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news.Belgium-based iTeos Therapeutics has filed its first patent applications protecting proprietary inhibitors of the intracellular enzyme TDO2, which is expressed at high levels in specific cancers.
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The company has partnered 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.
iTeos Therapeutics CEO Michel Detheux said the company is happy about realizing the potential of its small molecule immunomodulator discovery platform to create a new class of anti-cancer therapies in order to improve the benefits of conventional chemotherapy, immune checkpoint inhibition and/or therapeutic vaccination.
"We plan to move these TDO2 inhibitors forward to clinical stage as a first-in-class cancer immunotherapy," Detheux said.
The company has also started drug discovery programs on TDO2, and another enzyme expressed in cancer cells named IDO1, which are believed to contribute 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 signifies a paradigm shift in clinical oncology that assures to revolutionize the management of cancer.
The company said that indoleamine 2,3-dioxygenase (IDO1) and Tryptophan 2,3-dioxygenase (TDO2), major 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, so, specific inhibitors for each enzyme might have complementary therapeutic benefits.