LEFAMULIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H45NO5S
Molecular Weight	507.7278
Optical Activity	UNSPECIFIED
Defined Stereocenters	10 / 11
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C=C[C@]1(C)C[C@]([H])([C@]2(C)C([H])(C)CC[C@]3(CCC(=O)[C@@]23[H])[C@@]([H])(C)[C@]1([H])O)OC(=O)CS[C@]4([H])CC[C@]([H])(C[C@@]4([H])O)N

InChI

InChIKey=KPVIXBKIJXZQJX-CSOZIWFHSA-N

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-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/mesh/2002015 | https://www.nabriva.com/pipeline-research | https://www.ncbi.nlm.nih.gov/pubmed/30513017

LEFAMULIN is a pleuromutilin antibiotic under development for the treatment of community-acquired bacterial pneumonia, as well as acute bacterial skin and skin structure infections. It inhibits bacterial protein synthesis by binding to the peptidyl transferase center of the 50S ribosome, resulting in the cessation of bacterial growth.

Originator

Approval Year

C_max

Value	Dose	Analyte	Population
3.5 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3.6 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg 2 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.24 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
2.24 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
27 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
28.6 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg 2 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
30.7 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
32.7 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	150 mg 2 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	LEFAMULIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

Doses

Dose	Population	Adverse events
200 mg 2 times / day multiple, intravenous Highest studied dose Dose: 200 mg, 2 times / day Route: intravenous Route: multiple Dose: 200 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	healthy, adults Health Status: healthy Age Group: adults Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf
400 mg single, intravenous Highest studied dose Dose: 400 mg Route: intravenous Route: single Dose: 400 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	healthy, adults Health Status: healthy Age Group: adults Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf
600 mg 2 times / day multiple, oral Highest studied dose Dose: 600 mg, 2 times / day Route: oral Route: multiple Dose: 600 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	healthy, adults Health Status: healthy Age Group: adults Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf
750 mg single, oral Highest studied dose Dose: 750 mg Route: oral Route: single Dose: 750 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	healthy, adults Health Status: healthy Age Group: adults Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf
600 mg 2 times / day multiple, oral Recommended Dose: 600 mg, 2 times / day Route: oral Route: multiple Dose: 600 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	unhealthy, adults n = 368 Health Status: unhealthy Condition: community-acquired bacterial pneumonia (CABP) Age Group: adults Sex: M+F Population Size: 368 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	Other AEs: Diarrhea, Nausea... Other AEs: Diarrhea (12%) Nausea (5%) Vomiting (3%) Alanine aminotransferase increased (2%) Aspartate aminotransferase increased (2%) Liver function test increased (2%) Anemia (<2%) Thrombocytopenia (<2%) Atrial fibrillation (<2%) Palpitations (<2%) Abdominal pain (<2%) Constipation (<2%) Dyspepsia (<2%) Epigastric discomfort (<2%) Gastritis erosive (<2%) Clostridium difficile colitis (<2%) Oropharyngeal candidiasis (<2%) Vulvovaginal candidiasis (<2%) Somnolence (<2%) Urinary retention (<2%) Anxiety (<2%) Diarrhea (12%) Nausea (5%) Vomiting (3%) Alanine aminotransferase increased (2%) Aspartate aminotransferase increased (2%) Liver function test increased (2%) Anemia (<2%) Thrombocytopenia (<2%) Atrial fibrillation (<2%) Palpitations (<2%) Abdominal pain (<2%) Constipation (<2%) Dyspepsia (<2%) Epigastric discomfort (<2%) Gastritis erosive (<2%) Clostridium difficile colitis (<2%) Oropharyngeal candidiasis (<2%) Vulvovaginal candidiasis (<2%) Somnolence (<2%) Urinary retention (<2%) Anxiety (<2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf
