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lipopeptide antibiotic

Daptomycin

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

Daptomycin is a bacterial metabolite isolated from Streptomyces roseosporus. In a liposome leakage test at 30 ug/ml (after 1 hr CaCl2 preincubation), calcein leakage activity was 100.0%. In an organism-based antibacterial assay with 5 mM Ca2+, the minimum inhibitory concentration (MIC) for CHEMBL387675 against Bacillus subtilis 1046 was 5.0 ug.mL-1. Contraindication: a history of hypersensitivity to the active ingredient (daptomycin) precludes use.

Sources for this introduction: [1] [2] [3] [4]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

Daptomycin is a bacterial metabolite isolated from Streptomyces roseosporus.

Sources[3]iuphar-commentsIUPHAR ligand commentaryIt is a bacterial metabolite that was isolated from Streptomyces roseosporus [Reference 51708].
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “It is a bacterial metabolite that was isolated from Streptomyces roseosporus [Reference 51708].”

    IUPHAR ligand commentary · General comments

    iuphar-comments:10904:1bde3ce08e19:1bde3ce08e19

How does it work?

Target, response, and disposition.

Mechanism

A popPK model parameterized from measured concentrations was combined with Monte Carlo simulation to estimate the probability of meeting PK/PD targets (PTA).

Sources[5]pubmedPopulation pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections.Population pharmacokinetic (popPK) modelling and Monte Carlo simulations were performed to predict probabilities of target attainment (PTA).
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Population pharmacokinetic (popPK) modelling and Monte Carlo simulations were performed to predict probabilities of target attainment (PTA).”

    Population pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections. · METHODS

    pubmed:42637177:3c88bf85c9fe:3c88bf85c9fe

Mechanism

In a black lipid bilayer assay, CHEMBL387675 at 5 ug/ml produced a pore conductance of 500.0 pS, consistent with pore-forming activity measured via membrane current variation.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Unchecked (CHEMBL612545) Assay: Pore forming activity across black lipid bilayer membranes assessed as induction of variation in membrane current by measuring pore conductance at 5 ug/ml Assay format: assay format Standard result: Activity = 500.0 pS Document: CHEMBL4038308
Reported result
Activity = 500.0 pS
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Unchecked (CHEMBL612545) Assay: Pore forming activity across black lipid bilayer membranes assessed as induction of variation in membrane current by measuring pore conductance at 5 ug/ml Assay format: assay format Standard result: Activity = 500.0 pS Document: CHEMBL4038308”

    ChEMBL activities for CHEMBL387675 · Activity 18182209

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Mechanism

A retrospective multicountry drug-utilization analysis used IQVIA MIDAS consumption panels (2012–2021) to assess associations between generic market entry and daptomycin consumption.

Sources[4]pubmedImpact of generic market entry on the consumption of last-resort antibiotics in six European countries.We conducted a retrospective multicountry analysis using IQVIA MIDAS data (hospital and retail consumption panels: Austria, France, Germany, Italy, Spain; Hospital consumption only: Belgium) from 2012 to 2021. Substances included daptomycin, linezolid, tigecycline, teicoplanin, and moxifloxacin.
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “We conducted a retrospective multicountry analysis using IQVIA MIDAS data (hospital and retail consumption panels: Austria, France, Germany, Italy, Spain; Hospital consumption only: Belgium) from 2012 to 2021. Substances included daptomycin, linezolid, tigecycline, teicoplanin, and moxifloxacin.”

    Impact of generic market entry on the consumption of last-resort antibiotics in six European countries. · METHODS

    pubmed:42336237:eb9b973f4722:eb9b973f4722

Mechanism

In a liposome leakage test at 30 ug/ml (after 1 hr CaCl2 preincubation), calcein leakage activity was 100.0%.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: ADMET (CHEMBL612558) Assay: Membrane permeabilization activity in DOPC/DOPG large unilamellar liposomes assessed as leakage of calcein at 30 ug/ml preincubated with CaCl2 for 1 hr prior to testing Assay format: microsome format Standard result: Activity = 100.0 % Document: CHEMBL3867421
Reported result
Activity = 100.0 %
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: ADMET (CHEMBL612558) Assay: Membrane permeabilization activity in DOPC/DOPG large unilamellar liposomes assessed as leakage of calcein at 30 ug/ml preincubated with CaCl2 for 1 hr prior to testing Assay format: microsome format Standard result: Activity = 100.0 % Document: CHEMBL3867421”

    ChEMBL activities for CHEMBL387675 · Activity 16794059

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Pharmacokinetics

The dataset for popPK model development comprised 30 concentration measurements from 10 patients.

