On October 22, 2025 Onco3R Therapeutics, a clinical-stage immunology and oncology biotech company dedicated to transforming patients’ lives with best-in-class medicines, reported that it will present preclinical data from its FGFR3, SMARCA2 and P53 Y220C small molecules programs in 3 posters at the EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium on Molecular Targets and Cancer Therapeutics, taking place October 22-26, 2025, in Boston.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

"First generation precision medicines are often suboptimal in the clinic due to low target coverage, off-target toxicity and emergence of resistance. At Onco3R, our vision is to design best-in-class medicines to address the unmet needs left by first generation drugs and unlock the full potential of therapeutic targets" said François Gonzalvez, PhD, CSO and co-Founder of Onco3R Therapeutics.

"We are thrilled to present the first preclinical data from our lead oncology programs FGFR3, SMARCA2 and P53 Y220C. Each program has identified best-in-class molecules which offer the potential to deliver transformational efficacy and improved tolerability for patients. Our FGFR3 and SMARCA2 candidates, G-012 and G-141 respectively, have reached the optimum potency and selectivity profile to mitigate dose-limiting toxicities while maintaining maximum target coverage. This has translated into robust anti-tumor activity in vivo. The poster presentations will highlight data supporting the advancement of these two candidates towards the clinic, as well as the discovery of unique small molecule P53 reactivators."

"These compelling preclinical results further validate our patient-centric drug discovery approach, which integrates deep translational science with rational, structure-based and AI-augmented drug design", Pierre Raboisson, PhD, CEO and co-Founder of Onco3R Therapeutics said. "We look forward to advancing these two candidates and remain on track to initiate IND-enabling studies in mid-2026. The identification of these candidates, alongside the continued clinical progress of our SIK3 inhibitor O3R-5671 in autoimmune indications, reinforces Onco3R’s strong strategic position. With a robust pipeline and clear execution momentum, we are confidently advancing toward our next value-driving milestones."

Presentation details

Title: Discovery of Best-in-Class FGFR3 small molecule inhibitors with high isoform selectivity and activity against gatekeeper mutations

Session: Poster Session C

Session Date and Time: Saturday, October 25, 12:30-4pm

Presenting author: Sandrine Vendeville, PhD

Key findings from preclinical studies include:

G-012 demonstrated best-in-class potency and selectivity with favorable drug-like properties.

Based on translational modelling, the compound reached the optimal selectivity against other FGFR isoforms to mitigate off-target toxicity and maintain maximal target coverage.

G-012 showed robust anti-proliferative activity in FGFR3-driven cancer cells and induced significant tumor regression in vivo.

G-012 is currently advancing in 14 days toxicology studies.

IND-enabling studies are anticipated in mid-2026.

Title: Discovery of novel SMARCA2 small molecule inhibitors with best-in-class potency and selectivity for the treatment of SMARCA4-mutant cancers

Session: Poster Session C

Session Date and Time: Saturday, October 25, 12:30-4pm

Presenting author: Lijs Beke, PhD

Key findings from preclinical studies include:

G-141 combined best-in-class cellular potency and selectivity to allow optimal target coverage and unlock the full therapeutic potential of SMARCA2 inhibition.

The compound showed synthetic lethality in SMARCA4-deficient cells and induced robust anti-tumor activity in vivo without signs of SMARCA4-related toxicity.

G-141 showed favorable drug-like properties and is currently advancing in 14 days toxicology studies.

IND-enabling studies are anticipated in mid-2026.

Title: Discovery of a Best-in-Class small molecule p53 Y220C reactivator: Breaking through the potency ceiling

Session: Poster Session C

Session Date and Time: Saturday, October 25, 12:30-4pm

Presenting author: François Gonzalvez, PhD

Key findings from preclinical studies include:

Onco3R patient-centric drug discovery approach identified unique small molecule P53 reactivators with best-in-class cellular potency.

Onco3R leads exhibit the optimal potency and residence time to induce deep and sustain target engagement and fully unlock the tumor suppressive function of P53 in cells.

This translated into robust anti-proliferative activity in P53 Y220C mutant cancer cell lines (single digit nanomolar IC50s) and tumor regression in a Y220C P53 mutant xenograft model.

Further characterization of the lead candidates is ongoing.

(Press release, Onco3R Therapeutics, OCT 22, 2025, View Source [SID1234656951])