5-fluorouracil + imiquimod

The combination of 5-fluorouracil (5-FU) and imiquimod is a topical therapy used primarily for the treatment of actinic keratoses (AKs) and has also been explored for cutaneous squamous cell carcinoma in situ. This regimen leverages the distinct but complementary mechanisms of both agents to enhance efficacy compared to monotherapy. - **5-fluorouracil** is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and repair, leading to apoptosis in rapidly dividing cells such as precancerous or cancerous keratinocytes. It can also incorporate into RNA, interfering with nucleic acid function[4][3]. - **Imiquimod** is an immune response modifier that acts as a toll-like receptor 7 agonist, stimulating local cytokine production (including interferon-alpha, interleukins, and TNF-alpha), which enhances innate and adaptive immune responses against abnormal skin cells[6][10]. The combination aims to maximize cellular destruction through direct cytotoxicity (from 5-FU) while simultaneously harnessing the immune system for clearance of dysplastic or malignant cells (via imiquimod). Clinical studies suggest this dual approach may be more effective than either agent alone for field cancerization therapy in AKs[4][1][9].

Other names

5-FU + imiquimodfluorouracil + imiquimod