Sources[5]pubmedPopulation pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections.Ten patients contributed 30 daptomycin concentrations.
Reported result
10 patients; 30 concentrations
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Ten patients contributed 30 daptomycin concentrations.”

    Population pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections. · RESULTS

    pubmed:42637177:3c88bf85c9fe:3c88bf85c9fe

Pharmacokinetics

Model structure selection favored a two-compartment popPK model, and creatinine clearance plus lean body weight were identified as covariates improving fit.

Sources[5]pubmedPopulation pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections.A two-compartment model, with creatinine clearance and lean body weight as covariates best described the data.
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “A two-compartment model, with creatinine clearance and lean body weight as covariates best described the data.”

    Population pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections. · RESULTS

    pubmed:42637177:3c88bf85c9fe:3c88bf85c9fe

Pharmacokinetics

The study collected steady-state total (not explicitly unbound) daptomycin plasma concentrations for popPK modeling and PTA simulation.

Sources[5]pubmedPopulation pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections.Patients with haematological malignancies receiving contemporary daptomycin doses for confirmed VREfm BSIs had total daptomycin steady-state concentrations measured.
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Patients with haematological malignancies receiving contemporary daptomycin doses for confirmed VREfm BSIs had total daptomycin steady-state concentrations measured.”

    Population pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections. · METHODS

    pubmed:42637177:3c88bf85c9fe:3c88bf85c9fe

What has been studied?

What the evidence says.

Study findings

In a 6 to 8 hr growth-reduction assay with multidrug resistant Klebsiella pneumoniae (ATCC 13883), the EC50 was > 100000.0 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Klebsiella pneumoniae subsp. pneumoniae (CHEMBL613207) Assay: Antibacterial activity against multidrug resistant Klebsiella pneumoniae subsp. pneumoniae NCTC 9633 (ATCC 13883) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 > 100000.0 nM Document: CHEMBL3808280
Reported result
EC50 > 100000.0 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Klebsiella pneumoniae subsp. pneumoniae (CHEMBL613207) Assay: Antibacterial activity against multidrug resistant Klebsiella pneumoniae subsp. pneumoniae NCTC 9633 (ATCC 13883) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 > 100000.0 nM Document: CHEMBL3808280”

    ChEMBL activities for CHEMBL387675 · Activity 16606308

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

Using a two fold serial dilution method over 16 to 20 hrs, CHEMBL387675 inhibited growth of methicillin-resistant Staphylococcus aureus ATCC 33591 with MIC = 0.5 ug.mL-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 16 to 20 hrs by two fold serial dilution method Assay format: assay format Standard result: MIC = 0.5 ug.mL-1 Document: CHEMBL3853323
Reported result
MIC = 0.5 ug.mL-1
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 16 to 20 hrs by two fold serial dilution method Assay format: assay format Standard result: MIC = 0.5 ug.mL-1 Document: CHEMBL3853323”

    ChEMBL activities for CHEMBL387675 · Activity 16669141

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In an antibacterial assay, CHEMBL387675 inhibited Streptococcus pneumoniae PBS1399 with MIC = 0.25 ug.mL-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Streptococcus pneumoniae (CHEMBL347) Assay: Antibacterial activity against Streptococcus pneumoniae PBS1399 Assay format: assay format Standard result: MIC = 0.25 ug.mL-1 Document: CHEMBL3868582
Reported result
MIC = 0.25 ug.mL-1
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Streptococcus pneumoniae (CHEMBL347) Assay: Antibacterial activity against Streptococcus pneumoniae PBS1399 Assay format: assay format Standard result: MIC = 0.25 ug.mL-1 Document: CHEMBL3868582”

    ChEMBL activities for CHEMBL387675 · Activity 16801154

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In a microbroth dilution assay, CHEMBL387675 inhibited vancomycin sensitive Staphylococcus aureus JKD6004 with MIC = 0.0005 ug.mL-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against vancomycin sensitive Staphylococcus aureus JKD6004 by microbroth dilution assay Assay format: assay format Standard result: MIC = 0.0005 ug.mL-1 Document: CHEMBL3867421[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against vancomycin sensitive Staphylococcus aureus JKD6004 by microbroth dilution assay Assay format: assay format Standard result: MIC = 0.0005 ug.mL-1 Document: CHEMBL3867421
Reported result
MIC = 0.0005 ug.mL-1
Source records
2
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against vancomycin sensitive Staphylococcus aureus JKD6004 by microbroth dilution assay Assay format: assay format Standard result: MIC = 0.0005 ug.mL-1 Document: CHEMBL3867421”

