New Release: Alpha testing version has been released.

Teicoplanin

J01X - Other antibacterials ATC J01XA02 Unknown

JFDA label: Targocid Vial

Mechanism of Action

Disrupting Agent of Peptidoglycan — Peptidoglycan disrupting agent

TargetActionGene / class
Peptidoglycan efficacy DISRUPTING AGENT

Indications

Approved

  • Bacterial Infections — bacterial disease

Off-label

  • Infections
  • Osteomyelitis
  • Skin Diseases

Antimicrobial Spectrum

Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: EUCAST v16 · curated.

Bacteria

OrganismActivityMIC
Coagulase-negative staphylococci Susceptible 4.0 mg/L
Enterococcus faecalis Susceptible 2.0 mg/L
Enterococcus faecium Susceptible 2.0 mg/L
Enterococcus spp. Susceptible 2.0 mg/L
Staphylococcus aureus Susceptible 2.0 mg/L
Streptococcus A/B/C/G Susceptible 2.0 mg/L
Streptococcus pneumoniae Susceptible 2.0 mg/L
Viridans group streptococci Susceptible 2.0 mg/L
Staphylococcus aureus Resistant 2.0 mg/L

Class profile

gramStatusGram+
spectrumBreadthNarrow
atypicalCoverageNo
isBactericidal1
moaCategoryCell wall synthesis inhibitor (glycopeptide, D-Ala-D-Ala binding)
pdIndexTime-dependent
postAntibioticEffectShort
mrsaCoverage1
resistanceMechanismsVanA gene cluster (high-level resistance),Cell wall thickening (VISA phenotype)

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3 RID 1.4%

Until more information becomes available, monitor the breastfed infant for gastrointestinal disturbances such as diarrhea, particularly in newborn and preterm infants.

LactMed: monitor the infant.

Monitoring

EfficacyCulture and susceptibility testing; clinical resolution (temperature, WBC, CRP, procalcitonin)
ToxicityRenal function (dose adjustment in renal impairment); hepatic function for hepatically cleared agents; signs of C. difficile infection (diarrhoea)
Clinical pearlCulture results guide de-escalation to narrower-spectrum therapy. Review antibiotic appropriateness at 48–72 h (antimicrobial stewardship).
CounselingComplete the full course. Report persistent diarrhoea, rash, or lack of improvement after 48–72 h.

Chemistry & Properties

2D structure
FormulaC88H97Cl2N9O33
Molecular weight1879.7 g/mol
IUPAC name(1S,2R,19R,22R,34S,37R,40R,52S)-2-[(2R,3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-22-amino-5,15-dichloro-64-[(2S,3R,4R,5S,6R)-3-(decanoylamino)-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-26,31,44,49-tetrahydroxy-21,35,38,54,56,59-hexaoxo-47-[(3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-7,13,28-trioxa-20,36,39,53,55,58-hexazaundecacyclo[38.14.2.23,6.214,17.219,34.18,12.123,27.129,33.141,45.010,37.046,51]hexahexaconta-3,5,8,10,12(64),14,16,23(61),24,26,29(60),30,32,41(57),42,44,46(51),47,49,62,65-henicosaene-52-carboxylic acid
CAS61036-62-2
PubChem CID133065662
InChIKeyBJNLLBUOHPVGFT-CAYRISATSA-N
logP0.5 (XLogP 0.5)
Polar surface area662.0 Ų
H-bond acceptors / donors34 / 24
SMILESCCCCCCCCCC(=O)NC1C(C(C(OC1OC2=C3C=C4C=C2OC5=C(C=C(C=C5)C(C6C(=O)NC(C7=C(C(=CC(=C7)O)OC8C(C(C(C(O8)CO)O)O)O)C9=C(C=CC(=C9)C(C(=O)N6)NC(=O)C4NC(=O)C1C2=CC(=CC(=C2)OC2=C(C=CC(=C2)C(C(=O)NC(CC2=CC(=C(O3)C=C2)Cl)C(=O)N1)N)O)O)O)C(=O)O)OC1C(C(C(C(O1)CO)O)O)NC(=O)C)Cl)CO)O)O

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life7.13 h
Volume of distribution0.214 L/kg
Protein binding91.4%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP2B6Inhibitor

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (13)

BrandForm / strengthPackAgentCitizen (JOD)
TALINAC 200mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 200 mg 1 amp pack varies Al Hilal Drug Store
TALINAC 200mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 200 mg 10 amp pack varies Al Hilal Drug Store
TALINAC 200mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 200 mg 50 amp pack varies Al Hilal Drug Store
TALINAC 400mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 400 mg 1 amp pack varies Al Hilal Drug Store
TALINAC 400mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 400 mg 10 amp pack varies Al Hilal Drug Store
TALINAC 400mg/vial, Powder and solvent for Solution for Injection or Infusion Infusion 400 mg 50 amp pack varies Al Hilal Drug Store
TEICODIS 200 Vial Teicoplanin 200 mg 1 vial Professional Drug Store
TEICODIS 400 Vial Teicoplanin 400 mg 1 vial Professional Drug Store
Targocid Tablet 400 mg 1 ampoule Ulfa Pharma Co.
Targocid Vial Vial 200 mg/3 ml 1 amp Ulfa Pharma Co.
Targoplanin 200mg Lyophilised mass in vial (I.V/I.M/I.P) Vial 200 mg 1 vial Hikma Pharmaceuticals Co.Ltd/Jordan
Teco 200mg Powder For Solution For Injection Powder for Injection 200 mg 1 vial ORIENT DRUG STORE CO
Ticopex 200mg/Vial Powder for solution For Inj Powder for Injection 200 mg 1 vial MS PHARMA/JORDAN