Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C31H52N2O5S |
Molecular Weight | 564.82 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12C(=O)CC[C@]13CC[C@@H](C)[C@@]2(C)[C@@H](C[C@@](C)(C=C)[C@@H](O)[C@@H]3C)OC(=O)CSC(C)(C)CNC(=O)[C@H](N)C(C)C
InChI
InChIKey=LLYYNOVSVPBRGV-MVNKZKPCSA-N
InChI=1S/C31H52N2O5S/c1-10-29(8)15-22(38-23(35)16-39-28(6,7)17-33-27(37)24(32)18(2)3)30(9)19(4)11-13-31(20(5)26(29)36)14-12-21(34)25(30)31/h10,18-20,22,24-26,36H,1,11-17,32H2,2-9H3,(H,33,37)/t19-,20+,22-,24-,25+,26+,29-,30+,31+/m1/s1
Valnemulin (marketed under the trade name Econor) is a pleuromutilin antibiotic used to treat swine dysentery, ileitis, colitis and pneumonia. It is approved for veterinary use only. Valnemulin is an antibiotic belonging to the pleuromutilin group, which acts by the inhibition of the initiation of protein synthesis at the level of the bacterial ribosome. Valnemulin has activity against a range of bacteria including those responsible for enteric and respiratory disease in pigs. Valnemulin shows high activity against Mycoplasma spp. and spirochaetes such as Brachyspira hyodysenteriae and Brachyspira pilosicoli. Valnemulin has little activity against Enterobacteriaceae, such as Salmonella spp. and Escherichia coli. There appears to be no resistance development to valnemulin to date by M. hyopneumoniae and L. intracellularis. There have been some increases of MICs of valnemulin against B. hyodysenteriae and to a lesser degree B. pilosicoli, some of which appear to have developed resistance. Valnemulin binds to the ribosome and inhibits bacterial protein synthesis. Resistance development primarily occurs because of changes at the binding site associated with mutations of the ribosomal DNA genes. Econor 10% and 50% is indicated for: The treatment and prevention of swine dysentery. The treatment of clinical signs of porcine proliferative enteropathy (ileitis). The prevention of clinical signs of porcine colonic spirochaetosis (colitis) when the disease has been diagnosed in the herd. Treatment and prevention of swine enzootic pneumonia. At the recommended dosage of 10 - 12 mg/kg bodyweight lung lesions and weight loss are reduced, but infection with Mycoplasma hyopneumoniae is not eliminated. Econor 0.5% and 1% is indicated: For the treatment and prevention of swine dysentery. The treatment of clinical signs of porcine proliferative enteropathy (ileitis). The prevention of clinical signs of porcine colonic spirochaetosis (colitis) when the disease has been diagnosed in the herd.
Originator
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/veterinary/000042/WC500064379.pdf
Curator's Comment: # Novartis
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Curative | Econor Approved UseEconor 10% and 50%: The treatment and prevention of swine dysentery. The treatment of clinical signs of porcine proliferative enteropathy (ileitis). The prevention of clinical signs of porcine colonic spirochaetosis (colitis) when the disease has been diagnosed in the herd. Treatment and prevention of swine enzootic pneumonia. At the recommended dosage of 10 - 12 mg/kg bodyweight lung lesions and weight loss are reduced, but infection with Mycoplasma hyopneumoniae is not eliminated. Econor 0.5% and 1%: For the treatment and prevention of swine dysentery. The treatment of clinical signs of porcine proliferative enteropathy (ileitis). The prevention of clinical signs of porcine colonic spirochaetosis (colitis) when the disease has been diagnosed in the herd. Launch Date1999 |
PubMed
Title | Date | PubMed |
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The pleuromutilin drugs tiamulin and valnemulin bind to the RNA at the peptidyl transferase centre on the ribosome. | 2001 Sep |
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Efficacy and tolerability of early administration of valnemulin hydrochloride premix on epizootic rabbit enteropathy. | 2015 Jun |
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A novel method to determine valnemulin in feedingstuffs for several animal species by liquid chromatography-electrospray tandem mass spectrometry. | 2016 Nov |
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Determination of the Mutant Selection Window and Evaluation of the Killing of Mycoplasma gallisepticum by Danofloxacin, Doxycycline, Tilmicosin, Tylvalosin and Valnemulin. | 2017 |
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Pharmacokinetics of valnemulin after intravenous, intramuscular, and oral administration in layer chickens. | 2017 Aug |
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Antimicrobial susceptibility monitoring of Mycoplasma hyopneumoniae and Mycoplasma bovis isolated in Europe. | 2017 May |
Sample Use Guides
Pigs:Treatment and prevention of swine enzootic pneumonia. At the recommended dosage of 10–12 mg/kg bodyweight lung lesions and weight loss are reduced, but infection with Mycoplasma hyopneumoniae is not eliminated.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28532800
MIC50/MIC90 values for valnemulin against M. hyopneumoniae were ≤0.001/ ≤0.001mg/L respectively.
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EMA VETERINARY ASSESSMENT REPORTS |
ECONOR (AUTHORISED)
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Valnemulin
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C117845
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m11367
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9850878
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)