move
these TDO2 inhibitors forward to clinical stage as a first-in-class cancer immunotherapy.”

iTeos has initiated drug discovery programs on TDO2, and another enzyme expressed in
cancer cells named IDO1. These enzymes are believed to contribute significantly to the
ability of tumors to resist both natural and therapeutically induced immune attack,
including responses elicited by immune checkpoint inhibitors and therapeutic vaccines.
Immunotherapy represents a paradigm shift in clinical oncology that promises to
revolutionize the management of cancer. Yet not all patients respond equally to such
strategies. As such, inhibitors of TDO2 and IDO1 have the potential to significantly
increase the response rate to a variety of immunotherapies.

About TDO2 and IDO1

Indoleamine 2,3-dioxygenase (IDO1) and Tryptophan 2,3-dioxygenase (TDO2), key enzymes
in tryptophan catabolism, are constitutively expressed in many cancers, which often
express one of the two enzymes. Their elevated expression in tumors locally degrades the
amino acid tryptophan, blunting tumor surveillance by the immune system and so preventing
tumor rejection. Therefore, specific inhibitors for each enzyme might have complementary
therapeutic benefits.

About iTeos Therapeutics SA

Based in Gosselies, Belgium, iTeos Therapeutics SA (
http://www.iteostherapeutics.com) is a private biotechnology company targeting
metabolism of the tumor microenvironment to develop small-molecule immunomodulators for
cancer treatment. Originating from a partnership between Ludwig Cancer Research and de
Duve Institute at the Universite Catholique de Louvain, iTeos Therapeutics SA raised EUR9M
in April 2012, to build a discovery platform combining expertise in tumor immunology,
immunotherapy, drug discovery and development.


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SOURCE iTeos Therapeutics SA


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