| Primary information |
|---|
| ThPP ID | Th1146 |
| Therapeutic Peptide/Protein Name | Lucinactant |
| Sequence | KLLLLKLLLLKLLLLKLLLLK view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 2470.2 |
| Chemical Formula | C126H238N26O22 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | A new synthetic peptide containing surfactant for intratracheal use. It contains sinapultide, a novel, hydrophobic, 21-amino acid peptide (leucine and lysine repeating units, KL4 peptide) designed to mimic human surfactant protein-B (SB-P). It specifically mimics the C-terminal amphipathic helical domain of this protein. It also consists of phospholipids (dipalmitoylphosphatidylcholine, DPPC and palmitoyloleoyl phosphatidylglycerol,POPG) and a fatty acid (palmitic acid). It is completely devoid of animal-derived components. FDA approved it on March 6, 2012. |
| Indication/Disease | Intended for the prevention of respiratory distress syndrome (RDS) in premature infants at high risk for RDS. |
| Pharmacodynamics | Lucinactant is a new synthetic surfactant containing a protein that mimics human surfactant protein-B, is effective at preventing respiratory distress syndrome (RDS) and related complications in preterm infants. Lucinactant has been shown to have antiinflammatory properties, is resistant to proteolytic degradation and oxidation, and has no potential for transmitting animal-derived diseases. Lucinactant has proven safe and effective in the prevention of RDS in preterm infants and as a treatment for MAS in full-term infants and for adult ARDS. |
| Mechanism of Action | Pulmonary surfactant is a lipoprotein complex that is produced naturally in the lungs, where it lines the alveolar epithelium and serves to reduce surface tension, which facilitates alveoli expansion and allows gas exchange. Human surfactants contain phospholipids, predominantly dipalmitoylphosphatidylcholine (DPPC), in addition to surfactant proteins A, B, C and D. Surfactant is also a physical barrier to inhaled particle and noxious agents, enhances particle clearance, is involved in host defense against infection and possesses antiinflammatory properties. Several serious respiratory disorders have been associated with a loss or lack of endogenous surfactant. Lucinactant was designed to mimic the essential endogenous human surfactant protein B (SP-B). |
| Toxicity | Most common adverse reactions associated with the use of lucinactant are endotracheal tube reflux, pallor, endotracheal tube obstruction, and need for dose interruption. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Pulmonary surfactants |
| Patents Number | US5407914 |
| Date of Issue | 03/06/12 |
| Date of Expiry | 11/07/13 |
| Drug Interaction | N.A. |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Surfaxin |
| Company | Discovery Laboratories, Inc. |
| Brand Discription | It is a sterile, non-pyrogenic pulmonary surfactant intended for intratracheal use only. It is a synthetic formulation consisting of phospholipids, a fatty acid, and sinapultide (KL4peptide), a 21-amino acid hydrophobic synthetic peptide. Surfaxin is a white to off-white opaque gel-like suspension at 2° to 8°C (36° to 46°F), which becomes a free-flowing suspension upon warming for 15 minutes in a dry block heater set at 44°C (111°F). Each mL of Surfaxin provides 30 mg phospholipids (22.50 mg DPPC and 7.50 mg POPG, Na), 4.05 mg PA, and 0.862 mg sinapultide in tromethamine and sodium chloride. Glacial acetic acid is used to adjust the pH of the buffer to 7.4 (range 7.0 to 8.0). Surfaxin contains no preservatives. |
| Prescribed for | To prevent respiratory distress syndrome (RDS) in premature infants at high risk for RDS. It reduces the incidence of RDS at 24 hours and mortality due to RDS. |
| Chemical Name | N.A. |
| Formulation | Intratracheal Suspension: 8.5 mL suspension in a glass vial. Each mL contains 30 mg phospholipids [22.50 mg dipalmitoylphosphatidylcholine (DPPC) and 7.50 mg palmitoyloleoyl-phosphatidylglycerol, sodium salt (POPG, Na)], 4.05 mg palmitic acid (PA), and 0.862 mg sinapultide. |
| Physcial Appearnce | Suspension |
| Route of Administration | Intratracheal administration |
| Recommended Dosage | The recommended dose of surfaxin is 5.8 mL per kg birth weight. Up to 4 doses of surfaxin can be administered in the first 48 hours of life. Doses should be given no more frequently than every 6 hours. |
| Contraindication | None |
| Side Effects | Administration-related oxygen desaturation and bradycardia |
| Useful Link | http://www.drugbank.ca/drugs/DB04897 |
| PubMed ID | 17533176, 16740886, 16452346, 15833063, 15813666, 15805381, 12802703 |
| 3-D Structure | Th1146 (View) or (Download) |