Pentosan polysulfate

Also called pentosan polysulfate sodium, PPS, Elmiron (capsules), iPPS or Zilosul (Paradigm's injection), Zycosan and Cartrophen Vet (animal injections)1, 8, 11, 19

One repeating unit of pentosan polysulfate: a xylose sugar ring with two sulfate groups, as the sodium salt
Pentosan polysulfate repeating unitFull structure and downloads
StatusNot a peptideApproved for a different use
Evidence3/5For joints: small human studies, and the phase 3 knee trial failed its interim test
Status nowFDA-approved as Elmiron capsules for bladder pain from interstitial cystitis, with a warning about eye damage since 2020. Approved as an injection for arthritis in horses, not people.1, 2, 8
LatestSeptember 23, 2026: Paradigm's phase 3 knee osteoarthritis trial of injected pentosan met its futility rule at an interim look. The company went into voluntary administration on Sep 29.19, 21
NextParadigm's board says it plans to propose a deal with creditors to keep the company and its data alive, with "no assurance" it will be approved.24 No approval for joints is in sight. Full history

Pentosan polysulfate is not a peptide. It is a semi-synthetic chain of sulfated sugars made from beech-wood xylan, chemically similar to heparin.1, 7 In the US it is approved only as Elmiron capsules, for bladder pain or discomfort from interstitial cystitis.1 Since June 2020 its label has warned of retinal damage, called pigmentary maculopathy, with long-term use.2 Vets inject it for arthritis in horses and dogs. Animal products are sometimes injected by people for their own joints, a use no regulator has approved.8, 11 The human joint evidence is small. Paradigm Biopharmaceuticals' phase 3 knee trial failed its interim test in September 2026, and the company is in administration.19, 21

See every peptide's status in the regulatory tracker

In this guide
  1. Status and summary
  2. At a glance
  3. Where to get it
  4. Molecular structure
  5. What it is
  6. How it works
  7. Evidence map
  8. By goal
  9. How it's used
  10. Side effects
  11. Compared with
  12. Stacks
  13. Myths vs evidence
  14. All options
  15. Legal status history
  16. FAQ
  17. References

At a glance

What it isA sulfated sugar chain of 4,000 to 6,000 daltons. A weak blood thinner, about 1/15 as strong as heparin1, 7
Not a peptideIt contains no amino acids. It is listed here because it is sold and discussed alongside peptides
Best evidenceBladder pain: approved, though a 2015 trial found no benefit over placebo. Knee arthritis: small studies and a failed phase 3 interim1, 5, 19
Approved inUS and EU as capsules for bladder pain. US for horse arthritis, as an injection1, 6, 8
No good evidence forRebuilding cartilage in people, sports injuries, or any joint other than the knee
Legal statusPrescription drug. Using it for joints is off-label. Animal products are not approved for people1, 8
In sportNot named on WADA's 2026 list23
Main risksRetinal damage with long use. Bleeding, hair loss, stomach upset1, 2
Typical costElmiron needs a prescription. We don't list a price for off-label use

Where to get it

MoveWell sells nothing and links only to legal options. All options

PrescriptionElmiron capsules

Approved for bladder pain from interstitial cystitis, from a regular pharmacy. Not approved for joints.1

Details
Not for peopleHorse and dog injections

Zycosan is FDA-approved for horses only. Cartrophen Vet is a dog product. Neither is approved for human use.8, 11

Why
EndedKnee trial

Paradigm's phase 3 knee trial will not continue after failing its interim test.21

Status

Molecular structure

Not a chain of amino acids. A chain of xylose sugar rings, most carrying two sulfate groups. This shows one repeating unit; the wavy ends mark where the chain continues.