    ChEMBL activities for CHEMBL387675 · Activity 16794082

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c
  2. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against vancomycin sensitive Staphylococcus aureus JKD6004 by microbroth dilution assay Assay format: assay format Standard result: MIC = 0.0005 ug.mL-1 Document: CHEMBL3867421”

    ChEMBL activities for CHEMBL387675 · Activity 16794082

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In a broth microdilution assay run for 18 hrs, CHEMBL387675 inhibited Staphylococcus aureus SG511 with MIC = 50.0 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against Staphylococcus aureus SG511 after 18 hrs by broth microdilution method Assay format: assay format Standard result: MIC = 50.0 nM Document: CHEMBL4014288
Reported result
MIC = 50.0 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against Staphylococcus aureus SG511 after 18 hrs by broth microdilution method Assay format: assay format Standard result: MIC = 50.0 nM Document: CHEMBL4014288”

    ChEMBL activities for CHEMBL387675 · Activity 18069221

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In a mouse Streptococcus pneumoniae PBS1399 infection model, PD50 was > 100.0 mg kg-1 when given intravenously as a single dose after 2 hrs, with survival measured on day 7.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Streptococcus pneumoniae (CHEMBL347) Assay: Antibacterial activity against Streptococcus pneumoniae PBS1399 infected in mouse assessed as protection against bacterial infection by measuring mouse survival administered intravenously as single dose after 2 hrs of infection measured on day 7 Assay format: assay format Standard result: PD50 > 100.0 mg kg-1 Document: CHEMBL3868582
Reported result
PD50 > 100.0 mg kg-1
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Streptococcus pneumoniae (CHEMBL347) Assay: Antibacterial activity against Streptococcus pneumoniae PBS1399 infected in mouse assessed as protection against bacterial infection by measuring mouse survival administered intravenously as single dose after 2 hrs of infection measured on day 7 Assay format: assay format Standard result: PD50 > 100.0 mg kg-1 Document: CHEMBL3868582”

    ChEMBL activities for CHEMBL387675 · Activity 16801155

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In an organism-based bacterial growth reduction assay (6 to 8 hrs incubation), CHEMBL387675 showed EC50 = 5700.0 nM against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923).

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 5700.0 nM pChEMBL value: 5.24 Document: CHEMBL3808280[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 5700.0 nM pChEMBL value: 5.24 Document: CHEMBL3808280
Reported result
EC50 = 5700.0 nM
Source records
2
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 5700.0 nM pChEMBL value: 5.24 Document: CHEMBL3808280”

    ChEMBL activities for CHEMBL387675 · Activity 16606147

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c
  2. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Staphylococcus aureus (CHEMBL352) Assay: Antibacterial activity against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 5700.0 nM pChEMBL value: 5.24 Document: CHEMBL3808280”

    ChEMBL activities for CHEMBL387675 · Activity 16606147

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In an organism-based antibacterial assay with 5 mM Ca2+, the minimum inhibitory concentration (MIC) for CHEMBL387675 against Bacillus subtilis 1046 was 5.0 ug.mL-1.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 1.8 mM Ca2+ Assay format: organism-based format Standard result: MIC = 40.0 ug.mL-1 Document: CHEMBL3734663[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 5 mM Ca2+ Assay format: organism-based format Standard result: MIC = 5.0 ug.mL-1 Document: CHEMBL3734663[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 5 mM Ca2+ Assay format: organism-based format Standard result: MIC = 5.0 ug.mL-1 Document: CHEMBL3734663[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 1.8 mM Ca2+ Assay format: organism-based format Standard result: MIC = 40.0 ug.mL-1 Document: CHEMBL3734663
Reported result
MIC = 40.0 ug.mL-1
Source records
4
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 1.8 mM Ca2+ Assay format: organism-based format Standard result: MIC = 40.0 ug.mL-1 Document: CHEMBL3734663”

    ChEMBL activities for CHEMBL387675 · Activity 16389507

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c
  2. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 5 mM Ca2+ Assay format: organism-based format Standard result: MIC = 5.0 ug.mL-1 Document: CHEMBL3734663”

    ChEMBL activities for CHEMBL387675 · Activity 16389514

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c
  3. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 5 mM Ca2+ Assay format: organism-based format Standard result: MIC = 5.0 ug.mL-1 Document: CHEMBL3734663”

