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Pentosan Polysulfate

PPS · Elmiron

Wound Healing & RegenerationApproved
From$307.80/mgCompare prices
MW
1705.1g/mol
Formula
C29H38Na10O50S9

Pentosan polysulfate (PPS) is a polysulfated glycosaminoglycan derived from beechwood that is primarily studied for its therapeutic potential in various conditions, including interstitial cystitis and osteoarthritis. Researchers observed that PPS exhibits anti-inflammatory properties and may regulate hepcidin expression, which is crucial for iron homeostasis and has implications for conditions like anemia and osteoporosis. Key findings indicate that PPS can inhibit the differentiation and function of osteoclasts, potentially benefiting bone health, and it has shown promise in mitigating renal inflammation and albuminuria progression in diabetic nephropathy models. Current research continues to explore the multifaceted roles of PPS in both preclinical and clinical settings, highlighting its potential as a novel therapeutic agent across a range of disorders.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC29H38Na10O50S9
Molecular Weight1705.1 g/mol
CAS Number37319-17-8
PubChem CID92043424
ChEMBL IDCHEMBL2288852

Half-Life

INIntranasal

Not applicable

POOral

Poor bioavailability

Oral administration results in a longer half-life due to slow absorption.

Mechanism

Mechanism of Action

Pentosan polysulfate (PPS) acts primarily by inhibiting hepcidin expression through interference with the BMP6/SMAD signaling pathway, which is crucial for iron homeostasis. This inhibition leads to decreased osteoclastogenesis and reduced iron overload, promoting a balance between iron release and uptake. Additionally, PPS exhibits anti-inflammatory effects, potentially through the modulation of inflammatory cytokines such as IL-6, although the complete mechanism of action remains to be fully elucidated.

Research

68 Research Publications

2,370

Total Citations

17

Human/RCT

3.0

Avg. Influence

2025

Latest

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#01

The sulfate moieties of glycosaminoglycans are critical for the enhancement of beta-amyloid protein fibril formation.

In VitroInfluence8.0
220
Researchers observed that sulfate moieties in glycosaminoglycans, including pentosan polysulfate, are critical for enhancing beta-amyloid fibril formation, indicating their role in Alzheimer's disease pathology.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayoral(rat)8 weeks1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days5 mgintraarticular(rabbit)8 weeks5 mg/kgevery 48 hours(rabbit)not specified10 mg/kgevery 48 hours(rabbit)not specified75 mg/kgevery 48 hours(rabbit)not specified
PubMed
#02

Cyclosporine A and pentosan polysulfate sodium for the treatment of interstitial cystitis: a randomized comparative study.

HumanInfluence13.0
165
Researchers observed that cyclosporine A was superior to pentosan polysulfate in reducing daily micturition frequency and improving clinical outcomes in patients with interstitial cystitis.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayP.O.(rat)4 months1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months
PubMed
#03

Efficacy of pentosan polysulfate in the treatment of interstitial cystitis: a meta-analysis.

Hwang P, et al. · Urology · 1997

Meta-AnalysisInfluence2.0
125
Researchers found that pentosan polysulfate (Elmiron) is more effective than a placebo in reducing pain, urgency, and frequency of symptoms in patients with interstitial cystitis. However, it did not show a significant difference compared to placebo for nocturia symptoms.

Key findings

  1. 01Pentosan polysulfate was associated with a 16.6% improvement in pain symptoms compared to placebo.
  2. 02There was a 13.0% improvement in urgency symptoms with pentosan polysulfate versus placebo.
  3. 03No significant difference was observed for nocturia symptoms when comparing pentosan polysulfate to placebo.
PubMed
#04

Treatment of canine osteoarthritis with insulin-like growth factor-1 (IGF-1) and sodium pentosan polysulfate.

AnimalInfluence1.0
122
The study demonstrated that the combination of insulin-like growth factor-1 and sodium pentosan polysulfate maintained cartilage structure and biochemistry in a canine model of osteoarthritis.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayP.O.(rat)4 months1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months
PubMed
#05

Inhibition by pentosan polysulfate (PPS) of heparin-binding growth factors released from tumor cells and blockage by PPS of tumor growth in animals.

