More than 27 million Americans are affected by osteoarthritis, a degenerative disease that is the most common form of arthritis.
Osteoarthritis (OA) is caused by a breakdown of cartilage – the tissue that covers the ends of bones where they form a joint. Healthy cartilage allows bones to glide over one another, and it absorbs energy from the shock of physical movement. In osteoarthritis, the surface layer of cartilage breaks down and wears away. This results in bones under the cartilage rubbing together, causing pain, swelling, and stiffness. Bone spurs can develop, permanently changing the joint’s shape.
OA is by far the most common form of arthritis and has a growing impact on health care. Even now, there is no therapeutic agent that works directly on OA. However, a drug called pentosan polysulfate (PPS) is showing great promise for the treatment of OA.
In addition to arthritis it has beneficial properties in many other tissue processes such as cartilage protection, sports medical applications in joint tissue repair, stimulation of stem cells and differentiation of stem cells in repair biology, as well as anti-viral, anti-bacterial and anti-tumor properties. Pentosan is a multifunctional tissue-protective molecule of potential therapeutic application for a diverse range of disease processes.
Pentosan polysulfate sodium (PPS) Uses
Australian researcher and physician, Dr. Peter Ghosh from the University of Sydney has brought an old drug back into the light for arthritis sufferers. The drug is called pentosan polysulfate sodium (known in medical circles as PPS). To date, trials of the drug involving human patients have been proven highly successful. As PPS eliminates pain associated with arthritic disease by acting on bone marrow lesions that cause pain and cartilage degeneration. By controlling these lesions there is a reduction in symptoms and pain.
PPS is a very safe drug and has been successfully used for 70 years to treat urinary infections in women and is FDA-approved and used for the treatment of interstitial cystitis (or painful bladder syndrome), deep vein thrombosis and is fast tracked for use in osteoarthritis. The drug is neither an anabolic steroid nor an opioid-based pain reliever so is not considered to enhance performance.
Established and potential new therapeutic applications for Pentosan
The benefits of pentosan polysulfate include:
- Treats bone marrow edema lesions (BMLs)
- Sports medicine treatment of damaged joint tissues including tendons, menisci, and articular cartilage (Limiting cartilage deterioration & promoting new cartilage formation)
- Promotion of tissue repair and regeneration and pain relief in OA/RA
- Inhibition of Nerve Growth Factor production by osteocytes providing pain relief in OA/RA
- Stimulation of Hyaluronic acid synthesis by synoviocytes, fibroblasts
- Anti-inflammation: regulation of cytokine and inflammatory mediator production & inhibition of leucocyte trafficking in inflamed tissues
- Promotion of Intervertebral disc disease repair and regeneration and alleviation of low back pain
- Modulation of vascular coagulation, fibrinolysis and thrombocytopenia
- Promotion of protease inhibitor efficiency in tissues offering greater protection from proteolysis
- Thickening the joint fluid – thus acting as a better lubricant. Improving blood supply to the joint, in turn helping it heal. By virtue of these actions, it provides pain relief for a much longer period of time
- Prevention of lipid accumulation in blood vessels in atherosclerosis
- Anti-viral prevention of host cell infection/viral replication. Inhibits in vitro replication of HIV and other enveloped viruses
- Promotion of stromal Mesenchymal stem cells differentiation/proliferation/expansion for repair biology applications
Side Effects of Pentosan
Common side effects of PPS include swelling, headache, dizziness, nausea, indigestion, malaise and diarrhea.
how does pentosan work in arthritis?
In osteoarthritis, pentosan reduces the destruction of cartilage by affecting inflammatory mediators. It also increases the number of proteoglycans into the extracellular matrix. Proteoglycans are important because they allow tissues like collagen to withstand compression and swelling forces. Joint cartilage also contains Proteoglycans.
In the synovium, the part that surrounds the inner lining of your joint, pentosan increases both the production and the molecular weight of hyaluronan. Hyaluronan or Hyaluronic acid is a compound that occurs naturally in your body, and it is responsible for attracting and retaining moisture. Pentosan also has another anti-inflammatory function due to its fibrinolytic activity. This activity improves the blood flow not only in the synovium but also in the subchondral bone.
Nerve growth factor production in osteocytes is inhibited by Pentosan, reducing bone pain in osteoarthritis and rheumatoid arthritis (OA/RA). It also removes fatty compounds from lipid-engorged subchondral blood vessels in OA/RA cartilage, reducing joint pain.
Pentosan Polysulfate Studies
Recently, Paradigm Pharmaceuticals an Australian biotech company doing studies on Pentosan had reported an average 51.2% reduction in chronic knee pain by a group of osteoarthritis patients being treated with its injectable Pentosan Polysulfate Sodium drug. Researchers hope that it may work as well in relieving pain in other parts of the body.
Paradigm Biopharmaceuticals also concluded a phase 2A clinical trials of Pentosan Polysulfate to treat viral arthritis caused by mosquito-borne alphavirus infections, including the debilitating Ross River virus (RRV) and chikungunya virus (CHIKV). The clinical trials passed both safety and efficacy measures amongst participants with chronic RRV-induced arthralgia who were treated with the injectable pentosan polysulfate sodium (PPS). At their three-month follow-up, 72.7% of the study participants treated with PPS showed near remission of symptoms in contrast to those participants who were administered with a placebo (14.3%).
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In Vitro and In Vivo.
Pentosan Polysulfate Demonstrates Anti-human T-Cell Leukemia Virus Type 1 Activities