Pentosan polysulfate repeating unit: a xylose ring linked to its neighbors, with two sulfate groups highlighted and two sodium ions

The two sulfate groups that make it a "polysulfate"

Type
Semi-synthetic sulfated polysaccharide, not a peptide
Source
Xylan from beech wood
Unit
C5H6Na2O10S2, 336.2 g/mol
Chain weight
4,000 to 6,000 daltons, about 12 to 18 units
Salt
Sodium
Absorbed by mouth
About 6%

A simplified drawing: real batches are a mix of chain lengths. Source and weight from the label and a 2023 review; the unit formula is our calculation for a disulfated xylose unit.1, 7

What it is

Pentosan polysulfate is made by chemically adding sulfate groups to xylan, a sugar polymer taken from beech trees.7 The Elmiron label calls it a "heparin-like" carbohydrate that resembles the body's glycosaminoglycans, the sugar chains found in cartilage and the bladder lining.1 It is not a peptide. We cover it because it is often sold and discussed with injectable peptides for joints.

It comes in three main forms:

  • Elmiron capsules. FDA-approved for "the relief of bladder pain or discomfort associated with interstitial cystitis."1 The EU authorised it in 2017 for bladder pain syndrome with specific bladder findings.6
  • Animal injections. Zycosan was approved by FDA in December 2022 for arthritis signs in horses.8 Cartrophen Vet is authorised in some countries for arthritis in dogs.11, 12 FDA "strongly encourages" vets to use the approved horse product rather than unapproved or compounded pentosan.8
  • Paradigm's injection (iPPS, Zilosul). An investigational injection under the skin for knee osteoarthritis, with FDA Fast Track status.19

How it works

For joints, the case rests on lab and animal work.7

  • Cartilage cells. In lab studies it raised production of proteoglycans, key building blocks of cartilage.7
  • Inflammation and pain signals. It changed inflammatory signals and lowered nerve growth factor, a pain-related molecule, in cell studies.7
  • Blood flow. It is a weak anticoagulant that also helps break down clots.1, 7 A review says it may clear fat deposits from small vessels in the bone under cartilage.7

Only about 6% of an oral dose is absorbed.1 The joint products studied in people and animals are injected.8, 13

Evidence map

Each use is graded separately, because the evidence differs by use.

Bladder pain (interstitial cystitis)

FDA-approved on a modest trial result. A larger 2015 trial found no benefit over placebo

Knee osteoarthritis pain, injected

A 20-person open study and a small biomarker trial. The phase 3 trial failed its interim test

Rebuilding cartilage

Lab data and changes in blood and joint-fluid markers. No proof of cartilage regrowth in people

Sports injuries and other joints

Personal reports only, often with animal products

Scale: 5 FDA-approved, 4 strong human, 3 limited human, 2 animal or lab only, 1 anecdotal

Key studies

UseStudyModelFinding
Bladder painElmiron label trial1Human RCT n=151Pain improved by more than half in 38% vs 18% on placebo over 3 months
Bladder painNickel 20155Human RCT n=368Responders: 42.6% on the label dose vs 40.7% on placebo. "No treatment effect vs placebo"
Knee arthritisKumagai 201013Human n=20, no controlSix weekly injections. Pain and swelling improved for almost a year. Clotting tests changed
Knee arthritisPARA_OA_008, Skerrett 202614, 15Phase 2 RCT smallA cartilage-breakdown marker in joint fluid fell vs placebo. Not powered to show pain relief vs placebo
Knee arthritisPARA_OA_01218, 19Phase 3 538 treatedInterim result below the threshold to continue. Primary goal: pain at day 11217
Knee arthritisParadigm post hoc, Oct 202621Subgroup 16 sites in Australia, Moldova and Hong Kong; 95 with day-112 dataPain 1.1 points lower than placebo on a 0–10 scale. US sites favored placebo. Not independently verified
Horse arthritisZycosan field study10Animal 219 horsesSuccess in about 60% vs 36% on saline

Paradigm says operational problems at US sites left many missing pain scores, which counted against the drug in the interim analysis.19, 21 A company's own post hoc subgroup can't rescue a failed trial, but it may shape any future study. Paradigm also registered an earlier phase 2/3 knee trial, PARA_OA_002; we found no published results.16

By goal

Pick your goal to see what the evidence supports.

