CBX

 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

 3H (Suzhou) Pharmaceuticals (思康睿奇药业) commences its first-in-human study ( NCT06287918 ) of 3HP-2827, an FGFR2 inhibitor, in patients with solid tumors exhibiting FGFR2 alterations in the United States. The clinical trial aims to enroll an estimated 130 participants. 3HP-2827 The Investigational New Drug (IND) application was submitted to the China Center for Drug Evaluation (CDE) on December 30, 2023. The IND has been approved for use either as monotherapy or in combination with chemotherapy or immunotherapy in patients with advanced cancers. Additional IND applications will be filed in East Asian countries. The FGFR2 belongs to the FGFR family of tyrosine kinase receptors. The family consists of 4 genes that encode single-pass transmembrane receptors that bind to FGF on the extracellular domain. Ligand binding trigger a signaling cascade that may exercise several cellular functions, including cell survival. It is estimated that FGFR2 genomic alterations are present in around 10-15%