Drug intelligence / Profile preview

calcipotriene + 5-fluorouracil

Development stage
Unknown
Lead developer
SKNV
Modality
Small Molecules
Administration
Topical
01

Overview

Calcipotriene + 5-fluorouracil is a topical combination therapy consisting of the vitamin D analog calcipotriene (0.005%) and the antimetabolite chemotherapy agent 5-fluorouracil (5%). This combination is primarily investigated for the treatment of actinic keratoses (AKs) and the prevention of squamous cell carcinoma. Calcipotriene acts as an immunomodulator by inducing the expression of thymic stromal lymphopoietin (TSLP) in keratinocytes, which activates a T-cell-mediated anti-tumor immune response. 5-fluorouracil acts by inhibiting thymidylate synthase, leading to the death of rapidly proliferating tumor cells. Clinical research, particularly from academic centers like Massachusetts General Hospital, has demonstrated that the combination significantly reduces the risk of squamous cell carcinoma development compared to 5-fluorouracil alone by inducing CD4+ tissue-resident memory T cells (TRM) in the skin.

Other names
calcipotriol + 5-fluorouracilcalcipotriene/5-fluorouracil5-FU + calcipotriene
02

Targets

TSLP (Thymic stromal lymphopoietin)VDR (Vitamin D receptor)TS (Thymidylate synthase)

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