150 \| 600 mg\|mg 2 \| 2 times / day\|day multiple\|multiple, intravenous\|oral (complex) Recommended Dose: 150 \| 600 mg\|mg, 2 \| 2 times / day\|day Route: intravenous\|oral Route: multiple\|multiple Dose: 150 \| 600 mg\|mg, 2 \| 2 times / day\|day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	unhealthy, adults n = 273 Health Status: unhealthy Condition: community-acquired bacterial pneumonia (CABP) Age Group: adults Sex: M+F Population Size: 273 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf	Other AEs: Infusion site pain, Infusion site phlebitis... Other AEs: Infusion site pain (7%) Infusion site phlebitis (7%) Injection site reaction (7%) Alanine aminotransferase increased (3%) Aspartate aminotransferase increased (3%) Liver function test increased (3%) Nausea (3%) Hypokalemia (3%) Insomnia (3%) Headache (2%) Anemia (<2%) Thrombocytopenia (<2%) Atrial fibrillation (<2%) Palpitations (<2%) Abdominal pain (<2%) Constipation (<2%) Dyspepsia (<2%) Epigastric discomfort (<2%) Gastritis erosive (<2%) Clostridium difficile colitis (<2%) Oropharyngeal candidiasis (<2%) Vulvovaginal candidiasis (<2%) Somnolence (<2%) Urinary retention (<2%) Anxiety (<2%) Infusion site pain (7%) Infusion site phlebitis (7%) Injection site reaction (7%) Alanine aminotransferase increased (3%) Aspartate aminotransferase increased (3%) Liver function test increased (3%) Nausea (3%) Hypokalemia (3%) Insomnia (3%) Headache (2%) Anemia (<2%) Thrombocytopenia (<2%) Atrial fibrillation (<2%) Palpitations (<2%) Abdominal pain (<2%) Constipation (<2%) Dyspepsia (<2%) Epigastric discomfort (<2%) Gastritis erosive (<2%) Clostridium difficile colitis (<2%) Oropharyngeal candidiasis (<2%) Vulvovaginal candidiasis (<2%) Somnolence (<2%) Urinary retention (<2%) Anxiety (<2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211672s000,211673s000lbl.pdf
150 \| 600 mg\|mg 2 \| 2 times / day\|day multiple\|multiple, intravenous\|oral (complex) Recommended Dose: 150 \| 600 mg\|mg, 2 \| 2 times / day\|day Route: intravenous\|oral Route: multiple\|multiple Dose: 150 \| 600 mg\|mg, 2 \| 2 times / day\|day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	unhealthy, adults n = 273 Health Status: unhealthy Condition: community-acquired bacterial pneumonia (CABP) Age Group: adults Sex: M+F Population Size: 273 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf	Disc. AE: Infectious pleural effusion, Lung abscess... Other AEs: Infectious pleural effusion, Lung abscess... AEs leading to discontinuation/dose reduction: Infectious pleural effusion (1 patient) Lung abscess (1 patient) Pneumonia (1 patient) Pulmonary tuberculosis (1 patient) Acute respiratory distress syndrome (1 patient) Acute respiratory failure (1 patient) Chronic obstructive pulmonary disease (1 patient) Pulmonary edema (1 patient) Vomiting (2 patients) Abdominal pain upper (1 patient) Infusion site phlebitis (1 patient) Injection site reaction (1 patient) Hepatitis toxic (1 patient) Other AEs: Infectious pleural effusion (1 patient) Lung abscess (1 patient) Pneumonia (1 patient) Pulmonary tuberculosis (1 patient) Acute respiratory distress syndrome (1 patient) Acute respiratory failure (1 patient) Chronic obstructive pulmonary disease (1 patient) Pulmonary edema (1 patient) Vomiting (2 patients) Abdominal pain upper (1 patient) Infusion site phlebitis (1 patient) Injection site reaction (1 patient) Hepatitis toxic (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1601	inhibitor 1604 substrate 936 inducer 355	inhibitor 1702 substrate 1118 inducer 97	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 480 CYP1A2 1383 CYP2B6 717 CYP2C8 818 CYP2C19 1325 CYP3A4/5 241 BCRP 643 P-gp 1330 BSEP 376 OAT1 554 OAT3 588 OCT2 594 MATE1 290 MATE2 251 OATP1B1 733 OATP1B3 657	OCT1 302 P-gp 1400 CYP3A5 367 CYP2B6 616 CYP2C8 634 CYP2C19 910	CYP2B6 501 CYP2C8 159 CYP2C19 269

