inupadenant (EOS-850)

P1, N=57, Completed, iTeos Therapeutics | Recruiting --> Completed | Trial completion date: Nov 2023 --> May 2024 | Trial primary completion date: Oct 2023 --> May 2024

P1, N=119, Completed, iTeos Therapeutics | Active, not recruiting --> Completed | Trial primary completion date: Jun 2023 --> May 2024

P1/2, N=153, Active, not recruiting, iTeos Belgium SA | Recruiting --> Active, not recruiting | N=254 --> 153 | Trial completion date: Jan 2025 --> Jul 2025

P1/2, N=254, Recruiting, iTeos Belgium SA | N=376 --> 254 | Trial completion date: Sep 2024 --> Jan 2025 | Trial primary completion date: Jan 2024 --> Sep 2024

Using B cells derived from peripheral blood, the A2AR agonist CGS-21680 was shown to inhibit the maturation of B cells into plasma cells, and that maturation could be fully restored by inupadenant. This is in line with recent reports showing that B cells, plasma cells and tertiary lymphoid structures are associated with favorable responses to cancer immunotherapy. Interestingly, four out of the five non-progressors treated with inupadenant as monotherapy and with available biomarker data showed a reduction in ASC infiltration after inupadenant treatment, suggesting that inupadenant may promote terminal plasma cell differentiation and migration out of the tumor tissue and to the bone marrow.Altogether, these data support a novel plasma cell-centric mechanism of action of inupadenant, which may complement its reported T cell-mediated anti-tumor activity.

P1/2, N=276, Recruiting, iTeos Belgium SA

Inupadenant monotherapy was generally well-tolerated as of the DCO at a dose of 80 mg twice daily with initial evidence of clinical benefit, including 2 durable PRs in patients who have exhausted standard treatment options . Analysis of pre-treatment tumor biopsies has identified the A2A receptor as a biomarker which may be associated with clinical benefit.