Drug intelligence / Profile preview

alisertib + fluorouracil + oxaliplatin

Development stage
Preclinical
Lead developer
Puma Biotechnology
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of three chemotherapeutic agents: - **Alisertib** is a selective small molecule inhibitor of Aurora kinase A. It disrupts mitosis and inhibits tumor cell proliferation by blocking the activity of this serine/threonine kinase involved in cell cycle regulation. - **Fluorouracil (5-FU)** is an antimetabolite that interferes with DNA synthesis by inhibiting thymidylate synthase, leading to cytotoxicity in rapidly dividing cells. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks and inhibits DNA replication and transcription. While combinations such as FOLFOX (fluorouracil + oxaliplatin + folinic acid) are established for gastrointestinal cancers[2][3], the specific combination of alisertib with fluorouracil and oxaliplatin represents an investigational approach. Alisertib has been studied primarily in breast cancer and other solid tumors but not widely reported as combined specifically with both fluorouracil and oxaliplatin. The rationale for combining these agents would be to target multiple pathways involved in tumor growth—cell cycle regulation (alisertib), nucleotide synthesis inhibition (fluorouracil), and DNA damage induction (oxaliplatin).

02

Targets

DNATS (Thymidylate synthase)AURKA (Aurora kinase A)

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