    ChEMBL activities for CHEMBL387675 · Activity 16389514

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c
  4. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Bacillus subtilis (CHEMBL359) Assay: Antibacterial activity against Bacillus subtilis 1046 in presence of 1.8 mM Ca2+ Assay format: organism-based format Standard result: MIC = 40.0 ug.mL-1 Document: CHEMBL3734663”

    ChEMBL activities for CHEMBL387675 · Activity 16389507

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Study findings

In an organism-based bacterial growth reduction assay (6 to 8 hrs incubation), CHEMBL387675 showed EC50 = 33000.0 nM against multidrug resistant Enterococcus faecium NCTC 7171 (ATCC 19434).

Sources[1]chembl-activitiesChEMBL activities for CHEMBL387675Molecule: CHEMBL387675 Target: Enterococcus faecium (CHEMBL357) Assay: Antibacterial activity against multidrug resistant Enterococcus faecium NCTC 7171 (ATCC 19434) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 33000.0 nM pChEMBL value: 4.48 Document: CHEMBL3808280
Reported result
EC50 = 33000.0 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL387675 Target: Enterococcus faecium (CHEMBL357) Assay: Antibacterial activity against multidrug resistant Enterococcus faecium NCTC 7171 (ATCC 19434) assessed as reduction in bacterial growth incubated for 6 to 8 hrs Assay format: organism-based format Standard result: EC50 = 33000.0 nM pChEMBL value: 4.48 Document: CHEMBL3808280”

    ChEMBL activities for CHEMBL387675 · Activity 16606117

    chembl-activities:chembl387675:b05b3da6a63c:b05b3da6a63c

Risks and interactions

Risks, organized for scanning.

Contraindications

Contraindication: a history of hypersensitivity to the active ingredient (daptomycin) precludes use.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Daptomycin for Injection is contraindicated in patients with known hypersensitivity to daptomycin[seeWarnings and Precautions (5.1)].
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Daptomycin for Injection is contraindicated in patients with known hypersensitivity to daptomycin[seeWarnings and Precautions (5.1)].”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 4 CONTRAINDICATIONS

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Safety findings

Safety signal: daptomycin for injection has reported cases of muscle toxicity, including myopathy (with elevated CPK) and rhabdomyolysis, sometimes associated with acute renal failure.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Myopathy, defined as muscle aching or muscle weakness in conjunction with increases in creatine phosphokinase (CPK) values to greater than 10 times the upper limit of normal (ULN), has been reported with the use of daptomycin for injection. Rhabdomyolysis, with or without acute renal failure, has been reported[seeAdverse Reactions (6.2)].
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Myopathy, defined as muscle aching or muscle weakness in conjunction with increases in creatine phosphokinase (CPK) values to greater than 10 times the upper limit of normal (ULN), has been reported with the use of daptomycin for injection. Rhabdomyolysis, with or without acute renal failure, has been reported[seeAdverse Reactions (6.2)].”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 5.2 Myopathy and Rhabdomyolysis

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Products and regulatory status

Same ingredient. Different records.

Regulatory status

Label limitation: pneumonia is an excluded indication for this drug product.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Daptomycin for Injection is not indicated for the treatment of pneumonia.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Daptomycin for Injection is not indicated for the treatment of pneumonia.”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 1.3 Limitations of Use

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Regulatory status

Regulatory limitation: the product is not approved for pediatric use.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003This Daptomycin for Injection product is not approved for use in pediatric patients[seeUse in Specific Populations (8.4)].
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “This Daptomycin for Injection product is not approved for use in pediatric patients[seeUse in Specific Populations (8.4)].”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 1.3 Limitations of Use

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Regulatory status

This product has an FDA-labeled indication for adult S. aureus bloodstream infection, including cases with right-sided infective endocarditis, for both methicillin-susceptible and methicillin-resistant isolates.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Daptomycin for Injection is indicated for the treatment of adult patients withStaphylococcus aureusbloodstream infections (bacteremia), including adult patients with right-sided infective endocarditis, caused by methicillin-susceptible and methicillin-resistant isolates.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Daptomycin for Injection is indicated for the treatment of adult patients withStaphylococcus aureusbloodstream infections (bacteremia), including adult patients with right-sided infective endocarditis, caused by methicillin-susceptible and methicillin-resistant isolates.”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 1.2Staphylococcus aureusBloodstream Infections (Bacteremia) in Adult Patients, Including Those with Right-Sided Infective Endocarditis, Caused by Methicillin-Susceptible and Methicillin-Resistant Isolates

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Regulatory status

Label limitation: left-sided infective endocarditis due to S. aureus is not an indication for this product.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Daptomycin for Injection is not indicated for the treatment of left-sided infective endocarditis due toS. aureus.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Daptomycin for Injection is not indicated for the treatment of left-sided infective endocarditis due toS. aureus.”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 1.3 Limitations of Use

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Regulatory status

This product has an FDA-labeled indication for adult cSSSI when the infection is due to susceptible Gram-positive organisms (including methicillin-resistant Staphylococcus aureus).

