Pentosan Polysulfate

• ELMIRON ® (pentosan polysulfate sodium) is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis.

• ELMIRON ® is contraindicated in patients with known hypersensitivity to the drug, structurally related compounds, or excipients.contraindicated

The recommended dose of ELMIRON ® is 300 mg/day taken as one 100 mg capsule orally three times daily. The capsules should be taken with water at least 1 hour before meals or 2 hours after meals. Patients receiving ELMIRON ® should be reassessed after 3 months. If improvement has not occurred and if limiting adverse events are not present, ELMIRON ® may be continued for another 3 months. The clinical value and risks of continued treatment in patients whose pain has not improved by 6 months is not known.

Retinal Pigmentary Changes Pigmentary changes in the retina, reported in the literature as pigmentary maculopathy, have been identified with long-term use of ELMIRON ® (see ADVERSE REACTIONS ). Although most of these cases occurred after 3 years of use or longer, cases have been seen with a shorter duration of use. While the etiology is unclear, cumulative dose appears to be a risk factor. Visual symptoms in the reported cases included difficulty reading, slow adjustment to low or reduced light environments, and blurred vision. The visual consequences of these pigmentary changes are not fully characterized. Caution should be used in patients with retinal pigment changes from other causes in which examination findings may confound the appropriate diagnosis, follow-up, and treatment. Detailed ophthalmologic history should be obtained in all patients prior to starting treatment with ELMIRON ® . If there is a family history of hereditary pattern dystrophy, genetic testing should be considered. For patients with pre-existing ophthalmologic conditions, a comprehensive baseline retinal examination (including color fundoscopic photography, ocular coherence tomography (OCT), and auto-fluorescence imaging) is recommended prior to starting therapy. A baseline retinal examination (including OCT and auto-fluorescence imaging) is suggested for all patients within six months of initiating treatment and periodically while continuing treatment.

ELMIRON ® was evaluated in clinical trials in a total of 2627 patients (2343 women, 262 men, 22 unknown) with a mean age of 47 [range 18 to 88 with 581 (22%) over 60 years of age]. Of the 2627 patients, 128 patients were in a 3-month trial and the remaining 2499 patients were in a long-term, unblinded trial. Deaths occurred in 6/2627 (0.2%) patients who received the drug over a period of 3 to 75 months. The deaths appear to be related to other concurrent illnesses or procedures, except in one patient for whom the cause was not known. Serious adverse events occurred in 33/2627 (1.3%) patients. Two patients had severe abdominal pain or diarrhea and dehydration that required hospitalization. Because there was not a control group of patients with interstitial cystitis who were concurrently evaluated, it is difficult to determine which events are associated with ELMIRON ® and which events are associated with concurrent illness, medicine, or other factors. Adverse Experience in Placebo-Controlled Clinical Trials of ELMIRON ® 100 mg Three Times a Day for 3 Months Body System/Adverse Experience ELMIRON ® n=128 Placebo n=130 CNS Overall Number of Patients Within a body system, the individual events do not sum to equal overall number of patients because a patient may have more than one event.

Pregnancy Reproduction studies have been performed in mice and rats with intravenous daily doses of 15 mg/kg, and in rabbits with 7.5 mg/kg. These doses are 0.42 and 0.14 times the daily oral human doses of ELMIRON ® when normalized to body surface area. These studies did not reveal evidence of impaired fertility or harm to the fetus from ELMIRON ® . Direct in vitro bathing of cultured mouse embryos with pentosan polysulfate sodium (PPS) at a concentration of 1 mg/mL may cause reversible limb bud abnormalities. Adequate and well-controlled studies have not been performed in pregnant women. Because animal studies are not always predictive of human response, this drug should be used in pregnancy only if clearly needed.

Metabolism

Absorption In a clinical pharmacology study in which healthy female volunteers received a single oral 300 or 450 mg dose of pentosan polysulfate sodium containing radiolabeled drug as a solution under fasted conditions, maximal levels of plasma radioactivity were seen approximately at a median of 2 hours (range 0.6-120 hours) after dosing. Based on urinary excretion of radioactivity, a mean of approximately 6% of a radiolabeled oral dose of pentosan polysulfate sodium is absorbed and reaches the systemic circulation.

Overdose has not been reported. Based upon the pharmacodynamics of the drug, toxicity is likely to be reflected as anticoagulation, bleeding, thrombocytopenia, liver function abnormalities, and gastric distress (see CLINICAL PHARMACOLOGY and PRECAUTIONS ). At a daily dose of 900 mg for 32 weeks (n=127) in a clinical trial, rectal hemorrhage was reported as an adverse event in 15% of patients. At a daily dose of ELMIRON ® 900 mg for 16 weeks in a clinical trial that enrolled 51 patients in the ELMIRON ® group and 49 in the placebo group, elevated liver function tests were reported as an adverse event in 11.8% of patients in the ELMIRON ® group and 2% of patients in the placebo group. In the event of acute overdosage, the patient should be given gastric lavage if possible, carefully observed and given symptomatic and supportive treatment.

