MedPath

Metformin Repurposing in Oral Submucous Fibrosis: Unveiling In Vitro Signaling Pathways, Progressing to Clinical Trial

Phase 1
Completed
Conditions
Oral Submucous Fibrosis
Interventions
Registration Number
NCT06332612
Lead Sponsor
Ziauddin University
Brief Summary

OSF is a widespread health issue in Asian countries, notably Pakistan, linked to the consumption of pan, chalia, and gutka, affecting a rising number of young individuals as an epidemic. This condition significantly impairs oral function, resulting in ulcers and chronic lesions, often progressing to oral cancer. Current treatments focus on symptom relief and halting disease progression. This study explores the repurposing of metformin, an FDA-approved drug with antifibrotic properties, for OSF treatment. Our objective is to unveil its therapeutic potential and comprehend its impact on the dysregulated signaling pathways associated with OSF. This research offers promising insights for an enhanced management approach, providing hope for those grappling with this debilitating condition

Detailed Description

OSF stands as a persistent inflammatory and potentially malignant condition affecting the oral cavity, marked by progressive fibrosis of the oral mucosa. The spectrum of its manifestations spans from initial inflammation to the gradual emergence of fibrous bands, leading to restricted mouth opening and mucosal rigidity. Common symptoms encompass burning sensations, difficulty in swallowing, and alterations in taste perception. This health concern has gained prominence in Pakistan, experiencing a worrisome surge in prevalence from 8.3/105 to 16.2/105 in recent years. Formerly confined to Southeast Asia, OSF has now transcended borders, manifesting in Asian immigrant communities in Britain and America, evolving into a global oral potential malignant disorder (OPMD) with a malignant rate of 9.13% .

Presently, the corticosteroid-based approach effectively reduces inflammation in OSF but falls short in addressing the underlying molecular mechanisms contributing to fibrosis. Furthermore, the prolonged use of corticosteroids raises concerns about adverse effects, including mucosal atrophy and compromised tissue integrity. This study aims to investigate the potential of metformin, a recognized emerging drug for treating fibrosis, and its anti-fibrotic properties in various organs. The established safety profile of metformin adds an advantageous aspect to its potential applications.

Numerous studies indicate that metformin exhibits anti-fibrotic effects by inhibiting TGF-β1 production, reducing phosphorylation and nuclear translocation of Smad2/3. Additionally, metformin inhibits Smad2/3 phosphorylation independently and activates AMPK, hindering Smad3 phosphorylation. The impact on reactive oxygen species (ROS) generation moderates TGF-β1-induced Smad2/3 phosphorylation and myofibroblast differentiation.Metformin has shown promise in hindering collagen production and promoting trans differentiation in various organ, including the lung, kidney, heart and adipose tissue. A clinical trial reported metformin therapy's impact on postmenopausal ovaries, patients with type 2 diabetes mellitus (T2DM) exhibited isotropic collagen organization and reduced fibrosis during oophorectomy.The observed risk reduction for ovarian cancer in T2DM women using metformin suggests its potential as an ovarian cancer prophylaxis. Despite conflicting clinical trial results in liver fibrosis, metformin consistently improves hepatocyte damage and inflammation. Clinical trials have explored the role of metformin antitumor activity when combined with conventional chemotherapeutic drugs and in idiopathic pulmonary fibrosis it inhibits TGFβ1, suppressing collagen formation, activating PPARγ signaling and inducing lipogenic differentiation.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
30
Inclusion Criteria
  1. Patients with OSF- palpable bands on oral examination
  2. Patients with limited mouth opening due to OSF
  3. Patients who have not received any treatment for OSF in the previous three months
  4. Patients with habits of pan, Chalia, Ghutka
  5. Age group between 18 and 45 years
Exclusion Criteria
  1. Patients presenting with both OSCC and OSF
  2. Patients with limited mouth opening due to impaction of the third molar (impaction of third molar results in limited mouth opening hence such patients are excluded since limited mouth opening due to third molar impaction can be mistaken for OSF).
  3. Patients with limited mouth opening due to temporomandibular joint disorder (temporomandibular joint disorders can limit the ability of patient to open their mouth and hence can be mistaken for OSF)
  4. Any history of Metformin intolerance or contraindications.
  5. Presence of other severe medical conditions along with drug therapy.
  6. Pregnancy or lactation.
  7. Participation in other clinical trials concurrently.
  8. Inability to provide informed consent.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
MetforminTMetformin HydrochlorideTopical cream metformin thrice daily
Standardbetamethasone dipropionateGroup 1: Standard treatment with topical cream betamethasone and Pentoxifylline tablet.
StandardPentoxifyllineGroup 1: Standard treatment with topical cream betamethasone and Pentoxifylline tablet.
MetforminOMetformin HydrochlorideMetformin 500 mg thrice daily.
Primary Outcome Measures
NameTimeMethod
Assess Signaling pathway with optimal metformin concentration9 months

To evaluate the effect of TGF-beta Smad 2/3 and wnt/b-catenin signaling pathways in vitro

Morphological Change Extracellular Matrix (ECM) Structure8 months

Extracellular Matrix (ECM) Structure Unit: Qualitative description Alterations in ECM structure will be qualitatively assessed.

Cell Invasion Assays8 months

Unit: Invaded area (e.g., square millimeters) Assessment of cell invasion will be presented as the invaded area relative to untreated control cells.

Apoptosis Analysis8months

Unit: Percentage Apoptotic cells will be quantified and reported as a percentage of the total cell population.

Cell Migration Assays8months

Unit: Distance migrated (micrometers) The extent of cell migration will be quantified as the distance migrated from the original point.

Morphological Change Cell Density8 months

Unit: Cells per unit area Changes in cell density will be quantified and reported as cells per unit area. Sub-Measure 3: Extracellular Matrix (ECM) Structure Unit: Qualitative description Alterations in ECM structure will be qualitatively assessed.

Cell Viability8 months

Cell Viability by MTT Assay Unit: Percentage Assessment of cell viability will be reported as a percentage of untreated control cells.

Cytotoxicity8 Months

Cytotoxicity Unit: Percentage Measurement of cytotoxicity will be presented as a percentage relative to untreated control cells.

Morphological Changes Cell Shape8months

Unit: Qualitative description Cell shape alterations will be described qualitatively based on microscopic observations.

Secondary Outcome Measures
NameTimeMethod
Clinical Oral Mucosal Characteristics9 months

Unit: Descriptive score (based on a scale ranging from 0 to 3 (normal to severe).0=No changes 1=Soreness 2=Soreness and ulceration 3=Soreness, ulceration and ability to use a liquid diet only

Patient Mouth Opening9 months

Unit: Millimeters on a scale of Grade 0 = \> 35 mm, Grade1= 26-35mm, Grade 2= 15-25mm, Grade 3: \< 10mm

Patient Burning sensation pain9 months

Unit: Units on a scale (Verbal numeric rating scale graded on a 10-point scale from 0 to 10, where 0 indicated no burning sensation while 10 represented the worst burning sensation)

Trial Locations

Locations (1)

Ziauddin University

🇵🇰

Karachi, Sindh, Pakistan

© Copyright 2025. All Rights Reserved by MedPath