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Daptomycin for Injection is indicated for the treatment of adult patients with complicated skin and skin structure infections (cSSSI) caused by susceptible isolates of the following Gram-positive bacteria:Staphylococcus aureus(including methicillin-resistant isolates),Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus dysgalactiae subsp. equisimilis,andEnterococcus faecalis(vancomycin-susceptible isolates only).
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Daptomycin for Injection is indicated for the treatment of adult patients with complicated skin and skin structure infections (cSSSI) caused by susceptible isolates of the following Gram-positive bacteria:Staphylococcus aureus(including methicillin-resistant isolates),Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus dysgalactiae subsp. equisimilis,andEnterococcus faecalis(vancomycin-susceptible isolates only).”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 1.1 Complicated Skin and Skin Structure Infections (cSSSI)

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Administration context

The practical clinical context.

Dose records

Adult dosing for S. aureus bloodstream infection (including right-sided infective endocarditis) is 6 mg/kg IV once daily, with a labeled duration of 2 to 6 weeks, using 0.9% sodium chloride injection.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Administer Daptomycin for Injection 6 mg/kg to adult patients intravenously in 0.9% sodium chloride injection once every 24 hours for 2 to 6 weeks.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Administer Daptomycin for Injection 6 mg/kg to adult patients intravenously in 0.9% sodium chloride injection once every 24 hours for 2 to 6 weeks.”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 2.3 Dosage in Adult Patients withStaphylococcus aureusBloodstream Infections (Bacteremia), Including Those with Right-Sided Infective Endocarditis, Caused by Methicillin-Susceptible and Methicillin-Resistant Isolates

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Dose records

Adult dosing for cSSSI is weight-based (4 mg/kg) given intravenously once daily, with a labeled duration of 7 to 14 days, using 0.9% sodium chloride injection.

Sources[2]dailymedThese highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003Administer Daptomycin for Injection 4 mg/kg to adult patients intravenously in 0.9% sodium chloride injection once every 24 hours for 7 to 14 days.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Administer Daptomycin for Injection 4 mg/kg to adult patients intravenously in 0.9% sodium chloride injection once every 24 hours for 7 to 14 days.”

    These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 · 2.2 Dosage in Adults for cSSSI

    dailymed:1957b6ce-7382-4a7b-bf02-3595948d09c6:f48b3d79fe1c:f48b3d79fe1c

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, interaction
  • 107 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (60), assurance_score_below_0.72 (40), current_regulatory_source_required (22), extraction_ambiguity (63), high_risk_requires_regulatory_or_two_independent_sources (45), no_direct_support (95), proposal_not_staged (1)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL387675 ↗

    chembl-activities · published 2026-08-26 · retrieved 2026-08-26T08:42:26Z

  2. These highlights do not include all the information needed to use DAPTOMYCIN FOR INJECTION safely and effectively. See full prescribing information for DAPTOMYCIN FOR INJECTION.DAPTOMYCIN for injection, for intravenous useInitial U.S. Approval: 2003 ↗

    dailymed · published 2026-05-08 · retrieved 2026-09-04T19:33:06Z

  3. IUPHAR ligand commentary ↗

    iuphar-comments · published 2026-08-26 · retrieved 2026-08-26T08:42:26Z

  4. Impact of generic market entry on the consumption of last-resort antibiotics in six European countries. ↗

    pubmed · published 2026-09-01 · retrieved 2026-08-26T08:42:26Z

  5. Population pharmacokinetics of daptomycin in patients with haematological malignancies and vancomycin-resistant Enterococcus bloodstream infections. ↗

    pubmed · published 2026-08-24 · retrieved 2026-08-26T08:42:26Z

Publication history and provenance

Version 5 · Automated assessment · 2026-09-04T19:33:06Z

eecfc253888430874984eac016e5250f6cd5a9967f3ed5f0658d119f74fe184b