• Sep 26, 1996NDANDA020193Janssen Pharms

1. 1Maculopathy1,39120%
2. 2Off Label Use1,38920%
3. 3Retinal Pigmentation6078.9%
4. 4Dry Age-related Macular Degeneration5608.2%
5. 5Pigmentary Maculopathy4576.7%
6. 6Drug Ineffective3435.0%
7. 7Pain3044.4%
8. 8Product Use Issue2724.0%
9. 9Nausea2673.9%
10. 10Headache2353.4%
11. 11Cystitis Interstitial2133.1%
12. 12Macular Degeneration2123.1%
13. 13Diarrhoea2073.0%
14. 14Alopecia2063.0%
15. 15Fatigue1992.9%

Recent PubMed references pinned to Pentosan Polysulfate as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Retrospective study of visual acuity changes in patients with interstitial cystitis receiving pentosan polysulfate sodium.
  Current medical research and opinion · 2026 · Yuan Z, Vaughan S, Jeffcoat C, et al.
  PMID 41989996DOI 10.1080/03007995.2026.2656538
• Spectrum of Colopathy and Severe Polyposis Associated With Pentosan Polysulfate Sodium Maculopathy: A Retrospective Case Series.
  American journal of ophthalmology · 2026 · Feo A, Popovic MM, Faghihi S, et al.
  PMID 41785987DOI 10.1016/j.ajo.2026.02.050
• Effects of pentosan polysulfate sodium on joint structure and function out to six months in naturally-occurring canine osteoarthritis.
  PloS one · 2026 · Stapledon CJM, Krishnan R, Peat RA, et al.
  PMID 41666203DOI 10.1371/journal.pone.0342409
• Effects of pentosan polysulfate sodium on synovial fluid biomarkers in moderate to severe knee osteoarthritis: an exploratory, phase 2, randomized, double-blind, placebo-controlled trial.
  Arthritis research & therapy · 2026 · Skerrett DL, Stapledon CJM, Ahuja M, et al.
  PMID 41588475DOI 10.1186/s13075-026-03740-x
• Pentosan Polysulfate Maculopathy Following Subcutaneous Injections for Arthritis.
  JAMA ophthalmology · 2026 · Fung AT, Sarraf D, Carrillo JM, et al.
  PMID 41379439DOI 10.1001/jamaophthalmol.2025.5069
• A review of the clinical efficacy and adverse effects of disease modifying osteoarthritic drugs (DMOADs) in dogs with special focus on glucosamine and pentosan polysulfate; do they work?
  The Journal of veterinary medical science · 2025 · Bwalya EC, Wijekoon HS, Okumura M, et al.
  PMID 41183983DOI 10.1292/jvms.25-0293
• BPS symptom load during pentosane polysulfate sodium treatment in real life in France.
  The French journal of urology · 2025 · Saussine C, Gamé X, Levesque A, et al.
  PMID 40972775DOI 10.1016/j.fjurol.2025.102972
• Pentosan polysulfate maculopathy: clinical considerations, pathobiology, and causality.
  Progress in retinal and eye research · 2025 · Hall BP, Shiromani S, Vanderbeek BL, et al.
  PMID 40962246DOI 10.1016/j.preteyeres.2025.101400

The 10 most recently updated of 16 ClinicalTrials.gov registrations naming Pentosan Polysulfate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Investigate the Treatment Effect of Subcutaneous Injections of Pentosan Polysulfate Sodium Compared With Placebo in Adult Participants With Knee Osteoarthritis Pain.
  Recruiting · Phase 3 · Interventional · 466 enrolled · Paradigm Biopharmaceuticals Ltd.
  NCT06917404updated 2026-05-08
• A 3-Arm Study on G7 Acetabular Cup With Echo BiMetric Stem in Total Hip Arthroplasty
  Active not recruiting · Interventional · 360 enrolled · Zimmer Biomet
  NCT02518269updated 2025-11-25
• Evaluate the Efficacy and Safety of U101 Oral Capsules in the Prevention of Uncomplicated rUTIs in Women
  Recruiting · Phase 3 · Interventional · 348 enrolled · TCM Biotech International Corp.
  NCT07184827updated 2025-09-22
• Treatment and Duration Effect of Pentosan Polysulfate Sodium (PPS) in Participants With Knee Osteoarthritis Pain
  Completed · Observational · 133 enrolled · Paradigm Biopharmaceuticals Ltd.
  NCT04814719updated 2025-07-22
• A Study of Pentosan Polysulfate Sodium and the Development of Pigmentary Maculopathy and Pigmentary Retinopathy
  Completed · Observational · 2 enrolled · Janssen Research & Development, LLC
  NCT05179460updated 2025-06-26
• Pentosan Polysulfate Treatment's Effectiveness
  Completed · Interventional · 37 enrolled · Hisar Intercontinental Hospital
  NCT05744908updated 2025-05-22
• Intravesical Ozone Therapy for Interstitial Cystitis/Bladder Pain Syndrome
  Not yet recruiting · Interventional · 60 enrolled · Medipol University
  NCT06863220updated 2025-04-27
• Inhibitory Effect of a Polyphenol Supplement on Dietary Iron Absorption in Adults with Thalassemia
  Completed · Interventional · 20 enrolled · Swiss Federal Institute of Technology
  NCT05326503updated 2025-03-05
• Treatment Effects of Subcutaneous Injections of Pentosan Polysulfate Sodium vs Placebo in Participants With Knee OA Pain
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 602 enrolled · Paradigm Biopharmaceuticals USA (INC)
  NCT04809376updated 2024-04-08
• Radiation Cystitis Treated With Pentosan Polysulfate Sodium Trial
  Recruiting · Phase 2 · Phase 3 · Interventional · 72 enrolled · National Taiwan University Hospital
  NCT05245591updated 2022-05-04

Frequently asked questions

What is Pentosan Polysulfate used for?

According to FDA labeling, Pentosan Polysulfate carries indications including: ELMIRON ® (pentosan polysulfate sodium) is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Pentosan Polysulfate?

Pentosan Polysulfate is classified as Glycosaminoglycan.

What are the brand names for Pentosan Polysulfate?

Pentosan Polysulfate is marketed under brand names including Elmiron, Zycosan.

What are the contraindications for Pentosan Polysulfate?

Pentosan Polysulfate labeling lists contraindications including: ELMIRON ® is contraindicated in patients with known hypersensitivity to the drug, structurally related compounds, or excipients.. Always consult the full prescribing information and a clinician.