Elmiron capsulesAnimal injectionsParadigm injection
Approved forBladder pain, in peopleArthritis in horses or dogsNothing; investigational
Joint evidence in peopleNoneNoneSmall studies; phase 3 failed interim
Legal for joints in peopleOff-label, with a prescriptionNoTrial only, now ended

Sources: Elmiron label,1 FDA,8 Paradigm.21

How it's used

We don't give a dose for joints. None has been approved.

For interstitial cystitis, the Elmiron label dose is 300 mg a day, taken as one 100 mg capsule three times a day, with a review at 3 months.1 That is the label's dose for bladder pain only. The knee studies used injections under the skin, once or twice a week for about six weeks.13, 16 We report this as information, not instruction.

Side effects and who should avoid it

  • Retinal damage. Since June 2020 the label has warned of "pigmentary changes in the retina" with long-term use. Cumulative dose appears to be a risk factor, the changes may be permanent, and the label suggests a retinal exam within six months of starting and regular exams after that.1, 2 The first report described six patients who had taken it for a median of 15.5 years.3 A urogynecology society advises keeping total long-term exposure low.4
  • Bleeding. It is a weak blood thinner. In trials, 6.3% had rectal bleeding at the label dose. Bruising, nosebleeds and gum bleeding were also reported.1
  • Common side effects. Hair loss, diarrhea and nausea, each in about 4%, then headache and rash.1
  • Liver tests. Mild rises in liver enzymes in about 1.2%.1
  • Animal products in people. Zycosan is labeled "for intramuscular use in horses only."8 Animal products are not made or tested for human use.
  • Who should take extra care. People on blood thinners or with a bleeding risk, and people with a history of heparin-induced low platelets. Talk to a doctor first.1

Compared with

Pentosan polysulfateTB-500BPC-157
What it isSulfated sugar chain, not a peptide7-amino-acid peptide15-amino-acid peptide
Approved anywhereYes, for bladder pain and horse arthritisNoNo
Joint trials in peopleSmall studies; phase 3 failed interimNoneVery few, small
Main known riskRetinal damage, bleedingUnknownUnknown

Sources: Elmiron label,1 Paradigm.19 See our TB-500 and BPC-157 guides.

Stacks

We found no study of pentosan combined with BPC-157, TB-500 or other peptides. Because it thins the blood, combining it with other blood thinners, including aspirin and other anti-inflammatory painkillers, raises bleeding risk.1

Myths vs evidence

ClaimPentosan is a peptide
EvidenceNo. It is a sulfated sugar chain made from beech-wood xylan, with no amino acids.7
ClaimIt rebuilds cartilage
EvidenceNot shown in people. A phase 2 trial found changes in cartilage-breakdown markers, not cartilage regrowth.14
ClaimIt's FDA-approved for arthritis
EvidenceOnly for arthritis in horses. In people, it is approved only as capsules for bladder pain.1, 8
ClaimThe phase 3 knee trial is about to succeed
EvidenceIt met its futility rule in September 2026, and the company says it will not proceed.19, 21
ClaimHorse pentosan is the same drug, so it's fine for people
EvidenceThe active ingredient is related, but animal products are approved and tested for animals only.8

All options

MoveWell sells nothing. Checked November 1, 2026

Prescription

Elmiron capsules need a prescription and are approved for bladder pain from interstitial cystitis.1 A doctor may prescribe an approved drug off-label, but there is no approved human pentosan product for joints. Because pentosan is the active ingredient of an approved drug, a licensed 503A pharmacy may, in principle, compound it for a named patient with a prescription.22 We found no US pharmacy or telehealth service we could verify offering it for joints, so we list none.

Clinical trials

Paradigm's phase 3 knee trial is ending.21 We found no other open trial of pentosan for joints.

Veterinary products

Zycosan, Cartrophen Vet and similar products are for animals and need a vet's prescription.8, 11 We don't link them for human use.

FAQ

Is pentosan polysulfate a peptide?

No. It is a sulfated sugar chain, related to heparin. It has no amino acids.

Is it FDA-approved?

Yes, as Elmiron capsules for bladder pain from interstitial cystitis, and as Zycosan injections for arthritis in horses. It is not approved for joints in people.

Does it help knee arthritis?

Not proven. Small studies looked encouraging, but the phase 3 trial failed its interim test in September 2026.

