# Repurposing Itraconazole in Combination with Chemotherapy and Immune Checkpoint Inhibitor for Cancer

## TL;DR

This review explores using itraconazole, an antifungal drug, in combination with chemotherapy and immunotherapy to treat cancer, highlighting its potential and challenges.

## Contribution

The paper provides a comprehensive review of itraconazole's anticancer potential when combined with existing therapies, emphasizing mechanisms and clinical implications.

## Key findings

- Itraconazole shows anticancer activity across multiple tumor types when combined with other therapies.
- Combining itraconazole with chemotherapy and PD-1 inhibitors may enhance treatment through metabolic and immune pathway modulation.
- Drug interactions and toxicity remain key challenges for clinical translation.

## Abstract

Cancer remains a significant global health burden despite advances in diagnosis and treatment. In recent years, drug repurposing has emerged as a promising strategy in oncology, offering reduced costs and shorter development timelines compared with de novo drug discovery. Among repurposed agents, the antifungal drug itraconazole has demonstrated anticancer activity across multiple tumor types, particularly when used in combination with other therapeutic modalities. In this review, we summarize current preclinical and clinical evidence supporting the use of itraconazole in cancer therapy, with a specific focus on its combination with chemotherapeutic agents and programmed cell death protein 1 (PD-1) immune checkpoint inhibitors. We highlight proposed mechanisms underlying this synergy, including modulation of tumor metabolism, angiogenesis, and immune signaling pathways. Additionally, we discuss key challenges and limitations, such as drug–drug interactions and toxicity considerations, that must be addressed to optimize clinical translation. Overall, the combination of itraconazole with chemotherapy or anti-PD-1 therapy represents a promising therapeutic strategy warranting further investigation in well-designed trials.