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Showing posts with the label Lirafugratinib

Acerand Therapeutics has submitted the IND application for ACE-16229210, an FGFR2 inhibitor

 Acerand Therapeutics submitted an IND application for FGFR2  inhibitor ACE-16229210, its second candidate to enter clinical trials. The ACE-86225106 PARP1 inhibitor clinical trial enrolled its first patient in March 2024. FGFR pathway and inhibitors ACE-16229210 Recently, Acerand presented the preclinical results at the AACR Annual Meeting. ACE-16229210 potently inhibits FGFR2 (IC 50 = 6.2 nM) with excellent selectivity (>133-fold) over FGFR1 and FGFR4. It also potently (IC 50 <1 nM) and selectively (≥500-fold) inhibits FGFR2-induced ERK phosphorylation in multiple cancer cell lines harboring FGFR2 fusions, amplification, and mutations, but not those harboring FGFR1, FGFR3, or FGFR4 genetic alterations (IC 50 > 460 nM). This molecule shows a robust broad spectrum of antitumor activity with significant tumor regression at low doses (1-10 mg/kg) in several tumor xenograft and PDX models representing the major FGFR2 relevant tumor histologies including gastric, breast, ovari