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1641 details
Primary information
ThPP IDTh1146
Therapeutic Peptide/Protein NameLucinactant
SequenceKLLLLKLLLLKLLLLKLLLLK view full sequnce in fasta
Functional ClassificationIb
Molecular Weight2470.2
Chemical FormulaC126H238N26O22
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeN.A.
DescriptionA 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/DiseaseIntended for the prevention of respiratory distress syndrome (RDS) in premature infants at high risk for RDS.
PharmacodynamicsLucinactant 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 ActionPulmonary 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).
ToxicityMost common adverse reactions associated with the use of lucinactant are endotracheal tube reflux, pallor, endotracheal tube obstruction, and need for dose interruption.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesPulmonary surfactants
Patents NumberUS5407914
Date of Issue03/06/12
Date of Expiry11/07/13
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameSurfaxin
CompanyDiscovery Laboratories, Inc.
Brand DiscriptionIt 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 forTo 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 NameN.A.
FormulationIntratracheal 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 AppearnceSuspension
Route of AdministrationIntratracheal administration
Recommended DosageThe 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.
ContraindicationNone
Side EffectsAdministration-related oxygen desaturation and bradycardia
Useful Linkhttp://www.drugbank.ca/drugs/DB04897
PubMed ID17533176, 16740886, 16452346, 15833063, 15813666, 15805381, 12802703
3-D StructureTh1146 (View) or (Download)