Drug intelligence / Profile preview

apatinib + temozolomide + etoposide

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

Overview

Apatinib + temozolomide + etoposide is an investigational combination regimen composed of three small molecule chemotherapeutic agents. Apatinib is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), exerting antiangiogenic effects by blocking VEGF-mediated signaling and thus inhibiting tumor blood vessel formation. Temozolomide is an oral alkylating agent that induces DNA damage through methylation, leading to tumor cell death, and is commonly used in the treatment of gliomas and other brain tumors. Etoposide is a topoisomerase II inhibitor that causes DNA strand breaks, preventing cell division and promoting apoptosis; it has broad use in various solid tumors including lung cancer, lymphoma, neuroblastoma, and glioblastoma multiforme[6][10]. This triple-drug combination has been explored primarily in clinical trials for relapsed or refractory neuroblastoma as well as other advanced cancers. The rationale for combining these agents lies in their complementary mechanisms—antiangiogenesis (apatinib), DNA alkylation (temozolomide), and inhibition of DNA repair/replication (etoposide)—to enhance antitumor efficacy.

Other names
apatinib combined with temozolomide and etoposide
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TOP2A (DNA topoisomerase II)DNA

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