LEFAMULIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H45NO5S
Molecular Weight	507.726
Optical Activity	UNSPECIFIED
Defined Stereocenters	11 / 11
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

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

Molecular Formula	C28H45NO5S
Molecular Weight	507.726
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	11 / 11
E/Z Centers	0
Optical Activity	UNSPECIFIED

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
3.6 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 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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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
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

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 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 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
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	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

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 Health Status: unhealthy Age Group: adults Sex: M+F 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 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 Health Status: unhealthy Age Group: adults Sex: M+F 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 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 Health Status: unhealthy Age Group: adults Sex: M+F 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 1946	inhibitor 2438 substrate 1193 inducer 440	inhibitor 2507 substrate 1388 inducer 109	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP3A4/5 296 BCRP 910 P-gp 1741 BSEP 550 OAT1 725 OAT3 747 OCT2 779 MATE1 415 MATE2 267 OATP1B1 1079 OATP1B3 961	OCT1 393 P-gp 2052 CYP3A5 446 CYP2B6 776 CYP2C8 810 CYP2C19 1119	CYP2B6 669 CYP2C8 198 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 24.5 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 41 uM]
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 228.0	no [IC50 >122 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no [IC50 >200 uM]
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	weak [IC50 122 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	weak [IC50 122 uM]
P-gp 1932	inhibitor 4027 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 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [IC50 0.297 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 127;228	yes [IC50 42.2 uM]
MATE2 267	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [IC50 76.4 uM]
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 126;270	yes [Ki 0.86 uM]
OCT1 656	inhibitor 4027 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 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=227 Page: 227.0	no
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=270 Page: 270.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=228 Page: 125;228	yes
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000MultidisciplineR.pdf#page=126 Page: 125;269;270	yes
CYP3A4 1946	substrate 4014 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 2263	inhibitor 2237 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
eNovation Chemicals	D666959	https://www.enovationchem.com/ProductDetails.asp?ProductID=D666959
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

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.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:50:35 GMT 2025` Edited by `admin` on `Mon Mar 31 22:50:35 GMT 2025`
Record UNII	21904A5386
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

lefamulin [INN]

Preferred Name

English

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

Common Name

English

BC-3781

Code

English

Lefamulin [WHO-DD]

Common Name

English

LEFAMULIN [MI]

Common Name

English

Code System Code Type Description

RXCUI

2198944