Imiquimod

DERMATOLOGICALS

Key facts

Imiquimod is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 1997. Its mechanism of action is classified as Interferon Inducers. DrugCentral lists 5 molecular targets, including NUDT1, ADRA1D and HRH2. Recorded indications include Actinic keratosis, Condyloma acuminatum, Superficial basal cell carcinoma and Verruca.

• Approval status: ofp (first approved 1997 by the FDA).
• Mechanism of action: Interferon Inducers.
• Molecular targets: NUDT1, ADRA1D, HRH2 and ADORA2A (5 listed in DrugCentral).
• Indications: Actinic keratosis, Condyloma acuminatum, Superficial basal cell carcinoma and Verruca.
• ATC code: D06BB10 (Antivirals).
• Molecular formula: C14H16N4; molecular weight 240.31 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (4)

• Actinic keratosis
• Condyloma acuminatum
• Superficial basal cell carcinoma
• Verruca

Off-label uses (1)

• Neoplasm of vulva

Contraindications (5)

• Autoimmune disease
• Graft-versus-host disease
• Immunosuppression
• Photosensitivity
• Sunburn

Mechanism & targets

• Mechanism of action (MoA): Interferon Inducers

Molecular targets (5)

Target	Gene	Action	Activity
7,8-dihydro-8-oxoguanine triphosphatase	NUDT1	unknown	IC50 6.19
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 5.89
Histamine H2 receptor	HRH2	unknown	Ki 5.83
Adenosine receptor A2a	ADORA2A	unknown	Ki 5.53
Toll-like receptor 7	TLR7	agonist	EC50 4.97

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
1998-09-18	EMA	—	—
1997-02-27	FDA	—	MEDICIS

ATC classification

ATC code	Therapeutic hierarchy
D06BB10	DERMATOLOGICALS › ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE › CHEMOTHERAPEUTICS FOR TOPICAL USE › Antivirals

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Erythema	159.3
Skin irritation	142.0
Scab	123.3
Off label use	108.1
Application site erythema	102.7
Vital capacity decreased	94.2
Application site scab	86.2
Skin ulcer	85.7
Application site inflammation	78.6
Skin reaction	75.4
Skin erosion	73.7
Application site ulcer	73.1

Chemical structure

• Molecular formula: C₁₄H₁₆N₄
• Molecular weight: 240.31 g/mol
• CAS number: 99011-02-6
• InChIKey: DOUYETYNHWVLEO-UHFFFAOYSA-N
• PubChem CID: 57469

CC(C)CN1C=NC2=C(N)N=C3C=CC=CC3=C12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Imiquimod used for?

DrugCentral lists the following indications for Imiquimod: Actinic keratosis, Condyloma acuminatum, Superficial basal cell carcinoma and Verruca.

How does Imiquimod work?

Imiquimod is classified as Interferon Inducers; its molecular targets in DrugCentral include NUDT1, ADRA1D, HRH2 and ADORA2A.

When was Imiquimod first approved?

Imiquimod was first approved by the FDA in 1997.

What is the chemical formula of Imiquimod?

Imiquimod has the molecular formula C14H16N4 and a molecular weight of 240.31 g/mol.

Sources

• DrugCentral drug card 1429 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1282 — compound record and bioactivity
• PubChem CID 57469 — chemical identifiers
• DrugBank DB00724 — drug record
• FDA UNII P1QW714R7M — substance identity
• DailyMed: FDA labels for Imiquimod — current prescribing information (label search)
• UniProt P36639 (NUDT1) — target protein
• UniProt P25100 (ADRA1D) — target protein
• UniProt P25021 (HRH2) — target protein
• UniProt P29274 (ADORA2A) — target protein
• UniProt Q9NYK1 (TLR7) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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