Clinical Efficacy of 5-Fluorouracil and Bleomycin in Dermatology - Review

Sep 21, 2026

Uploaded by Logic

Bleomycin and 5-fluorouracil (5-FU) are widely used antineoplastic agents in dermatology that act by blocking the cell cycle. Topical and intralesional formulations have been examined across non-neoplastic and cancerous lesions, but head-to-head comparative data remain limited. This review summarizes their action mechanisms, compares clinical efficacy across hypertrophic scar, warts, skin cancer, vascular malformation, hemangioma, and vitiligo, and evaluates overall safety.

LanguageEnglish

CategoryResearch & Report

FormatPDF

Pages13

Reading Time33 min

AccessFree to download

Abstract

Introduction

Materials and Methods

Results

Review Clinical Efficacy of 5-Fluorouracil and Bleomycin in Dermatology Suyeon Kim , Yu Ri Woo , Sang Hyun Cho , Jeong Deuk Lee and Hei Sung Kim * Citation: Kim, S.; Woo, Y.R.; Cho, S.H.; Lee, J.D.; Kim, H.S. Clinical Efficacy of 5-Fluorouracil and Bleomycin in Dermatology. J. Clin. Med. 2024, 13, 335. [https://doi.org/10.3390/](https://doi.org/10.3390/)[ ](https://doi.org/10.3390/)jcm13020335 Academic Editor: Alexander C. Katoulis Received: 16 December 2023 Revised: 5 January 2024 Accepted: 5 January 2024 Published: 6 January 2024 Copyright: © 2024 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ([https://](https://)[ ](https://)[creativecommons.org/licenses/by/](creativecommons.org/licenses/by/)[ ](creativecommons.org/licenses/by/)[4.0/](4.0/)) . Department of Dermatology, Incheon St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, Seoul 06591, Republic of Korea; [clarakim9511@gmail.com](clarakim9511@gmail.com) (S.K.); [w1206@naver.com](w1206@naver.com) (Y.R.W.); [drchos@yahoo.co.kr](drchos@yahoo.co.kr) (S.H.C.); [leejd@catholic.ac.kr](leejd@catholic.ac.kr) (J.D.L.) * [Correspondence: hazelkimhoho@gmail.com](Correspondence: hazelkimhoho@gmail.com); Tel.: +82-10-6219-4389 Abstract: Bleomycin and 5-fluorouracil (5-FU) are widely used in various dermatological disorders. Both drugs are well-recognized as antineoplastic drugs and exert their effect by blocking the cell cycle. Topical and intralesional formulations are available and have been studied in both non-neoplastic and cancerous lesions. However, data comparing the effect of bleomycin and 5-FU in the dermatological disorders are limited. This review outlines the action mechanisms of both drugs and compares their clinical efficacies in a wide range of dermatologic diseases including hypertrophic scar, wart, skin cancer, vascular malformation, hemangioma, and vitiligo, and discusses the overall safety of the drugs. Intralesional bleomycin treatment is effective in hypertrophic scars and warts, but intralesional 5-FU may also be considered since it is cheaper and less painful. Moreover, intralesional 5-FU and bleomycin injection is a viable option for premalignant lesions (i.e., actinic keratosis) and inoperable skin cancers. Both bleomycin and 5-FU have been applied as treatment adjuncts for vitiligo, with 5-FU showing a slightly better outcome. Both agents have a good safety profile, and no serious side effects have been reported following their use in the field of dermatology. Keywords: 5-fluorouracil; bleomycin; dermatology; injection; topical 1. Introduction Bleomycin is an antitumor antibiotic which effectively blocks the cell cycle and cleaves DNA [1] . Bleomycin is composed of water-soluble glycosylated peptides, a key factor in its action mechanism. By chelating Fe (II) (Fe2+, element iron in its +2 oxidation state) to Fe (III) (Fe3+, element iron in its +3 oxidation state) and creating free radicals, bleomycin exerts oxidative damage to the DNA. In addition to solid tumors and Hodgkin’s lymphoma, the FDA has approved systemic bleomycin as an adjunct chemotherapy agent for squamous cell carcinoma on the head and neck, cervix, penis, and skin [2] . 5-Fluorouracil (5-FU) is a pyrimidine analog that is composed of a pyrimidine and furan ring. 5-FU can be incorporated into both DNA and RNA and disrupts their synthesis by inhibiting thymidylate synthase [3] . 5-FU, a chemotherapeutic agent, is well recognized for its use in many cancer types including ovarian, gastroenterology, and breast cancer. In the dermatology field, the FDA has approved topical 5-FU as a treatment modality for actinic keratosis and superficial basal cell carcinoma [4] . Dermatologists have been actively using bleomycin and 5-FU off-label for various skin diseases such as warts, hypertrophic scars, vas

FAQs

Why are bleomycin and 5-FU used in dermatology?

Both are antineoplastic drugs that exert effects by blocking the cell cycle. Their actions involve mechanisms that ultimately disrupt DNA and cellular processes.

How do the review’s findings compare intralesional bleomycin and intralesional 5-FU?

Intralesional bleomycin is described as effective for hypertrophic scars and warts, while intralesional 5-FU may be considered as an alternative due to being cheaper and less painful.

What evidence exists on safety and overall side effects?

Both agents are reported to have a good safety profile, with no serious side effects reported following their use in dermatology.

Sep 21, 2026

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