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

 Biosion submitted the IND application for BSI-992, a TROP2 ADC, on April 9th, 2024 in China. The TROP2 targeting antibody, discovered by Biosion, was licensed to OBI Pharma in 2021. OBI ADC Technology OBI Pharma (台灣浩鼎) owns the ex-China right of BSI-992/OBI-992 , with the US FDA clearing  an IND application for a Phase 1/2 Study in Jan 2024. The phase 1 trial in the US is estimated to be completed in 2025Q2. Besides OBI-992, OBI Pharma has also discovered a next-generation anti-TROP2 ADC, OBI-902, using the GlycOBI platform in various drug-antibody ratios (DAR). Furthermore, a BsADC targeting TROP2 and HER2 is currently in the preclinical stage. BSI-992/ OBI-992 OBI-992 is a TROP2-directed antibody-drug-conjugate (ADC) that carries a potent topoisomerase I inhibitor and uses a hydrophilic, enzyme-cleavable linker. Upon binding to TROP2 on the surface of cancer cells, OBI-992 is internalized into the cell and trafficked to lysosomes where the linker is cleaved by cathepsin B, releasing

 Innovent has initiated a phase 1 study (NCT06349408 ) of IBI3001, a bispecific ADC that targets B7-H3 and EGFR, in patients with solid tumors. Additionally, Innovent is conducting a phase 1 trial ( NCT05774873 ) of IBI344, a bispecific antibody that also targets B7-H3 and EGFR. Schematic overview of crosstalk between the EGFR signaling and the B7/CD28 family Recent research has suggested that the overexpression of novel B7/CD28 family proteins, including B7-H3 may be linked to EGFR signaling and could potentially lead to resistance to EGFR-targeted treatments by promoting an immune-depressed environment within the tumor microenvironment. IBI3001 According to the statement by Innovent, IBI3001 is a  site-specifically glycan-conjugated ADC that consists of a topoisomerase I inhibitor  with  multiple anti-tumor mechanisms of action : (1) enhanced EGFR signaling blockade; (2) EGFR- and B7-H3-aided payload internalization and cytotoxicity; and (3) potent bystander killing effects of ADC.