tissue factor pathway inhibitor

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Ligands
tissue factor pathway inhibitor (Human)

GtoPdb Ligand ID: 11181

Compound class: Endogenous peptide in human, mouse or rat

Comment: TFPI is a serine protease inhibitor that regulates the tissue factor (TF)-dependent blood coagulation pathway (extrinsic pathway). It inhibits activated factor X (Xa) and VIIa-TF proteases in an autoregulatory loop. Some isoforms are tethered to the cell membrane by expression of a glycosylphosphatidylinositol (GPI) anchor, others isoforms are secreted [1-2]. Inhibition of the TFPI restores hemostasis, which is a mechanism being exploited for therapeutic benefit in inherited bleeding disorders.

Species: Human

References
1. Hansen L, Petersen LC, Lauritzen B, Clausen JT, Grell SN, Agersø H, Sørensen BB, Hilden I, Almholt K. (2014) Target-mediated clearance and bio-distribution of a monoclonal antibody against the Kunitz-type protease inhibitor 2 domain of Tissue Factor Pathway Inhibitor. Thromb Res, 133 (3): 464-71. [PMID:24393663]
2. Hilden I, Lauritzen B, Sørensen BB, Clausen JT, Jespersgaard C, Krogh BO, Bowler AN, Breinholt J, Gruhler A, Svensson LA et al.. (2012) Hemostatic effect of a monoclonal antibody mAb 2021 blocking the interaction between FXa and TFPI in a rabbit hemophilia model. Blood, 119 (24): 5871-8. [PMID:22563084]
3. Parng C, Singh P, Pittman DD, Wright K, Leary B, Patel-Hett S, Rakhe S, Stejskal J, Peraza M, Dufield D et al.. (2018) Translational Pharmacokinetic/Pharmacodynamic Characterization and Target-Mediated Drug Disposition Modeling of an Anti-Tissue Factor Pathway Inhibitor Antibody, PF-06741086. J Pharm Sci, 107 (7): 1995-2004. [PMID:29571739]

References

1. Hansen L, Petersen LC, Lauritzen B, Clausen JT, Grell SN, Agersø H, Sørensen BB, Hilden I, Almholt K. (2014)
Target-mediated clearance and bio-distribution of a monoclonal antibody against the Kunitz-type protease inhibitor 2 domain of Tissue Factor Pathway Inhibitor.
Thromb Res, 133 (3): 464-71. [PMID:24393663]

2. Hilden I, Lauritzen B, Sørensen BB, Clausen JT, Jespersgaard C, Krogh BO, Bowler AN, Breinholt J, Gruhler A, Svensson LA et al.. (2012)
Hemostatic effect of a monoclonal antibody mAb 2021 blocking the interaction between FXa and TFPI in a rabbit hemophilia model.
Blood, 119 (24): 5871-8. [PMID:22563084]

3. Parng C, Singh P, Pittman DD, Wright K, Leary B, Patel-Hett S, Rakhe S, Stejskal J, Peraza M, Dufield D et al.. (2018)
Translational Pharmacokinetic/Pharmacodynamic Characterization and Target-Mediated Drug Disposition Modeling of an Anti-Tissue Factor Pathway Inhibitor Antibody, PF-06741086.
J Pharm Sci, 107 (7): 1995-2004. [PMID:29571739]