Drug as perpetrator

Target	Modality	Activity
BSEP 377	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 24.5 uM]
CYP2C8 865	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 41 uM]
OAT1 558	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
OAT3 590	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
OCT2 595	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
CYP1A2 1532	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2B6 884	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2C19 1392	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2C9 1648	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2D6 1738	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2B6 884	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C19 1392	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C8 865	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C9 1648	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2D6 1738	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
OATP1B1 748	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	weak [IC50 122 uM]
OATP1B3 666	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	weak [IC50 122 uM]
P-gp 1514	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 50;126;270	weak [IC50 13.76 uM]
MATE1 292	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [IC50 0.297 uM]
BCRP 713	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 127;228	yes [IC50 42.2 uM]
MATE2 251	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [IC50 76.4 uM]
CYP3A4/5 293	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [Ki 0.86 uM]
OCT1 495	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;228;270	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2B6 616	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C19 910	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C8 634	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C9 936	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2D6 1118	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP3A5 367	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 270.0	no
OCT1 302	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 125;228	yes
P-gp 1400	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=126 Page: 125;269;270	yes
CYP3A4 1601	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=126 Page: 126;269;270	yes	yes (co-administration study) Comment: increased the arithmetic mean Cmax and AUC0-inf of LEF by 58% and 165%, respectively, when administered with ketoconazole (strong inhibitor); reduced the arithmetic mean Cmax and AUC0-inf of LEF by 57% and 72%, respectively, when administered with rifampin (strong inducer) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=126 Page: 126;269;270

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1507	inhibitor 1489 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=45 Page: 45.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY34218	https://www.001chemical.com/chem/1061337-51-6
BioChemPartner	BCP24164	http://www.biochempartner.com/1061337-51-6-BCP24164
DC Chemicals	DC8172	http://www.dcchemicals.com/product_show-Lefamulin_BC_3781_.html
Excenen	EX-A3600	https://www.excenen.com/searchresultlist.php?id=EX-A3600
Lab Network	LN01343920	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343920
Molcore	MC34218	https://www.molcore.com/product/1061337-51-6
MuseChem	I007398	https://www.musechem.com/product/I007398.html
Smolecule	S532713	http://www.smolecule.com/products/s532713
THE BioTek	bt-272945	https://www.thebiotek.com/product/inhibitors/bt-272945
THE BioTek	bt-468058	https://www.thebiotek.com/product/others/bt-468058
eNovation Chemicals	D666959	https://www.enovationchem.com/ProductDetails.asp?ProductID=D666959

PubMed

Title	Date	PubMed
Simultaneous assessment of the pharmacokinetics of a pleuromutilin, lefamulin, in plasma, soft tissues and pulmonary epithelial lining fluid.	2016 Apr	26747098
In Vitro Activity of Lefamulin Tested against Streptococcus pneumoniae with Defined Serotypes, Including Multidrug-Resistant Isolates Causing Lower Respiratory Tract Infections in the United States.	2016 Jul	27161634
Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic.	2018 Sep	30019769
Lefamulin: a promising new pleuromutilin antibiotic in the pipeline.	2019 Jan	30513017

Sample Use Guides

In Vitro Use Guide

Lefamulin was evaluated against various Streptococcus pneumoniae serotypes that were collected from adults with lower respiratory tract infections. 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.

Name

Type

Language

LEFAMULIN

Official Name

English

LEFAMULIN [USAN]

Common Name

English

ACETIC ACID, 2-(((1R,2R,4R)-4-AMINO-2-HYDROXYCYCLOHEXYL)THIO)-, (3AS,4R,5S,6S,8R,9R,9AR,10R)-6-ETHENYLDECAHYDRO-5-HYDROXY-4,6,9,10-TETRAMETHYL-1-OXO-3A,9-PROPANO-3AH-CYCLOPENTACYCLOOCTEN-8-YL ESTER

Systematic Name

English

LEFAMULIN [WHO-DD]

Common Name

English

(+)-LEFAMULIN

Common Name

English

BC-3781

Code

English

LEFAMULIN [INN]

Common Name

English

Code System Code Type Description

RXCUI

2198944