1,2-Dipalmitoyl-sn-glycero-3-phosphocholine

734.04

733.562134

232-642-4

319X2NFW0A

DTXSID5046720

C47462

R - Respiratory system

29232000

111

1.97

Solid

234 °C

60.5-61.5ºC at 760 mmHg

H2O: Very poor solubility

−20°C

D23 +6.6° (c = 4.2 in 1:1 chloroform-methanol)

283.19 Ų [M+CH3COO]- [CCS Type: TIMS, Method: single field calibrated]|281.91 Ų [M+H]+ [CCS Type: TIMS, Method: single field calibrated]|289.5 Ų [M+CF3COO]-

NONH for all modes of transport

3

24/25

Stable. Incompatible with strong oxidizing agents.

In clinical trials, there are reports of pulmonary hemorrhage when colfosceril palmitate is administered in infants with a weight of fewer than 700 grams at birth. Another potential risk of the use of colfosceril palmitate is the formation of mucus plugging in the endotracheal tube which can be prevented by performing suction prior to dosing.

Colfosceril palmitate stays and gets metabolized in the pulmunar tissue, thus it is not able to bind to plasma proteins.

Colfosceril palmitate is indicated for the treatment of respiratory distress syndrome (RDS) in premature infants. The official label is referred as a intratracheal suspension for prophylactic treatment of infants of less than 1350 grams of birth weight under risk of developing RDS, or in infants with birth weight greater than 1350 grams with pulmonary immaturity, or as rescue treatment of infants that already developed RDS. The central feature of RDS is a surfactant deficiency due to lung immaturity. This lung condition is more frequently presented due to risk factors like prematurity, delayed lung maturation caused by maternal diabetes or male gender, or surfactant dysfuntion due to perinatal asphyxia, pulmonary infection or delivery without labor.|Treatment of respiratory distress syndrome

Colfosceril palmitate has shown to significantly reduce the risk of pneumothoraces, pulmonary interstitial emphysema and mortality. Unlike naturals surfactants, colfosceril palmitate reduces the risk of bronchopulmonary dysplasia, intraventricular hemorrhage and patent ductus arteriosus. In clinical placebo-controlled trials, there was a significant reduction in the number of deaths attributed to hyaline membrane disease, the incidence of pulmonary air leaks, oxygen requirements and mean airway pressure. Some reports have indicated a lack of therapeutic effect due to the absence of surfactant protein.

The absorption is done directly in the alveolus into the lung tissue. As the lung surfactant is distributed in the bronchi, bronchioles and alveoli, its highest concentration is at the alveolar air-fluid interface where it remains as a monolayer.|After 5 days, most of the administered dose (56%) is distributed throughout the body with renal and fecal excretion being the minor elimination pathway representing the 4 and 2% of the eliminated dose respectively. The major route of elimination is by expelled air which accounts for 28% of the administered dose.|Colfosceril palmitate is distributed uniformly to all lobes of the lung, distal airways and alveolar spaces. It will not enter the systemic circulation in healthy lungs, however when the integrity of the tissue is distrupted colfosceril can reach systemic circulation. Even 5 days after administration, there are traces of colfosceril palmitate retained in the body that represented 72% of the administered dose which by then have entered pathways of lipid metabolism to become tissue associated.|After 5 days of drug administration, the lung and liver would contain 10% of the administered dose and the elimination via renal excretion accounts only for 8% of the administered dose. This proved a very small renal clearance and confirmed that the major elimination route is by expired air.

Colfosceril palmitate is catabolized and reutilized for further synthesis and secretion in lung tissues.

The half-life of colfosceril palmitate is registered to be in the range of 20-36 hours.

Treatment with colfosceril palmitate aims to reinflate a collapsed area of the lung, improve compliance and reduce intrapulmonary shunting. The actions of colfosceril palmitate are perfomed by replacing the defficient or innefective endogenous lung surfactant and thus, reducing the tension and stabilizing the alveoli from collapsing. Colfosceril palmitate will form a very thin film that will cover the surface of the alveolar cells and therefore it will reduce surface tension.

1,2-dipalmitoyl-sn-glycero-3-phosphocholine

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Lipids -> Glycerophospholipids [GP] -> Glycerophosphocholines [GP01] -> Diacylglycerophosphocholines [GP0101]