AnimalInfluence7.0
120
The study demonstrated that pentosan polysulfate effectively inhibited tumor growth in vivo by blocking the paracrine effects of heparin-binding growth factors released from various human tumor cell lines.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayP.O.(rat)4 months1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months
PubMed
#06

Tumor growth dependent on Kaposi's sarcoma-derived fibroblast growth factor inhibited by pentosan polysulfate.

AnimalInfluence6.0
108
Researchers observed that pentosan polysulfate selectively inhibited tumor growth induced by Kaposi's sarcoma-derived fibroblast growth factor in a xenograft model, indicating its potential as a therapeutic agent.
200, 400, 800, 1200 nmol/L(canine)25 mg/kg/dayoral(mouse)4 months100 mg3 times daily(human)6 months5 mgintraarticular(rabbit)8 weeks20 μg/g(rat)30 days5 mg/kg, 10 mg/kg, or 75 mg/kgevery 48 hours(rabbit)
PubMed
#07

Combined anti-inflammatory and anti-AGE drug treatments have a protective effect on intervertebral discs in mice with diabetes.

AnimalInfluence4.0
107
Researchers observed that combined treatment with pentosan polysulfate and pyridoxamine mitigated degenerative changes in intervertebral discs in diabetic mice, suggesting a protective effect against diabetes-induced spinal pathology.
200, 400, 800, 1200 nmol/L(canine)25 mg/kg/dayoral(mouse)4 months100 mg3 times daily(human)6 months5 mgintraarticular(rabbit)8 weeks20 μg/g(rat)30 days5 mg/kg, 10 mg/kg, or 75 mg/kgevery 48 hours(rabbit)
PubMed
#08

Heparan sulfates and coxsackievirus-adenovirus receptor: each one mediates coxsackievirus B3 PD infection.

In VitroInfluence5.0
94
Researchers observed that coxsackievirus B3 variant PD utilizes specific modified heparan sulfates for entry into cells, with pentosan polysulfate inhibiting viral replication in vitro.
200, 400, 800, 1200 nmol/L(canine)25 mg/kg/dayoral(mouse)4 months100 mg3 times daily(human)6 months5 mgintraarticular(rabbit)8 weeks20 μg/g(rat)30 days5 mg/kg, 10 mg/kg, or 75 mg/kgevery 48 hours(rabbit)
PubMed
#09

Pentosan polysulfate: a novel therapy for the mucopolysaccharidoses.

AnimalInfluence1.0
92
The study demonstrated that pentosan polysulfate significantly reduced inflammatory markers and improved clinical outcomes in mucopolysaccharidosis type VI rats, suggesting its potential as a therapy for this condition.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayP.O.(rat)4 months1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months
PubMed
#10

Spontaneous HIT syndrome: Knee replacement, infection, and parallels with vaccine-induced immune thrombotic thrombocytopenia.

ReviewInfluence5.0
87
Researchers observed that spontaneous heparin-induced thrombocytopenia can occur without prior exposure to heparin or polyanionic medications, resembling a secondary immune response.
10 mginjection(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified25 mg/kg/dayP.O.(rat)4 months1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months
PubMed
Safety

Safety & Handling

Research Gaps

No long-term human trials have been conducted to assess the safety and efficacy of pentosan polysulfate in treating conditions like interstitial cystitis and diabetic nephropathy, particularly regarding potential side effects such as pigmentary maculopathy. Additionally, the precise mechanisms by which pentosan polysulfate exerts its anti-inflammatory effects and regulates hepcidin expression remain unclear, necessitating further investigation into its pharmacodynamics and interactions with other therapies.

Solubility

Pentosan Polysulfate is highly soluble in water but has limited solubility in organic solvents such as acetonitrile and DMSO.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

Legal Status

🇩🇪DE

Approved for specific medical use. Not a controlled substance.

🇺🇸US

FDA approved for interstitial cystitis. Not a controlled substance.

🇦🇺AU

TGA approved for specific indications.

🇬🇧UK

MHRA approved for specific medical use.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Community Insights

Publications per Year

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Pricing

Price Comparison

  • BESTPeptaNovaEU
    1mg
    $307.80
    Price/mg
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    0.1mg
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    Price/mg
    $1620.00/mg
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  • PeptaNovaEU
    0.05mg
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    Price/mg
    $4212.00/mg
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Mechanism

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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer