Pentosan polysulfate sodium (brand name ELMIRON) is a low molecular weight heparin-like compound. It has anticoagulant and fibrinolytic effects and is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis. The mechanism of action of pentosan polysulfate sodium in interstitial cystitis is not known but was discovered, that it t binds Fibroblast growth factors (FGFs) as well as other heparin-binding growth factors.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2095217 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | ELMIRON Approved UseELMIRON® (pentosan polysulfate sodium) is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis. Launch Date8.4369598E11 |
PubMed
Title | Date | PubMed |
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[Thrombopenia and fatal intracerebral hemorrhage caused by pentosan polysulfate]. | 1988 Jan 30 |
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Pentosan induced cerebral sagittal sinus thrombosis: a variant of heparin induced thrombocytopenia. | 1998 Dec |
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Effect of pentosan polysulfate therapy on intravesical potassium sensitivity. | 2002 Mar |
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Toxicity and carcinogenicity of Elmiron in F344/N rats and B6C3F1 mice following 2 years of gavage administration. | 2003 Dec |
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Metabolism of [3H]pentosan polysulfate sodium (PPS) in healthy human volunteers. | 2005 Aug |
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Cyclophosphamide induced hemorrhagic cystitis successfully treated with pentosanpolysulphate. | 2005 Jan |
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Sulfated dextrans enhance in vitro amplification of bovine spongiform encephalopathy PrP(Sc) and enable ultrasensitive detection of bovine PrP(Sc). | 2010 Oct 4 |
Sample Use Guides
The recommended dose of ELMIRON® (pentosan polysulfate sodium, capsules) 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.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22214865
Effect of pentosan polysulfate (PPS) on p38, ERK1/2 and JNK MAPK activation was studied. Canine chondrocytes were plated onto 6-well culture plates in serum free DMEM for 24 hr. Cells were pre-treated with 100 µg/ml of PPS for 1 hr and then incubated with 10 ng/ml of recombinant human (rh) IL-1β for 5, 15, 30, 60 or 240 min. It was shown, that phosphorylation of p38 and ERK were inhibited by 100 mg/ml of PPS, while JNK remained constant despite PPS pretreatment prior to rhIL-1β stimulation. Effect of PPS on NF-κB translocation induced by rhIL- 1β: Under control conditions, a diffuse cytoplasmic staining was seen and the average percentage of NF-κB positive nuclei cells was 9.5%. On the other hand, 78.2% of chondrocytes incubated with rhIL- 1β had a nuclear staining pattern, indicating NF-κB nuclear translocation. Preincubation with 10 and 100 µg/ml PPS reduced NF-κB translocation rate.
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LIVERTOX |
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FDA ORPHAN DRUG |
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N0000007893
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SUBSTANCE RECORD