marstacimab

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Ligands
marstacimab

GtoPdb Ligand ID: 13403

Synonyms: Hympavzi® | marstacimab-hncq

marstacimab is an approved drug (EMA & FDA (2024))

Comment: Marstacimab (PF-06741086) is a monoclonal antibody that targets tissue factor pathway inhibitor (TFPI) [4]. The antibody blocks the inhibitory effect of TFPI on the FVIIa-TF complex interaction with coagulation factor Xa. This mechanism is proposed to increase coagulation activity of both the intrinsic and extrinsic coagulation pathways, for example in patients with severe haemophilia A or B.

References
1. Cardinal M, Kantaridis C, Zhu T, Sun P, Pittman DD, Murphy JE, Arkin S. (2018) A first-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of PF-06741086, an anti-tissue factor pathway inhibitor mAb, in healthy volunteers. J Thromb Haemost, 16 (9): 1722-1731. [PMID:29908043]
2. Lamb YN. (2024) Marstacimab: First Approval. Drugs, [Epub ahead of print]. [PMID:39715914]
3. Mahlangu J, Luis Lamas J, Cristobal Morales J, Malan DR, Teeter J, Charnigo RJ, Hwang E, Arkin S. (2023) Long-term safety and efficacy of the anti-tissue factor pathway inhibitor marstacimab in participants with severe haemophilia: Phase II study results. Br J Haematol, 200 (2): 240-248. [PMID:36220152]
4. 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. Cardinal M, Kantaridis C, Zhu T, Sun P, Pittman DD, Murphy JE, Arkin S. (2018)
A first-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of PF-06741086, an anti-tissue factor pathway inhibitor mAb, in healthy volunteers.
J Thromb Haemost, 16 (9): 1722-1731. [PMID:29908043]

2. Lamb YN. (2024)
Marstacimab: First Approval.
Drugs, [Epub ahead of print]. [PMID:39715914]

3. Mahlangu J, Luis Lamas J, Cristobal Morales J, Malan DR, Teeter J, Charnigo RJ, Hwang E, Arkin S. (2023)
Long-term safety and efficacy of the anti-tissue factor pathway inhibitor marstacimab in participants with severe haemophilia: Phase II study results.
Br J Haematol, 200 (2): 240-248. [PMID:36220152]

4. 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]