Drug intelligence / Profile preview

LY3295668 erbumine + topotecan + cyclophosphamide

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral (LY3295668 Erbumine), Intravenous (topotecan, Cyclophosphamide)
01

Overview

LY3295668 erbumine + topotecan + cyclophosphamide is a combination therapy under clinical investigation primarily for relapsed or refractory neuroblastoma in pediatric patients. - **LY3295668 erbumine** is a selective small molecule inhibitor of Aurora kinase A, an enzyme frequently overexpressed in cancers and implicated in cell cycle regulation, mitosis, and tumorigenesis. By inhibiting Aurora kinase A, it aims to halt proliferation and induce apoptotic cell death in tumor cells[3][4]. - **Topotecan** is a small molecule chemotherapy agent classified as a topoisomerase I inhibitor, which induces cytotoxicity by interfering with DNA replication, resulting in DNA strand breaks and cell death. - **Cyclophosphamide** is a small molecule alkylating chemotherapy agent that cross-links DNA, preventing cell division and causing cell death. The combination has demonstrated manageable safety profiles, with myelosuppression as the most common high-grade adverse event. Clinical responses such as partial response and stable disease have been observed, and phase 1 dose-escalation studies have established a recommended phase 2 dosage for combination therapy[4][6][7]. Eli Lilly and Company is the developer and sponsor for LY3295668 erbumine[4][6], while topotecan and cyclophosphamide are widely available chemotherapy agents produced by various pharmaceutical manufacturers. Primary clinical investigations focus on relapsed/refractory neuroblastoma in children, though LY3295668 erbumine alone or in other combinations is also investigated in various cancers[4][6][7].

Other names
LY3295668 erbumine + topotecan + cyclophosphamide
02

Targets

AURKA (Aurora kinase A)DNAAURKB (Aurora kinase B)TOP1 (DNA Topoisomerase I)

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