Recently, she was invited to talk about her work at NIH, and Mealey is the only veterinarian among researchers studying how to improve
brain penetration of HIV drugs.
This asset is one of five IDO1 inhibitors in clinical development worldwide and EOS200271 is the only IDO1 inhibitor with
excellent brain penetration confirmed in patients.
iTeos is now developing EOS200271 which is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1), which has demonstrated the same anti-tumour activity in multiple preclinical tumour models in combination with immune checkpoint inhibitors as competitors, but also has demonstrated
superior brain penetration.
Pfizer initiated a Phase 1 clinical study for EOS200271 (NCT02764151) as a single agent in patients with malignant gliomas (brain cancer), an area of significant unmet need, based
on brain penetration of the compound.
While EOS200271 was originally licensed from iTeos to Pfizer in December 2014, the candidate was returned to iTeos at the end of 2017, after demonstrating interim data from 17 patients which confirmed the safety and
brain penetration of EOS200271 at doses ranging up to 500 mg BID.
This asset is one of four IDO1 inhibitors in clinical development worldwide and EOS200271 is the only IDO1 inhibitor with
excellent brain penetration.
«We wondered whether we could make a safer and more tolerable form of DON by enhancing
its brain penetration and limiting its exposure to the rest of the body and, thus, toxicity,» says Barbara Slusher, Ph.D., professor of neurology, medicine, psychiatry, neuroscience and oncology at the Johns Hopkins University School of Medicine and director of Johns Hopkins Drug Discovery.
Some preliminary pharmicokinetics has been performed in mice, showing
no brain penetration.
Interim data from 17 patients confirmed the safety and
brain penetration of EOS200271 at doses ranging up to 500 mg BID, the maximum dose tested by Pfizer in the study.