Drug intelligence / Profile preview

imiquimod

Development stage
Approved
Lead developer
3M
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Topical
01

Overview

Imiquimod is a small molecule immune response modifier used topically to treat actinic keratosis, superficial basal cell carcinoma, and external genital and perianal warts (condyloma acuminata). It acts primarily as an agonist of toll-like receptor 7 (TLR7), and to a lesser extent TLR8, leading to activation of the innate immune system. This results in the induction of pro-inflammatory cytokines such as interferon-alpha (IFN-α), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), and others. Imiquimod stimulates antigen-presenting cells including Langerhans cells, dendritic cells, macrophages, natural killer cells, and B lymphocytes. Its antitumor effects are mediated both by direct induction of apoptosis in tumor cells via caspase activation and upregulation of proapoptotic proteins from the Bcl-2 family as well as by indirect stimulation of cell-mediated immunity. Imiquimod was originally developed by 3M's pharmaceutical division.

Brand names
AldaraZyclaraVyloma
Other names
1-isobutyl-1 H-imidazo[4,5-c]quinolin-4-amine
02

Targets

OGFR (Opioid growth factor receptor)TLR8 (Toll-like receptor 8)TLR7 (Toll-like receptor 7)

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