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Topical Cytotoxic Agents at a Glance
  • Topical and intralesional cytotoxic agents are effective in the treatment of skin cancers and inflammatory and infectious dermatologic conditions.
  • They aim for maximum efficacy against cutaneous targets while sparing normal tissue and minimizing systemic toxicity.
  • They comprise 5-fluorouracil, nitrogen mustard, carmustine, vinblastine, bleomycin, methotrexate, podophyllin, and miltefosine.

Mechanism of Action and Formulations

Topical 5-fluorouracil (5-FU) has been used in clinical practice since the 1960s. It is a structural analogue of thymine that blocks DNA synthesis by inhibiting thymidylate synthetase (Table 220-1). Topical 5-FU is commercially available as a 0.5% cream carried in a microsphere vehicle, as a 1% solution or 1% cream, as a 2% or 5% solution, and as a 5% cream. The solution can also be used for intralesional injection.

Table 220-1 Topical and Intralesional Cytotoxic Agents Used in Dermatology: Mechanism of Action, Formulation, Main Indications, and Common Side Effects


5-FU 5% cream has been approved by the US Food and Drug Administration (FDA) since 1970 for the treatment of actinic keratoses in any location and superficial basal cell carcinomas; 5-FU 0.5% cream is FDA approved for treatment of actinic keratoses of the face and anterior scalp. 5-FU is used twice daily until an ...

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