imiquimod

Trade name: aldara

Small moleculeapproved

Approved

Feb 27, 1997

Imiquimod is an immune response modifier that acts as a toll-like receptor 7 agonist. Imiquimod is commonly used topically to treat warts on the skin of the genital and anal areas. Imiquimod does not cure warts, and new warts may appear during treatment. Imiquimod does not fight the viruses that cause warts directly, however, it does help to relieve and control wart production. It is not used on warts inside the vagina, penis, or rectum. Imiquimod is also used to treat a skin condition of the face and scalp called actinic keratoses. Imiquimod can also be used to treat certain types of skin cancer called superficial basal cell carcinoma. Imiquimod is particularly useful on areas where surgery or other treatments may be difficult, complicated or otherwise undesirable, especially the face and lower legs. Imiquimod's mechanism of action is via stimulation of innate and acquired immune responses, which ultimately leads to inflammatory cell infiltration within the field of drug application followed by apoptosis of diseased tissue. Imiquimod does not have direct antiviral activity. Studies of mice show that imiquimod may induce cytokines, including interferon-alpha (IFNA) as well as several IFNA genes (IFNA1, IFNA2, IFNA5, IFNA6, and IFNA8) as well as the IFNB gene. Imiquimod also induced the expression of interleukin (IL)-6, IL-8, and tumor necrosis factor alpha genes. In the treatment of basal cell carcinoma, Imiquimod appears to act as a toll-like receptor-7 agonist, and is thought to exert its anti-tumor effect via modification of the immune response and stimulation of apoptosis in BCC cells. In treating basal cell carcinoma it may increase the infiltration of lymphocytes, dendritic cells, and macrophages into the tumor lesion. Imiquimod is used for the topical treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adults. Also indicated for the treatment of external genital and perianal warts/condyloma acuminata in individuals 12 years old and above. — NCATS

Clinical trial activity

163 trials · 158 clinical orgs · 17 marketing orgs

Phase 1
44
Phase 2
71
Phase 3
42
Phase 4
28

Earliest trial started Jun 1, 1999 (NCT00031759)

Timeline

1990s

  1. Feb 27, 1997

    Earliest FDA Approval

  2. Feb 27, 1997

    Medicis — NDA Secondary Org

  3. Feb 27, 1997

    Bausch Health Companies — Marketing Organization

  4. Feb 27, 1997

    Bausch Health Companies — NDA Secondary Org

  5. Jan 1, 1999

    Earliest Phase 2 Sponsor(trial)

2000s

  1. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2004

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Feb 25, 2010

    Fougera — Marketing Organization

  2. Sep 7, 2010

    Padagis Us — Marketing Organization

  3. Sep 7, 2010

    Perrigo — Marketing Organization

  4. Feb 28, 2011

    ANDA Repository — Marketing Organization

  5. Feb 28, 2011

    Encube Ethicals Pvt. Ltd. — Marketing Organization

  6. Mar 24, 2011

    Graceway — NDA Secondary Org

  7. Apr 15, 2011

    Taro Pharmaceuticals — Marketing Organization

  8. Apr 15, 2011

    Sun Pharmaceuticals — Marketing Organization

  9. Apr 18, 2011

    Cosette — Marketing Organization

  10. Apr 18, 2011

    G & W Laboratories Inc. — Marketing Organization

  11. Apr 18, 2011

    ACP Nimble — Marketing Organization

  12. Mar 6, 2012

    Glenmark Pharmaceuticals — Marketing Organization

  13. Apr 6, 2012

    Apotex — Marketing Organization

  14. Jun 24, 2014

    Strides Pharma Science — Marketing Organization

Indications

Studied for

Mechanism of action

Approval history

  • approvedFeb 27, 1997

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)CN1C=NC2=C1C3=C(C=CC=C3)N=C2N
Mol. weight
240.3036 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Black box warning

Sources

Also known as

  • 1h-imidazo(4,5-c)quinolin-4-amine, 1-(2-methylpropyl)-
  • 1-isobutyl-1h-imidazo(4,5-c)quinolin-4-amine
  • 1-isobutyl-1h-imidazo[4,5-c]quinolin-4-amine
  • 1-isobutyl-1h-imidazo[4,5-c]quinolin-4-amine
  • 4-amino-1-isobutyl-1h-imidazo(4,5-c)quinoline
  • 4-amino-1-isobutyl-1h-imidazo(4,5-c)quinoline
  • aldara
  • aldara
  • aldara
  • aldara
  • aldara
  • aldara
  • beselna
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimod
  • imiquimodum
  • imiquimodum
  • imiquinod
  • r 837
  • r 837
  • r 837
  • r-837
  • r-837
  • r-837
  • s 26308
  • s-26308
  • s-26308
  • s-26308
  • tmx-101
  • tmx-101
  • zartra
  • zartra
  • zyclara
  • zyclara
  • zyclara
  • zyclara
  • zyclara

