[EN] CONTROLLED-RELEASE TYROSINE KINASE INHIBITOR COMPOUNDS WITH LOCALIZED PK PROPERTIES<br/>[FR] COMPOSÉS INHIBITEURS DE TYROSINE KINASE À LIBÉRATION CONTRÔLÉE PRÉSENTANT DES PROPRIÉTÉS PHARMACOCINÉTIQUES LOCALISÉES
申请人:ASCENDIS PHARMA ONCOLOGY DIV A/S
公开号:WO2020254613A1
公开(公告)日:2020-12-24
The present invention relates to a water-insoluble controlled-release tyrosine kinase inhibitor ("TKI") compound for use in the treatment of a cell-proliferation disorder, wherein said water-insoluble controlled-release TKI compound releases one or more TKI drug, wherein the water-insoluble controlled-release TKI compound is administered by intra-tissue administration and wherein the total amount of TKI moieties and TKI drug molecules remaining locally in such tissue 3 days after said intra-tissue administration is at least 25% of the amount of TKI moieties or TKI drug molecules administered by said intra-tissue administration; and to related aspects.
本发明涉及一种水不溶性控释酪氨酸激酶抑制剂(“TKI”)化合物,用于治疗细胞增殖紊乱,其中所述水不溶性控释TKI化合物释放一种或多种TKI药物,所述水不溶性控释TKI化合物通过组织内给药给予,并且在所述组织内给药后的第3天,所述组织中残留的TKI基团和TKI药物分子的总量至少为所述组织内给药给予的TKI基团或TKI药物分子总量的25%;以及相关方面。