Ensereptide (PXL01) is a polypeptide derived from human lactoferrin. PXL01 has several mechanisms of action; including immunomodulation and enhancement of fibrinolytic activity. PXL01 produces its immunomodulatory action by inhibiting the release of pro-inflammatory cytokines, such as IL-1β, IL-6 and Il-8 as well as TNF- α (tumor necrosis factor alpha). PXL01 also inhibits the local production of PAI-1 which is an important mediator of fibrinolysis. The anti-inflammatory properties combined with the modulation of fibrinolysis are assumed to account for the ability of the product candidate to prevent post-surgical adhesions and scar formation. Ensereptide (PXL01) is being developed by ProMore Pharma for the treatment of post-surgical adhesions and for prevention of dermal scarring after surgery or trauma.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| PXL01 in sodium hyaluronate for improvement of hand recovery after flexor tendon repair surgery: randomized controlled trial. | 2014 |
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| Effect of lactoferrin peptide (PXL01) on rabbit digit mobility after flexor tendon repair. | 2012-12 |
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| A lactoferrin-derived peptide (PXL01) for the reduction of adhesion formation in flexor tendon surgery: an experimental study in rabbits. | 2011-10 |
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| Effect of major abdominal surgery on the host immune response to infection. | 2010-06 |
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| A novel polypeptide derived from human lactoferrin in sodium hyaluronate prevents postsurgical adhesion formation in the rat. | 2009-12 |
Patents
| Substance Class |
Protein
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| Protein Sub Type | |
| Sequence Type | COMPLETE |
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SMV73KW49C
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| Record Status |
Validated (UNII)
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SMV73KW49C
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TARGET->INHIBITOR OF EXPRESSION |
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TARGET->INHIBITOR OF EXPRESSION |
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TARGET->ACTIVATOR OF EXPRESSION |
Increased expression of PRG4 mRNA in tendons treated with rabPXL01 in HA, but not in tendon sheaths. In addition, treatment with rabPXL01 in HA led to repression of the mRNA levels for the pro-inflammatory mediators interleukin (IL)-1?, IL-6, and IL-8 in tendon sheaths.
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TARGET->INHIBITOR OF EXPRESSION |
Increased expression of PRG4 mRNA in tendons treated with rabPXL01 in HA, but not in tendon sheaths. In addition, treatment with rabPXL01 in HA led to repression of the mRNA levels for the pro-inflammatory mediators interleukin (IL)-1?, IL-6, and IL-8 in tendon sheaths.
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ACTIVE MOIETY |
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
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| AMINO ACID SUBSTITUTION | [1_1] | Glu | ACETYL GLUTAMIC ACID | MA61H539YZ | ||
| AMINO ACID SUBSTITUTION | [1_25] | Arg | ARGININAMIDE, L- | 29626ZE0WY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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