1061337-51-6|Lefamulin|(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-(((1R,2R,4R)-4-amino-2-hydroxycyclohexyl)thio)acetate|-范德生物科技公司

Lefamulin

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names：
(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-(((1R,2R,4R)-4-amino-2-hydroxycyclohexyl)thio)acetate
CAS号：
1061337-51-6
MDL Number：
MF(分子式)： C28H45NO5S MW(分子量)： 507.73
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Lefamulin
英文别名	BC-3781; BC 3781; BC3781; Lefamulin; Xenleta
CAS号	1061337-51-6
Inchi	InChI=1S/C28H45NO5S/c1-6-26(4)14-22(34-23(32)15-35-21-8-7-18(29)13-20(21)31)27(5)16(2)9-11-28(17(3)25(26)33)12-10-19(30)24(27)28/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H3/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27+,28+/m1/s1
InchiKey	KPVIXBKIJXZQJX-FCEONZPQSA-N
分子式 Formula	C28H45NO5S
分子量 Molecular Weight	507.73
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Lefamulin(CAS:1061337-51-6 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	Lefamulin, also known as BC-3781, is a semi-synthetic compound that inhibits the synthesis of bacterial protein, which is required for bacteria to grow. Lefamulin acts by binding to the peptidyl transferase center, or PTC, on the bacterial ribosome in such a way that it interferes with the interaction of protein production at two key sites known as the “A” site and the “P” site, resulting in the inhibition of bacterial proteins and the cessation of bacterial growth. Lefamulin’s binding occurs with high affinity, high specificity and at molecular sites that are different than other antibiotic classes. Lefamulin exhibited MIC50 and MIC90 values of 0.12 and 0.25 μg/ml, respectively, against the entire collection (n = 822). Similar results were obtained for lefamulin against each of the most common serotypes as well as against multidrug-resistant isolates and strains that are nonsusceptible to ceftriaxone or erythromycin. Lefamulin may be useful for the treatment of community-acquired respiratory tract infections.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Tang HJ, Lai CC. Lefamulin for treating community-acquired bacterial pneumonia in adult patients aged < 65 years. Clin Infect Dis. 2019 Dec 1[1]pii: ciz1173. doi: 10.1093/cid/ciz1173. [Epub ahead of print] PubMed PMID: 31822903.

[2]Lee YR, Jacobs KL. Leave it to Lefamulin: A Pleuromutilin Treatment Option in Community-Acquired Bacterial Pneumonia. Drugs. 2019 Nov;79(17):1867-1876. doi: 10.1007/s40265-019-01219-5. Review. PubMed PMID: 31705486.

[3] Lefamulin (Xenleta) for Community-Acquired Bacterial Pneumonia. JAMA. 2019 Nov 5;322(17):1709-1710. doi: 10.1001/jama.2019.16482. PubMed PMID: 31688883.

[4] File TM, Goldberg L, Das A, Sweeney C, Saviski J, Gelone SP, Seltzer E, Paukner S, Wicha WW, Talbot GH, Gasink LB. Efficacy and Safety of Intravenous-to-oral Lefamulin, a Pleuromutilin Antibiotic, for the Treatment of Community-acquired Bacterial Pneumonia: The Phase III Lefamulin Evaluation Against Pneumonia (LEAP 1) Trial. Clin Infect Dis. 2019 Oct 18. pii: ciz710. doi: 10.1093/cid/ciz710. [Epub ahead of print] PubMed PMID: 31626688.

[5] Lefamulin (Xenleta) for community-acquired bacterial pneumonia. Med Lett Drugs Ther. 2019 Sep 23;61(1581):145-148. Review. PubMed PMID: 31599865.

6: Alexander E, Goldberg L, Das AF, Moran GJ, Sandrock C, Gasink LB, Spera P, Sweeney C, Paukner S, Wicha WW, Gelone SP, Schranz J. Oral Lefamulin vs Moxifloxacin for Early Clinical Response Among Adults With Community-Acquired Bacterial Pneumonia: The LEAP 2 Randomized Clinical Trial. JAMA. 2019 Sep 27. doi: 10.1001/jama.2019.15468. [Epub ahead of print] PubMed PMID: 31560372.7: Malani PN. Lefamulin-A New Antibiotic for Community-Acquired Pneumonia. JAMA. 2019 Sep 27. doi: 10.1001/jama.2019.16215. [Epub ahead of print] PubMed PMID: 31560367.8: Koulenti D, Xu E, Yin Sum Mok I, Song A, Karageorgopoulos DE, Armaganidis A, Lipman J, Tsiodras S. Lefamulin. Comment on: "Novel Antibiotics for Multidrug-Resistant Gram-Positive Microorganisms. Microorganisms, 2019, 7, 270". Microorganisms. 2019 Sep 24;7(10). pii: E386. doi: 10.3390/microorganisms7100386. PubMed PMID: 31554342; PubMed Central PMCID: PMC6843636.9: Perry W, Golan Y. Therapeutic potential of lefamulin in the treatment of community-acquired pneumonia. Future Microbiol. 2019 Jul;1

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