| Primary information |
|---|
| ThPP ID | Th1047 |
| Therapeutic Peptide/Protein Name | Alpha-1-proteinase inhibitor |
| Sequence | EDPQGDAAQKTDTSHHDQDHPTFNKITPNLAEFAFSLYRQLAHQSNSTNI view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 44324.5 |
| Chemical Formula | C2001H3130N514O601S10 |
| Isoelectric Point | 5.37 |
| Hydrophobicity | -0.302 |
| Melting Point (℃) | 59 |
| Half Life | N.A. |
| Description | Human alpha-1 proteinase inhibitor or alpha-1-antitrypsin, prepared from human plasma via Cohn alcohol fractionation followed by PEG and zinc chloride fractionation. |
| Indication/Disease | For treatment of panacinar emphysema. |
| Pharmacodynamics | Prevents excessive accumulation of active neutrophil elastase and consequent proteolysis of elastin tissues in alveolar lung structures. This prevents the development of emphysema. |
| Mechanism of Action | Alpha-1 proteinase inhibitor is a serine protease inhibitor (Serpin). Its primary mechanism is inhibiting the action of the serine protease called elastase (also plasmin and thrombin) in the lungs. The reactive center loop (RCL) of alpha-1 proteinase inhibitor extends out from the body of the protein and directs binding to the target protease. The protease cleaves the serpin at the reactive site, establishing a covalent linkage between the carboxyl group of the serpin reactive site and the serine hydroxyl of the protease. The resulting inactive serpin-protease complex is highly stable. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | 5632 ± 2006 mL [ARALAST NP] |
| Clearance | 940 ± 275 mL/day [Patients with congenital deficiency with single IV infusion of 60mg/kg] |
| Categories | Serine Proteinase Inhibitors |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Neutrophil elastase |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Aralast |
| Company | Baxter |
| Brand Discription | ARALAST is an Alpha-1 proteinase inhibitor. ARALAST contains approximately 67% Alpha-PI with the C-T-terminal lysine truncation. |
| Prescribed for | Its used to treat lung problems (emphysema) caused by a certain inherited disease (alpha-1-proteinase inhibitor deficiency). In people with this condition, lung damage is caused by elastase, a natural substance that the body needs to kill bacteria in the |
| Chemical Name | N.A. |
| Formulation | ARALAST NP is available as a lyophilized powder in single dose vials containing 0.5 gram or 1 gram of functional Alpha 1 -Protenase inhibitor |
| Physcial Appearnce | Lyophilized powder |
| Route of Administration | Intravenous infusion |
| Recommended Dosage | Recommended dose is 60 mg/kg of body weight, administered once in a week. |
| Contraindication | ARALAST NP is contraindicated in immunoglobulin A deficient patients with antibodies against IgA, due to the risk of severe hypersensitivity. |
| Side Effects | Fever, chills, body aches, flu symptoms, sores in your mouth and throat; pain or burning when you urinate; wheezing, chest pain or tightness, trouble breathing; or vision changes. |
| Useful Link | http://www.baxter.com/downloads/healthcare_professionals/products/Aralast_NP_PI.pdf |
| PubMed ID | 16773239 |
| 3-D Structure | Th1047 (View) or (Download) |