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07251413Phase 1/Phase 2 (Phase 2)Oct 22, 2025Institute of Oncology Dr. Rosell (IOR), Regeneron, University of Barcelona
NCT07210775Phase 1/Phase 2 (Phase 2)Oct 1, 2025University of Southern California
NCT06840470Phase 4Mar 31, 2025University of Michigan
NCT06686043Phase 2Aug 23, 2024Baylor University
NCT06411106N/AJun 30, 2024Leiden University
NCT06356012Phase 4Apr 2, 2024Barretos Cancer Hospital, Farmoquimica S.A., Fundação de Amparo à Pesquisa do Estado de São Paulo, Hospital de Cancer de Barretos - Fundacao Pio XII
NCT05838599Early Phase 1 (Phase 1)Jul 1, 2023Northwestern University
NCT05212246Phase 3Apr 1, 2023Department of Veteran Affairs
NCT05740969Phase 2Feb 1, 2023University of Copenhagen
NCT05468606Early Phase 1 (Phase 1)Jan 31, 2023Leiden University
NCT05375903Phase 1Jun 1, 2022UroGen Pharma
NCT05315024N/AApr 30, 2022The University of Hong Kong
NCT05314127Phase 2Apr 15, 2022Zagazig University
NCT05055050Phase 1Feb 28, 2022University of Texas at Houston
NCT04808245Phase 1Dec 6, 2021Deutsche Krebshilfe e.V., German Cancer Research Center, Humboldt University, Johannes Gutenburg University, Roche
NCT05028322Phase 2Nov 1, 2021University of Lorraine
NCT04883645Early Phase 1 (Phase 1)Sep 30, 2021Columbia University
NCT04842422Phase 4Apr 16, 2021Medical University of Graz
NCT04143451Phase 3Oct 23, 2019The University of Hong Kong
NCT04116320Phase 1Oct 8, 2019Theraclion, University of Virginia
Showing 20 of 163 trials
Page 1 / 9

Organizations

Research & Development (158)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GracewayFor profit161042001
National Cancer Institute (NCI)Government16241999
MedaFor profit10832001
The University of Hong KongAcademic/Hospital7722012
Maastricht UniversityAcademic/Hospital6432014
University of MinnesotaAcademic/Hospital5422000
3MFor profit4022000
Medical University of GrazAcademic/Hospital4322011
National Institutes of Health (NIH)Government4032004
University of TuebingenAcademic/Hospital4422002
University of ViennaAcademic/Hospital4432008
ActavisFor profit3322008
Department of Veteran AffairsGovernment3332007
Leiden UniversityAcademic/Hospital3232015
Mayo ClinicAcademic/Hospital3121999
New York UniversityAcademic/Hospital3222005
United States NavyGovernment3332004
University of PittsburghAcademic/Hospital3322012
University of VirginiaAcademic/Hospital3312004
AIDS Malignancy ConsortiumAcademic/Hospital2212014
158 organizations
Page 1 / 8

Marketing (21)

OrganizationOrg typeRelationshipDate
3MFor profitNDA
3MFor profitIND
ACP NimbleFor profitMKTGApr 18, 2011
ANDA RepositoryFor profitMKTGFeb 28, 2011
ApotexFor profitMKTGApr 6, 2012
Bausch Health CompaniesFor profitMKTGFeb 27, 1997
Bausch Health CompaniesFor profitNDA2Feb 27, 1997
CosetteFor profitMKTGApr 18, 2011
Encube Ethicals Pvt. Ltd.For profitMKTGFeb 28, 2011
FougeraFor profitMKTGFeb 25, 2010
G & W Laboratories Inc.For profitMKTGApr 18, 2011
Glenmark PharmaceuticalsFor profitMKTGMar 6, 2012
Glenmark PharmaceuticalsFor profitSYNMar 6, 2012
Glenmark PharmaceuticalsFor profitSYNMar 6, 2012
GracewayFor profitNDA2Mar 24, 2011
MedicisFor profitNDA2Feb 27, 1997
Padagis UsFor profitMKTGSep 7, 2010
PerrigoFor profitMKTGSep 7, 2010
Strides Pharma ScienceFor profitMKTGJun 24, 2014
Sun PharmaceuticalsFor profitMKTGApr 15, 2011
Taro PharmaceuticalsFor profitMKTGApr 15, 2011