Identification Name Dalfopristin Accession Number DB01764 (EXPT01246) Type Small Molecule Groups Approved Description
Dalfopristin is a combination of two antibiotics (Dalfopristin and quinupristin) used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium. It is not effective against Enterococcus faecalis infections. Dalfopristin inhibits the early phase of protein synthesis in the bacterial ribosome and quinupristin inhibits the late phase of protein synthesis.
Dalfopristina Dalfopristine Dalfopristinum External IDs RP 54476 / RP-54476 Product Ingredients Approved Prescription Products Not Available Approved Generic Prescription Products Not Available Approved Over the Counter Products Not Available Unapproved/Other Products Not Available International Brands Not Available Brand mixtures
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Synercid Dalfopristin Quinupristin Powder, for solution Intravenous Monarch Pharmaceuticals, Inc. 2000-07-05 2008-05-28 Canada Categories UNII R9M4FJE48E CAS number 112362-50-2 Weight Average: 690.847 Monoisotopic: 690.329849908 Chemical Formula C 34H 50N 4O 9S InChI Key SUYRLXYYZQTJHF-VMBLUXKRSA-N InChI
SMILES Pharmacology Indication
For the treatment of bacterial infections (usually in combination with quinupristin).
Structured Indications Pharmacodynamics
Dalfopristin is a streptogramin antibiotic, derived from pristinamycin IIA.
Mechanism of action
The site of action of dalfopristin is the bacterial ribosome. Dalfopristin
has been shown to inhibit the early phase of protein synthesis.
Target Kind Pharmacological action Actions Organism UniProt ID Streptogramin A acetyltransferase Protein yes
Enterococcus faecium P50870 details Related Articles Absorption Not Available Volume of distribution Not Available Protein binding
Converted to an active non-conjugated metabolite by hydrolysis.
Route of elimination Not Available Half life
The elimination half-life is approximately 0.70 hours.
Clearance Not Available Toxicity Not Available Affected organisms Enteric bacteria and other eubacteria
Enterococcus faecalis Pathways Not Available Pharmacogenomic Effects/ADRs Not Available Interactions Drug Interactions
Drug Interaction Drug group Aripiprazole The serum concentration of Aripiprazole can be increased when it is combined with Dalfopristin. Approved, Investigational BCG vaccine The therapeutic efficacy of Bcg can be decreased when used in combination with Dalfopristin. Investigational Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Dalfopristin. Approved Flibanserin The serum concentration of Flibanserin can be increased when it is combined with Dalfopristin. Approved Hydrocodone The serum concentration of Hydrocodone can be increased when it is combined with Dalfopristin. Approved, Illicit Lomitapide The serum concentration of Lomitapide can be increased when it is combined with Dalfopristin. Approved Nimodipine The serum concentration of Nimodipine can be increased when it is combined with Dalfopristin. Approved Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Dalfopristin. Approved Pimozide The serum concentration of Pimozide can be increased when it is combined with Dalfopristin. Approved Food Interactions Not Available References Synthesis Reference Not Available General References Allington DR, Rivey MP: Quinupristin/dalfopristin: a therapeutic review. Clin Ther. 2001 Jan;23(1):24-44. [ PubMed:11219478 ] Lamb HM, Figgitt DP, Faulds D: Quinupristin/dalfopristin: a review of its use in the management of serious gram-positive infections. Drugs. 1999 Dec;58(6):1061-97. [ PubMed:10651391 ] Manzella JP: Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections. Am Fam Physician. 2001 Dec 1;64(11):1863-6. [ PubMed:11764864 ] Paradisi F, Corti G, Messeri D: Antistaphylococcal (MSSA, MRSA, MSSE, MRSE) antibiotics. Med Clin North Am. 2001 Jan;85(1):1-17. [ PubMed:11190346 ] External Links ATC Codes Not Available AHFS Codes Not Available PDB Entries FDA label Download (67.1 KB) MSDS Not Available Clinical Trials Clinical Trials Pharmacoeconomics Manufacturers Not Available Packagers Not Available Dosage forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous Powder, for solution Intravenous Prices Not Available Patents Not Available Properties State Solid Experimental Properties Not Available Predicted Properties Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.6544 Blood Brain Barrier - 0.9286 Caco-2 permeable - 0.6574 P-glycoprotein substrate Substrate 0.7988 P-glycoprotein inhibitor I Non-inhibitor 0.6395 P-glycoprotein inhibitor II Non-inhibitor 0.9399 Renal organic cation transporter Non-inhibitor 0.9011 CYP450 2C9 substrate Non-substrate 0.7897 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.5 CYP450 1A2 substrate Non-inhibitor 0.8118 CYP450 2C9 inhibitor Non-inhibitor 0.7261 CYP450 2D6 inhibitor Non-inhibitor 0.8606 CYP450 2C19 inhibitor Non-inhibitor 0.6834 CYP450 3A4 inhibitor Non-inhibitor 0.7363 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9392 Ames test Non AMES toxic 0.6184 Carcinogenicity Non-carcinogens 0.6071 Biodegradation Not ready biodegradable 0.6975 Rat acute toxicity 2.6096 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9396 hERG inhibition (predictor II) Non-inhibitor 0.7254
ADMET data is predicted using
, a free tool for evaluating chemical ADMET properties. (
Spectra Mass Spec (NIST) Not Available Spectra Taxonomy Description This compound belongs to the class of organic compounds known as macrolide lactams. These are cyclic polyketides containing both a cyclic amide and a cyclic ester group. Kingdom Organic compounds Super Class Phenylpropanoids and polyketides Class Macrolide lactams Sub Class Not Available Direct Parent Macrolide lactams Alternative Parents Alpha amino acid esters / Macrolactams / 2-heteroaryl carboxamides / Tertiary carboxylic acid amides / Heteroaromatic compounds / Sulfones / Oxazoles / Pyrrolidines / Lactones / Lactams / Trialkylamines / Carboxylic acid esters / Cyclic ketones / Secondary alcohols / Secondary carboxylic acid amides / Monocarboxylic acids and derivatives / Azacyclic compounds / Oxacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives show 11 more Substituents Macrolide lactam / Alpha-amino acid ester / Macrolactam / Alpha-amino acid or derivatives / 2-heteroaryl carboxamide / Azole / Heteroaromatic compound / Oxazole / Pyrrolidine / Sulfone / Sulfonyl / Tertiary carboxylic acid amide / Amino acid or derivatives / Carboxamide group / Carboxylic acid ester / Ketone / Lactam / Lactone / Secondary alcohol / Secondary carboxylic acid amide / Cyclic ketone / Tertiary amine / Tertiary aliphatic amine / Monocarboxylic acid or derivatives / Carboxylic acid derivative / Organoheterocyclic compound / Azacycle / Oxacycle / Organic oxygen compound / Amine / Organonitrogen compound / Organooxygen compound / Organosulfur compound / Alcohol / Organopnictogen compound / Carbonyl group / Organic oxide / Organic nitrogen compound / Hydrocarbon derivative / Aromatic heteropolycyclic compound show 30 more Molecular Framework Aromatic heteropolycyclic compounds External Descriptors Not Available