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Pentosan Polysulfate

PPS · Elmiron

Wound Healing & RegenerationApproved

MW: 1705.1g/mol
Formula: C29H38Na10O50S9

Pentosan polysulfate (PPS) is a polysulfated glycosaminoglycan derived from beechwood, primarily recognized for its role in the management of interstitial cystitis. Researchers primarily study PPS for its potential therapeutic effects in various conditions, including osteoarthritis and diabetic nephropathy. Key findings from recent studies indicate that PPS may inhibit the formation and function of osteoclasts, which are involved in bone resorption, and it has demonstrated anti-inflammatory properties that could mitigate renal damage in diabetic models. Additionally, PPS has been shown to downregulate hepcidin expression, a peptide crucial for iron regulation, suggesting its broader implications in managing iron-related disorders. Current research continues to explore the multifaceted roles of PPS in various therapeutic contexts, highlighting its potential beyond its established use.

Chemical Profile

Chemical Structure

Formula	C29H38Na10O50S9
Molecular Weight	1705.1 g/mol
CAS Number	37319-17-8
PubChem CID	92043424
ChEMBL ID	CHEMBL2288852

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 hepcidin expression through interference with the BMP6/SMAD signaling pathway, thereby regulating iron homeostasis and affecting osteoclast differentiation and function. It also exerts anti-inflammatory effects, reducing renal inflammation and oxidative stress in diabetic nephropathy models, although the precise receptors and complete signaling mechanisms involved remain to be fully elucidated. Additionally, its role in modulating bladder wall integrity in interstitial cystitis suggests involvement in pathways related to bladder sensory neuropeptide activation and mast cell stabilization.

Research

78 Research Publications

2,593

Total Citations

Human/RCT

3.1

Avg. Influence

2025

Latest

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01Top

#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

02Top

#02

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

HumanInfluence13.0

167

The study demonstrated that cyclosporine A was superior to pentosan polysulfate in reducing micturition frequency and improving clinical outcomes in patients with interstitial cystitis.

10 mgintravesical(human)single procedure200, 400, 800, 1200 nmol/Lnot specified(canine)not specified1.5 mg/kgtwice daily(human)6 months100 mg3 times daily(human)6 months15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days5 mg/kgoral(rabbit)not specified10 mg/kgoral(rabbit)not specified75 mg/kgoral(rabbit)not specified

PubMed

03Top

#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

01Pentosan polysulfate was associated with a 16.6% improvement in pain symptoms compared to placebo.
02There was a 13.0% improvement in urgency symptoms with pentosan polysulfate versus placebo.
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 effectively maintained cartilage structure and biochemistry in a canine model of osteoarthritis.

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

121

The study demonstrated that pentosan polysulfate significantly inhibits tumor growth in nude mice by blocking the paracrine effects of heparin-binding growth factors released from tumor cells.

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

The study demonstrated that oral treatments with pentosan polysulfate and pyridoxamine mitigate diabetes-induced degenerative changes in intervertebral discs and vertebrae in a mouse model by reducing AGE accumulation and inflammation.

100 mgP.O.(human)6 months25 mg/kg/dayoral(mouse)4 months10 mg/kgevery 48 hours(rabbit)7 days prior to PC injection15 mg/kgsubcutaneously(rat)30 days10 mg/kgsubcutaneously(rat)30 days

PubMed

#08

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

In VitroInfluence5.0

Researchers observed that coxsackievirus B3 variant PD utilizes specific modified heparan sulfates for entry into cells, with pentosan polysulfate inhibiting viral replication in vitro.

PubMed

#09

Pentosan polysulfate: a novel therapy for the mucopolysaccharidoses.

AnimalInfluence1.0

The study demonstrated that pentosan polysulfate significantly reduces inflammatory markers and improves clinical outcomes in mucopolysaccharidosis type VI rat models.

PubMed

#10

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

ReviewInfluence5.0

The study demonstrated that spontaneous HIT syndrome can occur without prior exposure to heparin or polyanionic medications, suggesting an autoimmune mechanism.

PubMed

Safety

Safety & Handling

Research Gaps

No long-term human studies have been conducted to assess the safety and efficacy of pentosan polysulfate in treating interstitial cystitis, 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 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

🇩🇪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

Publications per Year

45 total

Pricing

Price Comparison

BESTRoyal Peptides WholesaleUS
11.5mg
$125.00
Price/mg
$10.87/mg
View
PeptaNovaEU
0.1mg
$162.00
Price/mg
$1620.00/mg
View

Vendor	Amount	Price	Price/mg	Link
BESTRoyal Peptides WholesaleUS	11.5mg	$125.00	$10.87/mg	View
PeptaNovaEU	0.1mg	$162.00	$1620.00/mg	View

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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