alpha1-proteinase inhibitor

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Ligands
alpha1-proteinase inhibitor

GtoPdb Ligand ID: 7487

alpha1-proteinase inhibitor is an approved drug

Compound class: Peptide or derivative

Comment: This is the human protein isolated and purified from donor plasma. There are 4 approved versions (Prolastin-C [7], Zemaira [6], Aralast [4] and Glassia [5]), which show minor chemical differences as a result of the methods used during purification [2]. PEGylated recombinant alpha-1-proteinase inhibitor has been tested [1,3], but no recombinant protein drug as been approved to date.
US FDA approval dates: Prolastin-C (1987), Zemaira (2003), Aralast (2010) and Glassia (2010).

References
1. Hubbard RC, McElvaney NG, Sellers SE, Healy JT, Czerski DB, Crystal RG. (1989) Recombinant DNA-produced alpha 1-antitrypsin administered by aerosol augments lower respiratory tract antineutrophil elastase defenses in individuals with alpha 1-antitrypsin deficiency. J Clin Invest, 84 (4): 1349-54. [PMID:2794066]
2. Kolarich D, Turecek PL, Weber A, Mitterer A, Graninger M, Matthiessen P, Nicolaes GA, Altmann F, Schwarz HP. (2006) Biochemical, molecular characterization, and glycoproteomic analyses of alpha(1)-proteinase inhibitor products used for replacement therapy. Transfusion, 46 (11): 1959-77. [PMID:17076852]
3. Mast AE, Salvesen G, Schnebli HP, Pizzo SV. (1990) Evaluation of the rapid plasma elimination of recombinant alpha 1-proteinase inhibitor: synthesis of polyethylene glycol conjugates with improved therapeutic potential. J Lab Clin Med, 116 (1): 58-65. [PMID:2376698]
4. Mordwinkin NM, Louie SG. (2007) Aralast: an alpha 1-protease inhibitor for the treatment of alpha-antitrypsin deficiency. Expert Opin Pharmacother, 8 (15): 2609-14. [PMID:17931094]
5. Sandhaus RA, Stocks J, Rouhani FN, Brantly M, Strauss P. (2014) Biochemical efficacy and safety of a new, ready-to-use, liquid alpha-1-proteinase inhibitor, GLASSIA (alpha1-proteinase inhibitor (human), intravenous). COPD, 11 (1): 17-25. [PMID:23822603]
6. Stocks JM, Brantly M, Pollock D, Barker A, Kueppers F, Strange C, Donohue JF, Sandhaus R. (2006) Multi-center study: the biochemical efficacy, safety and tolerability of a new alpha1-proteinase inhibitor, Zemaira. COPD, 3 (1): 17-23. [PMID:17175661]
7. Stocks JM, Brantly ML, Wang-Smith L, Campos MA, Chapman KR, Kueppers F, Sandhaus RA, Strange C, Turino G. (2010) Pharmacokinetic comparability of Prolastin®-C to Prolastin® in alpha₁-antitrypsin deficiency: a randomized study. BMC Clin Pharmacol, 10: 13. [PMID:20920295]

References

1. Hubbard RC, McElvaney NG, Sellers SE, Healy JT, Czerski DB, Crystal RG. (1989)
Recombinant DNA-produced alpha 1-antitrypsin administered by aerosol augments lower respiratory tract antineutrophil elastase defenses in individuals with alpha 1-antitrypsin deficiency.
J Clin Invest, 84 (4): 1349-54. [PMID:2794066]

2. Kolarich D, Turecek PL, Weber A, Mitterer A, Graninger M, Matthiessen P, Nicolaes GA, Altmann F, Schwarz HP. (2006)
Biochemical, molecular characterization, and glycoproteomic analyses of alpha(1)-proteinase inhibitor products used for replacement therapy.
Transfusion, 46 (11): 1959-77. [PMID:17076852]

3. Mast AE, Salvesen G, Schnebli HP, Pizzo SV. (1990)
Evaluation of the rapid plasma elimination of recombinant alpha 1-proteinase inhibitor: synthesis of polyethylene glycol conjugates with improved therapeutic potential.
J Lab Clin Med, 116 (1): 58-65. [PMID:2376698]

4. Mordwinkin NM, Louie SG. (2007)
Aralast: an alpha 1-protease inhibitor for the treatment of alpha-antitrypsin deficiency.
Expert Opin Pharmacother, 8 (15): 2609-14. [PMID:17931094]

5. Sandhaus RA, Stocks J, Rouhani FN, Brantly M, Strauss P. (2014)
Biochemical efficacy and safety of a new, ready-to-use, liquid alpha-1-proteinase inhibitor, GLASSIA (alpha1-proteinase inhibitor (human), intravenous).
COPD, 11 (1): 17-25. [PMID:23822603]

6. Stocks JM, Brantly M, Pollock D, Barker A, Kueppers F, Strange C, Donohue JF, Sandhaus R. (2006)
Multi-center study: the biochemical efficacy, safety and tolerability of a new alpha1-proteinase inhibitor, Zemaira.
COPD, 3 (1): 17-23. [PMID:17175661]

7. Stocks JM, Brantly ML, Wang-Smith L, Campos MA, Chapman KR, Kueppers F, Sandhaus RA, Strange C, Turino G. (2010)
Pharmacokinetic comparability of Prolastin®-C to Prolastin® in alpha₁-antitrypsin deficiency: a randomized study.
BMC Clin Pharmacol, 10: 13. [PMID:20920295]