Metabolism, Excretion, and Pharmacokinetics of [14C]Tigecycline, a First-In-Class Glycylcycline Antibiotic, after Intravenous Infusion to Healthy Male Subjects

  title={Metabolism, Excretion, and Pharmacokinetics of [14C]Tigecycline, a First-In-Class Glycylcycline Antibiotic, after Intravenous Infusion to Healthy Male Subjects},
  author={Matthew Hoffmann and William Demaio and R. A. Juste Jord{\'a}n and Rasmy E. Talaat and Dawn Harper and John L. Speth and Joann Scatina},
  journal={Drug Metabolism and Disposition},
  pages={1543 - 1553}
Tigecycline, a novel, first-in-class glycylcycline antibiotic, has been approved for the treatment of complicated intra-abdominal infections and complicated skin and skin structure infections. The pharmacokinetics, metabolism, and excretion of [14C]tigecycline were examined in healthy male volunteers. Tigecycline has been shown to bind to bone; thus, to minimize the amount of radioactivity binding to bone and to maximize the recovery of radioactivity, tigecycline was administered intravenously… 

Pharmacokinetics, Distribution, Metabolism, and Excretion of Omadacycline following a Single Intravenous or Oral Dose of 14C-Omadacycline in Rats

ABSTRACT The absorption, distribution, metabolism, and excretion (ADME) of omadacycline, a first-in-class aminomethylcycline antibiotic with a broad spectrum of activity against Gram-positive,

Pharmacokinetics and Safety of a Single Intravenous Dose of the Antibiotic Tigecycline in Patients With Cirrhosis

A single intravenous dose of tigecycline 100 mg was safe and well‐tolerated in patients with cirrhosis with varying degrees of hepatic functional reserve and doses should be reduced by 50%, to 25 mg, every 12 hours in Patients with severely decompensated disease.

Clinical disposition, metabolism and in vitro drug–drug interaction properties of omadacycline

Omadacycline was metabolically stable in human liver microsomes and hepatocytes and did not inhibit or induce any of the nine cytochrome P450 or five transporters tested and was a substrate of P-glycoprotein, but not of the other transporter.

Clinical Pharmacokinetics and Pharmacodynamics of Tigecycline

Tigecycline is the first representative of a new drug class, the glycylcyclines, and was approved in 2005 by the US FDA for the treatment of complicated skin and skin structure infections, as well as complicated intra-abdominal infections.

Tigecycline pharmacokinetics, tolerability, safety, and effect on intestinal microflora in healthy Japanese male subjects

The pharmacokinetic profile of tigecycline was similar to non‐Japanese subjects; tolerability and change in intestinal microflora were also similar; the most common adverse events were nausea and vomiting.

Tigecycline and cyclosporine interaction—an interesting case of biliary-excreted drug enhancing the oral bioavailability of cyclosporine

  • N. Srinivas
  • Medicine, Biology
    European Journal of Clinical Pharmacology
  • 2009
An interesting observation of enhanced blood levels of cyclosporine in a renal transplant patient upon co-medication with tigecycline is reported, and additional views are brought in for consideration to explain this intriguing phenomenon.

Serum and urine pharmacokinetics of tigecycline in obese class III and normal weight adults.

  • M. Pai
  • Medicine, Biology
    The Journal of antimicrobial chemotherapy
  • 2014
A lower CFR is predicted against certain Gram-negative pathogens with the current standard tigecycline dosing regimen, irrespective of TBW and the effects of total body weight (TBW) on PK parameters are assessed.

Pharmacokinetics of tigecycline in turkeys following different routes of administration

Because TIG is not absorbed from the gastrointestinal tract in turkeys to a clinically significant degree, this drug given p.o. could find application in commercial turkey farms only to treat gastrointestinal tract infections.

Comparison of the pharmacokinetic properties of vancomycin, linezolid, tigecyclin, and daptomycin

The present article reviews the pharmacokinetic properties of vancomycin, linezolid, tigecycline and daptomycin and examines their oral bioavailability, elimination pathways, and half-life.



Pharmacokinetics of Tigecycline after Single and Multiple Doses in Healthy Subjects

Tigecycline exhibits linear pharmacokinetics and is safe and well tolerated in the dose ranges examined, and side effects, mainly nausea and vomiting, were seen in these studies.


  • H. EisnerR. Wulf
  • Medicine
    The Journal of pharmacology and experimental therapeutics
  • 1963
The metabolism of C 14 -labeled chlortetracycline following oral, intraperitoneal and intravenous administration in the rat and intravenously in the dog has been studied and significant amounts of radioactivity were excreted via the feces.

The metabolism and tissue distribution of radioisotopically labeled demethylchlortetracycline.

Radio-activity determinations on serum taken at various hours following the dosage substantiated the property of prolonged maintenance of antibiotic in the blood stream following a given dose of demethylchlortetracycline.

Pharmacokinetics in the interpretation of chronic toxicity tests: the last-in, first-out phenomenon.

Metabolism of tetracycline in the rat and the dog.

Data show that with the exception of metal chelate formation, tetracycline is chemically unaltered by the rat, and the urines from the dog also contained unchanged drug thus indicating that in this species no metabolic transformation of tetrACYcline had occurred.

Pharmacokinetic Profile of Tigecycline in Serum and Skin Blister Fluid of Healthy Subjects after Multiple Intravenous Administrations

ABSTRACT The pharmacokinetics of tigecycline, when given as a 100-mg loading dose followed by 50 mg every 12 h, were determined in serum and blister fluid. The peak tigecycline concentration and

Evidence for metabolic inertness of doxycycline.

Both ion-exchange and reversed-phase chromatography failed to reveal significant by-products in urine and feces, except for minor amounts of 4-epidoxycycline, and enzymatic hydrolysis procedures did not present any evidence of the conjugates.

Identification and determination of the two principal metabolites of minocycline in humans.

The glycylcyclines: a comparative review with the tetracyclines.

Tigecycline appears to be a promising new antibacterial based on in vitro and pharmacokinetic/pharmacodynamic activity; however more clinical data are needed to fully evaluate its potential.