Can it damage my eyes?

Yes, with long-term use. The label warns of retinal pigment changes that may be permanent, and suggests a retinal exam within six months of starting and regular exams after that.

Can I use the horse or dog version?

Those products are approved for animals only. They are not tested or made for people.

What dose do people use for joints?

We don't give one. No joint dose is approved.

Is it banned in sport?

It isn't named on WADA's 2026 list. Check with your anti-doping agency if you are tested.

References

24 sources, with links
  1. Elmiron (pentosan polysulfate sodium) capsules, prescribing information, revised Jul 2024 (Drugs.com copy of the FDA label). Link
  2. Elmiron prescribing information, revised Jun 2020, NDA 020193 supplement 14 (copy of the Drugs@FDA label hosted by Legal Examiner). PDF
  3. Pearce WA, Chen R, Jain N. Pigmentary maculopathy associated with chronic exposure to pentosan polysulfate sodium. Ophthalmology 2018;125(11):1793–1802. PMID 29801663
  4. American Urogynecologic Society. Practice advisory: possible drug-induced retinal maculopathy secondary to long-term use of pentosan polysulfate sodium (Elmiron) (Aug 2020). Link
  5. Nickel JC et al. Pentosan polysulfate sodium for treatment of interstitial cystitis/bladder pain syndrome: insights from a randomized, double-blind, placebo controlled study. J Urol 2015. Epistemonikos record
  6. European Medicines Agency. Elmiron: EPAR (authorised Jun 2, 2017). ema.europa.eu
  7. Smith MM, Melrose J. Pentosan polysulfate affords pleotropic protection to multiple cells and tissues. Pharmaceuticals 2023;16(3):437. DOI 10.3390/ph16030437
  8. FDA Center for Veterinary Medicine. FDA approves first injectable pentosan for osteoarthritis in horses (Dec 20, 2022). fda.gov
  9. AVMA News. FDA approves first injectable pentosan for osteoarthritis in horses (Dec 26, 2022). Link
  10. EquiManagement. Pentosan shown to control clinical signs of osteoarthritis in horses. Link
  11. Swedish Medical Products Agency. Cartrophen vet 100 mg/ml solution for injection for dogs, package leaflet. PDF
  12. VCA Animal Hospitals. Pentosan polysulfate sodium. Link
  13. Kumagai K et al. Sodium pentosan polysulfate resulted in cartilage improvement in knee osteoarthritis: an open clinical trial. BMC Clin Pharmacol 2010;10:7. DOI 10.1186/1472-6904-10-7
  14. Paradigm Biopharmaceuticals. iPPS phase 2 biomarker results published in Arthritis Research & Therapy (ASX release, Jan 28, 2026). PDF
  15. Biotech Dispatch. Peer-reviewed validation strengthens Paradigm's osteoarthritis program (Jan 29, 2026). Link
  16. PARA_OA_002, NCT04809376 (registry mirror). Link
  17. PARA_OA_012, NCT06917404 (registry mirror). Link
  18. Paradigm Biopharmaceuticals. DSMB safety review of PARA_OA_012 (ASX release, Aug 13, 2026). PDF
  19. Paradigm Biopharmaceuticals. Phase 3 interim result below continuation threshold (ASX release, Sep 23, 2026). PDF
  20. Biotech Dispatch. Disappointment for Paradigm as phase 3 knee osteoarthritis trial below continuation threshold (Sep 23, 2026). Link
  21. Paradigm Biopharmaceuticals (Administrators Appointed). Update on PARA_OA_012 (ASX release, Oct 15, 2026). PDF
  22. FDA. Bulk drug substances used in compounding under section 503A of the FD&C Act. fda.gov
  23. World Anti-Doping Agency. 2026 Prohibited List (copy hosted by SEGAS). PDF
  24. Kalkine Media. Paradigm Biopharmaceuticals enters voluntary administration following phase 3 trial futility in September quarter (summary of the company's quarterly report, Oct 30, 2026). Link

This page is for education and is not medical advice. Pentosan polysulfate is not approved for joint use in people. Talk to a clinician before using it.