Drug intelligence / Profile preview

apatinib + pirarubicin + ifosfamide

Development stage
Preclinical
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Apatinib + pirarubicin + ifosfamide is an investigational combination therapy involving three agents with distinct mechanisms of action, primarily evaluated in the context of advanced or refractory solid tumors such as osteosarcoma and metastatic cancers. **Apatinib** is a small-molecule tyrosine kinase inhibitor highly selective for vascular endothelial growth factor receptor-2 (VEGFR-2), blocking angiogenesis and restricting tumor blood supply. **Pirarubicin** is an anthracycline antineoplastic agent structurally related to doxorubicin, functioning as a DNA intercalator and topoisomerase II inhibitor, resulting in double-strand DNA breaks and apoptosis. **Ifosfamide** is an alkylating agent from the oxazaphosphorine class, inducing DNA crosslinking and inhibition of DNA replication, leading to cell death. This combination is typically explored when tumors progress despite standard chemotherapy. While apatinib monotherapy shows activity in advanced osteosarcoma, combinations with chemotherapy, including pirarubicin and ifosfamide, are being tested for potentially improved outcomes in chemo-refractory disease[1][4].

02

Targets

DNAVEGFR2 (Vascular endothelial growth factor receptor 2)TOP2A (DNA topoisomerase II)

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