Healing & repairPolysaccharide (non-peptide)Evidence B4 cited

Pentosan Polysulfate

PPS (Elmiron)

aka PPS · Elmiron · pentosan polysulfate sodium

A semi-synthetic polysaccharide researched for chondroprotective and anti-inflammatory effects in joint and bladder tissue.

Molecular wt
4000-6000g/mol
CAS
37319-17-8
Half-life
1 day
established
Tmax
2 h

Sequence

Read this before quoting the sequence
Not a peptide. Pentosan polysulfate sodium is a semi-synthetic, sulfated linear polysaccharide (a xylan-derived, heparin-like macromolecular carbohydrate that chemically and structurally resembles glycosaminoglycans), so no amino acid sequence exists.
Source ↗

Mechanism of action

Pentosan Polysulfate works by mimicking the structure of glycosaminoglycans, which are natural components of the extracellular matrix in cartilage. It binds to proteins and cells, reducing inflammation and preventing the breakdown of cartilage. Additionally, it inhibits enzymes that degrade cartilage and may improve blood flow to affected tissues.

What the evidence actually shows

Grade B

There are several human trials investigating Pentosan Polysulfate for osteoarthritis, showing moderate efficacy in reducing pain and improving joint function. However, the long-term effects and optimal dosing require further research. The evidence for its use in interstitial cystitis is more robust, with FDA approval for this condition.

Regulatory status

Status
Approved prescription medicine (US).
Approved as
ELMIRON (pentosan polysulfate sodium) 100 mg capsules, indicated for the relief of bladder pain or discomfort associated with interstitial cystitis; Janssen Pharmaceuticals.
Clinical stage
Marketed / approved.
UK
prescription_only

In the UK, Pentosan Polysulfate is available by prescription for specific conditions like interstitial cystitis.

Source ↗

Pharmacokinetics

Half-life
1 day
Tmax
2 h
Absorption
oral
Elimination
hepatic
Washout
7 days
Low-confidence pharmacokinetics
These figures are recorded as established rather than measured in a published PK study. Treat them as an order of magnitude. Anything downstream of them — accumulation, steady state, washout — inherits that uncertainty.

Dosing — what backs each figure

Pentosan polysulfate sodium has an FDA-approved oral label (ELMIRON, 100 mg three times daily for interstitial cystitis) carrying a pigmentary maculopathy warning, plus multiple published human osteoarthritis trials using parenteral dosing at 2 mg/kg SC weekly or 3 mg/kg IM weekly for 4-6 weeks. The oral and injectable routes serve different indications and are not interchangeable.

ClinicalApproved labelling or a published human trial

Handling and storage

No compound-specific stability data exists
Marketed as ELMIRON 100 mg oral gelatin-coated capsules; there is no lyophilised or reconstituted presentation. Label storage: 'Store at 20 °C to 25 °C (68 °F to 77 °F); excursions permitted to 15 °C to 30 °C (59 °F to 86 °F).' No light-protection or freeze-thaw instruction is given. The bulk drug substance is described in the label as a white odourless powder that is slightly hygroscopic and soluble in water to 50% at pH 6. General peptide handling still applies — reconstitute gently, keep it cold, keep it dark — but any specific figure you see quoted for this compound elsewhere is someone's assumption, not a measurement.

Safety

Commonly reported
  • ·Gastrointestinal discomfort
  • ·Headache
  • ·Nausea
Rarely reported
  • ·Serious bleeding events
  • ·Liver function abnormalities
Contraindications
  • ·Active bleeding disorders
  • ·Hypersensitivity to the compound
Drug interactions
  • ·Anticoagulants, as Pentosan Polysulfate may increase bleeding risk

Reported combinations

Reported as synergistic
  • ·Glucosamine, which may enhance cartilage protection
Reported as antagonistic
  • ·NSAIDs, which may increase gastrointestinal bleeding risk when combined

Combination claims in this dataset are largely unsourced and should be treated as folk knowledge until a citation appears beside them.

References (4)

Data provenance

Chemistry and citations on this page were checked against primary sources on 2026-08-14. Values that could not be verified were left blank rather than filled with a plausible guess.

Could not verify
molecularFormula, regulatory.wada, halfLife

Research use only
This profile is educational reference material. It is not medical advice, not a prescription, and not an endorsement of self-administration. Compounds discussed here are research chemicals and most are not approved for human therapeutic use.