Identification

Name
Lancovutide
Accession Number
DB05029
Type
Small Molecule
Groups
Investigational
Description

Lancovutide, a peptide antibiotic, is in clinical development for the treatment of cystic fibrosis. Duramycin is a 19-amino-acid tetracyclic peptide produced by Streptoverticillium cinnamoneus and is closely related to cinnamycin (Ro09-0198). It belongs to the lantibiotics. Lantibiotics are bacteriocins that are characterized by the presence of a high proportion of unusual amino acids.

Synonyms
  • Duramycin
External IDs
MOLI-1901 / MOLI1901
Categories
UNII
BPR0F3X56H
CAS number
1391-36-2
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in cystic fibrosis and eye disorders/infections.

Pharmacodynamics
Not Available
Mechanism of action

Duramycin becomes deposited in cellular membranes where it binds to phosphatidylethanolamine. It may thereby change biophysical membrane properties and perturb ion channel function. Duramycin stimulates secretion of electrically charged atoms (ions) of chloride from epithelial cells in the lungs. Increased chloride secretion is accompanied by obligatory increase in water secretion from same cells. This may prevent the thickening of lung secretions and prevent further mucus build up and its progressive contribution to lung tissue damage.

Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347909900

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentCystic Fibrosis (CF)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phospholipase a2 activity
Specific Function
Selectively hydrolyzes arachidonyl phospholipids in the sn-2 position releasing arachidonic acid. Together with its lysophospholipid activity, it is implicated in the initiation of the inflammatory...
Gene Name
PLA2G4A
Uniprot ID
P47712
Uniprot Name
Cytosolic phospholipase A2
Molecular Weight
85238.2 Da
References
  1. Tanaka K, Itazaki H, Yoshida T: Cinatrins, a novel family of phospholipase A2 inhibitors. II. Biological activities. J Antibiot (Tokyo). 1992 Jan;45(1):50-5. [PubMed:1548189]
  2. Marki F, Hanni E, Fredenhagen A, van Oostrum J: Mode of action of the lanthionine-containing peptide antibiotics duramycin, duramycin B and C, and cinnamycin as indirect inhibitors of phospholipase A2. Biochem Pharmacol. 1991 Oct 24;42(10):2027-35. [PubMed:1741778]
  3. Hechard Y, Sahl HG: Mode of action of modified and unmodified bacteriocins from Gram-positive bacteria. Biochimie. 2002 May-Jun;84(5-6):545-57. [PubMed:12423799]

Drug created on October 21, 2007 16:23 / Updated on November 02, 2018 06:08