proflavine

Small moleculeexperimental

Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps. — NCATS

Clinical trial activity

21 trials · 15 clinical orgs · 0 marketing orgs

Phase 1
10
Phase 2
5
Phase 3
0
Phase 4
1

Earliest trial started Feb 1, 2009 (NCT01384227)

Timeline

2000s

  1. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2014

    Earliest Phase 2 Sponsor(trial)

Indications

Mechanism of action

  • DNABINDING AGENT

    DNA binding agent

  • DNADISRUPTING AGENT

    DNA disrupting agent

Chemistry & pharmacology

Loading structure…

SMILES

Nc1ccc2cc3ccc(N)cc3nc2c1
Mol. weight
209.25 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 2,8-diaminoacridine
  • 2,8-diaminoacridine
  • 3,6-acridinediamine
  • 3,6-acridinediamine
  • 3,6-diaminoacridine
  • 3,6-diaminoacridine
  • diaminoacridine
  • diaminoacridine
  • proflavin
  • proflavin
  • proflavin
  • proflavina
  • proflavina
  • proflavine
  • proflavine
  • proflavine
  • proflavine
  • proflavine
  • proflavine
  • proflavine
  • proflavine hemisulfate
  • proflavine hemisulfate
  • proflavine sulfate
  • proflavin hemisulfate
  • proflavin sulfate
  • proflavinum
  • proflavinum

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06435286Phase 2Nov 1, 2024Baylor University, Hospital de Cancer de Barretos - Fundacao Pio XII, Instituto do Cancer do Estado de São Paulo, University of Texas at Houston, William Marsh Rice University
NCT05554133N/AMar 1, 2023National Institute of Dental and Craniofacial Research (NIDCR), University of Texas at Houston
NCT05396781Phase 2Jan 13, 2022Baylor University, University of Sao Paulo, William Marsh Rice University
NCT04563754Phase 1/Phase 2 (Phase 2)Jul 30, 2019Baylor University, Icahn School of Medicine at Mount Sinai, Medical University of South Carolina, University of California, San Francisco, University of Texas at Houston, William Marsh Rice University
NCT03379389Phase 4Mar 31, 2018Fundação Educacional Serra dos Órgãos, Laboratório Gross S.A.
NCT02714439Early Phase 1 (Phase 1)Jun 1, 2017University of Texas at Houston, University of Texas, Galveston, William Marsh Rice University
NCT02790853Early Phase 1 (Phase 1)May 25, 2016National Cancer Institute (NCI), University of Texas at Houston
NCT02206048N/AOct 1, 2015University of Texas at Houston
NCT02420665N/ASep 1, 2015National Cancer Institute (NCI), National Institutes of Health (NIH), University of Texas at Houston
NCT02207959Phase 1Jan 1, 2015Icahn School of Medicine at Mount Sinai, William Marsh Rice University
NCT02095847Phase 2Mar 21, 2014University of Texas at Houston
NCT02029937Phase 2Jan 1, 2014Baylor University, William Marsh Rice University
NCT02335372N/AJun 1, 2013University of Texas at Houston
NCT02018367Phase 1Sep 1, 2012Baylor University, William Marsh Rice University
NCT01456143N/ADec 31, 2011Baylor University, Icahn School of Medicine at Mount Sinai, William Marsh Rice University
NCT01384864Early Phase 1 (Phase 1)Aug 1, 2011Baylor University, William Marsh Rice University
NCT01269190N/ADec 1, 2010National Institutes of Health (NIH), University of Texas at Houston
NCT01384708Early Phase 1 (Phase 1)Aug 1, 2010Baylor University, William Marsh Rice University
NCT01384240Early Phase 1 (Phase 1)Apr 1, 2010Baylor University, Icahn School of Medicine at Mount Sinai
NCT01384695Early Phase 1 (Phase 1)Jun 1, 2009Baylor University, Icahn School of Medicine at Mount Sinai
Showing 20 of 21 trials
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Organizations

Research & Development (15)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Baylor UniversityAcademic/Hospital111132009
University of Texas at HoustonAcademic/Hospital10732010
William Marsh Rice UniversityAcademic/Hospital10032010
Icahn School of Medicine at Mount SinaiAcademic/Hospital6132009
National Cancer Institute (NCI)Government2022015
National Institutes of Health (NIH)Government2012010
Fundação Educacional Serra dos ÓrgãosAcademic/Hospital1112018
Hospital de Cancer de Barretos - Fundacao Pio XIIAcademic/Hospital1012024
Instituto do Cancer do Estado de São PauloAcademic/Hospital1012024
Laboratório Gross S.A.For profit1012018
Medical University of South CarolinaAcademic/Hospital1012019
National Institute of Dental and Craniofacial Research (NIDCR)Government1012023
University of California, San FranciscoAcademic/Hospital1012019
University of Sao PauloAcademic/Hospital1012022
University of Texas, GalvestonAcademic/Hospital1112017
15 organizations
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