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Pentosan Polysulfate

PPS · Elmiron

Wound Healing & RegenerationApproved
From$10.87/mgCompare prices
MW
1705.1g/mol
Formula
C29H38Na10O50S9

Pentosan polysulfate (PPS) is a polysulfated glycosaminoglycan derived from beechwood, classified as a heparin analogue. Researchers primarily study PPS for its potential applications in conditions such as osteoarthritis and interstitial cystitis, as well as its role in regulating iron metabolism. Key findings from recent studies indicate that PPS inhibits hepcidin-facilitated osteoclast differentiation and function, which may have implications for osteoporosis, while also demonstrating anti-inflammatory effects in models of diabetic nephropathy. Additionally, PPS has been shown to downregulate hepcidin expression in both in vitro and in vivo settings, suggesting a novel mechanism for managing iron homeostasis. Current research continues to explore the multifaceted therapeutic potential of PPS across various medical conditions.

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 the expression of hepcidin, a key regulator of iron homeostasis, through interference with the BMP6/SMAD signaling pathway. This inhibition leads to reduced osteoclastogenesis and iron overload by downregulating osteoclast-specific genes such as cathepsin K and ferroportin 1. Additionally, PPS exhibits anti-inflammatory effects and may exert antioxidant properties, although the complete mechanism of action remains to be fully elucidated.

Research

71 Research Publications

2,456

Total Citations

19

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
168
The study demonstrated that cyclosporine A was superior to pentosan polysulfate in improving clinical outcomes for interstitial cystitis patients, with significant reductions in micturition frequency.
200, 400, 800, 1200 nmol/L(canine)1, 5, 10, 20, 40 μg/mL(canine)10 mginjection(human)25 mg/kg/dayoral(mouse)4 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days20 μg/g(rat)30 days2 μg/g(rat)30 days5 mgintraarticular(rabbit)8 weeks10 mg/kgevery 48 hours(rabbit)75 mg/kgevery 48 hours(rabbit)5 mg/kgevery 48 hours(rabbit)
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
Researchers observed that the combination of insulin-like growth factor-1 and sodium pentosan polysulfate maintained cartilage structure and biochemistry in a canine model of osteoarthritis.
200, 400, 800, 1200 nmol/L(canine)1, 5, 10, 20, 40 μg/mL(canine)10 mginjection(human)25 mg/kg/dayoral(mouse)4 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days20 μg/g(rat)30 days2 μg/g(rat)30 days5 mgintraarticular(rabbit)8 weeks10 mg/kgevery 48 hours(rabbit)75 mg/kgevery 48 hours(rabbit)5 mg/kgevery 48 hours(rabbit)
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
Researchers observed that pentosan polysulfate inhibited tumor growth in athymic nude mice by blocking the paracrine effects of heparin-binding growth factors released from tumor cells.
200, 400, 800, 1200 nmol/L(canine)1, 5, 10, 20, 40 μg/mL(canine)10 mginjection(human)25 mg/kg/dayoral(mouse)4 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days20 μg/g(rat)30 days2 μg/g(rat)30 days5 mgintraarticular(rabbit)8 weeks10 mg/kgevery 48 hours(rabbit)75 mg/kgevery 48 hours(rabbit)5 mg/kgevery 48 hours(rabbit)
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
Researchers observed that pentosan polysulfate significantly reduced inflammatory markers and improved clinical outcomes in mucopolysaccharidosis type VI rats.
200, 400, 800, 1200 nmol/L(canine)1, 5, 10, 20, 40 μg/mL(canine)10 mginjection(human)25 mg/kg/dayoral(mouse)4 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days20 μg/g(rat)30 days2 μg/g(rat)30 days5 mgintraarticular(rabbit)8 weeks10 mg/kgevery 48 hours(rabbit)75 mg/kgevery 48 hours(rabbit)5 mg/kgevery 48 hours(rabbit)
PubMed
#10

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

ReviewInfluence5.0
87
Researchers observed that pentosan polysulfate can trigger heparin-induced thrombocytopenia-like reactions, highlighting its potential risks in patients with pre-existing conditions.
200, 400, 800, 1200 nmol/L(canine)1, 5, 10, 20, 40 μg/mL(canine)10 mginjection(human)25 mg/kg/dayoral(mouse)4 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days20 μg/g(rat)30 days2 μg/g(rat)30 days5 mgintraarticular(rabbit)8 weeks10 mg/kgevery 48 hours(rabbit)75 mg/kgevery 48 hours(rabbit)5 mg/kgevery 48 hours(rabbit)
PubMed
Safety

Safety & Handling

Research Gaps

No long-term studies have been conducted to assess the safety and efficacy of pentosan polysulfate in patients with interstitial cystitis, particularly regarding its potential side effects such as pigmentary maculopathy. Additionally, the specific mechanisms by which pentosan polysulfate exerts its anti-inflammatory effects and regulates hepcidin expression in humans remain unclear, necessitating further investigation.

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

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Pricing

Price Comparison

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    Price/mg
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    Price/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