Company: HMDCF
Filing Date: 2025-03-19
Form Type: 20-F
Source: 0001410578-25-000377
Chunk: 425

Company: HUTCHMED (China) Ltd
Filing Date: 2025-03-19
Form: 20-F
Item: Item 4
Chunk 425
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 NMIBC; 15-20% MIBC)
​       ​   Salivary adenoid cystic (n/a)   ​   Lung squamous (3%)                         ​   Cervical (5%)                      
​       ​   Breast (1%)                     ​   Glioblastoma (3-7%)                        ​   ​                                  
​       ​   ​                               ​   Myeloma (15-20%)                           ​   ​                                  

Source:   M. Touat et al., “Targeting FGFR Signaling in Cancer,” Clinical Cancer Research (2015); 21(12); 2684-94.
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Fanregratinib Pre-clinical Evidence
Preclinical data of fanregratinib was presented at AACR 2023. Fanregratinib potently inhibited the tyrosine kinase activities of recombinant FGFR 1, 2, and 3 in vitro (IC50 values of 6, 4, and 6 nM, respectively) with weaker activity against FGFR4 (IC50 = 425 nM). It selectively inhibited proliferation of tumor cell lines with dysregulated FGFR signaling (GI50: 3~105 nM) compared with cell lines lacking FGFR aberrations (GI50: > 1.5 μM). Oral administration could induce time- and dose-dependent inhibition of phosphorylation of FGFR and resulted in remarkable and dose-dependent anti-tumor activity in multiple FGFR-altered tumor models. Fanregratinib at a dose of 50 mg/kg/day could induce tumor regression in most tumor models tested. It significantly improved anti-tumor activity of anti-PD-1 antibody in a FGFR2 fusion model by priming the immune environment. Fanregratinib has good pharmacokinetic properties characterized by rapid absorption following oral dosing, good bioavailability, moderate tissue distribution and moderate clearance in all pre-clinical animal species. Fanregratinib was found to have little inhibitory effect on major cytochrome P450 enzymes, indicating low likelihood of drug-to-drug interaction issues.
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Fanregratinib Clinical Development

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Treatment                                            Patient Focus                  Sites       Phase       Status/Plan                                                          NCT #      
Fanregratinib                                    ​   2L IHCC with FGFR fusion   ​   China