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QuickView for Daptomycin (compound)


PubChem Substance
Name: Daptomycin
PubChem Substance ID: 12013658
Description: A cyclic lipopeptide antibiotic that inhibits GRAM-POSITIVE BACTERIA.
Synonyms:
Cubicin; Dapcin; Daptomycin; LY-146032; Cidecin
DrugBank
Identification
Name: Daptomycin
Name (isomeric): DB00080
Drug Type: biotech
Description: A cyclic lipopeptide antibiotic that inhibits GRAM-POSITIVE BACTERIA.
Synonyms:
LY 146032
Brand: Cubicin
Category: Anti-Bacterial Agents
CAS number: 103060-53-3
Pharmacology
Indication: For the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms.
Pharmacology:
Daptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant Staphylococcus aureus), streptococci and corynebacteria. Daptomycin is derived ...
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Mechanism of Action:
Daptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the ...
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Protein binding: Daptomycin is reversibly bound to human plasma proteins, primarily to serum albumin, in a concentration-independent manner. The overall mean binding ranged from 90 to 93%.
Biotransformation: Minor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified.
Route of elimination: Daptomycin is excreted primarily by the kidney. In a mass balance study of 5 healthy subjects using radiolabeled daptomycin, approximately 78% of the administered dose was recovered from urine based on total radioactivity (approximately 52% of the dose based on microbiologically active concentrations) and 5.7% of the dose was recovered from feces (collected for up to 9 days) based on total radioactivity. Because renal excretion is the primary route of elimination, dosage adjustment is necessary in patients with severe renal insufficiency (CLCR <30 mL/min)
Half Life: 7 days
Affected organisms: Enteric bacteria and other eubacteria

Targets