Drug intelligence / Profile preview

onvansertib + nanoliposomal irinotecan + leucovorin + fluorouracil

Development stage
Unknown
Lead developer
Cardiff Oncology
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

This regimen is an investigational **combination therapy** composed of four agents: - **Onvansertib** is a highly selective small-molecule inhibitor targeting *polo-like kinase 1 (PLK1)*, a serine/threonine kinase crucial for mitosis, which induces cell cycle arrest and apoptosis in cancer cells. - **Nanoliposomal irinotecan** is a liposome-encapsulated formulation of the topoisomerase I inhibitor irinotecan, designed for improved delivery and reduced toxicity, resulting in DNA damage and cell death. - **Leucovorin** (folinic acid) is a folate derivative that enhances the binding of fluorouracil to thymidylate synthase, potentiating its antimetabolite effect. - **Fluorouracil** (5-FU) is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA and RNA synthesis and leading to cancer cell death. This combination is being studied primarily in advanced or metastatic colorectal cancer, especially for *KRAS*-mutant or *RAS*-mutated cases that are resistant to other therapies. Early clinical evidence suggests enhanced antitumor activity and improved objective response rates compared to chemotherapy alone[1][3][5].

Brand names
N/A (this specific 4-drug combination has no unique brand name; individual components have brand names such as Onvansertib, Onivyde [for nanoliposomal irinotecan], Fusilev [for leucovorin], Adrucil [for 5-FU])
Other names
onvansertib + MM-398 + leucovorin + 5-FUonvansertib + nanoliposomal irinotecan + folinic acid + 5-FU
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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