Gemifioxacin(CAS: 175463-14-6)

Molecular Structure

Gemifloxacin mesylate (trade name Factive, Oscient Pharmaceuticals) is an oral broad-spectrum

quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic

bronchitis and mild-to-moderate pneumonia. Vansen Pharma Inc. has licensed the active

ingredient from LG Life Sciences of Korea.

Indications

Gemifloxacin is indicated for the treatment of infections caused by susceptible strains of the

designated microorganisms in the conditions listed below.

Acute bacterial exacerbation of chronic bronchitis caused by S. pneumoniae, Haemophilus

influenzae, Haemophilus parainfluenzae, or Moraxella catarrhalis

Community-acquired pneumonia (of mild to moderate severity) caused by S. pneumoniae

(including multi-drug resistant strains, Haemophilus influenzae, Moraxella catarrhalis,

Mycoplasma pneumoniae, Chlamydia pneumoniae, or Klebsiella pneumoniae

Microbiology

Gemifloxacin has been shown to be active against most strains of the following microorganisms:

Aerobic gram-positive microorganisms – Streptococcus pneumoniae

including multi-drug resistant Streptococcus pneumoniae (MDRSP). MDRSP includes isolates

previously known as PRSP (penicillin-resistant Streptococcus pneumoniae), and are strains

resistant to two or more of the following antibiotics: penicillin, 2nd generation cephalosporins,

e.g., cefuroxime, macrolides, tetracyclines and trimethoprim/sulfamethoxazole.

Staphylococcus aureus and Streptococcus pyogenes

Aerobic gram-negative microorganisms – Haemophilus influenzae, Haemophilus parainfluenzae,

Klebsiella pneumoniae (many strains are moderately susceptible), Moraxella catarrhalis,

Acinetobacter lwoffii, Klebsiella oxytoca, Legionella pneumophila, Proteus vulgaris.

Other microorganisms – Chlamydia pneumoniae, Mycoplasma pneumoniae

Adverse effects

See also: Adverse effects of fluoroquinolones

Fluoroquinolones are generally well tolerated with most side effects being mild and serious

adverse effects being rarely. Some of the serious adverse effects which occur more commonly

with fluoroquinolones than with other antibiotic drug classes include CNS and tendon toxicity.

The currently marketed quinolones have safety profiles similar to that of other antimicrobial classes.

The serious events may occur with therapeutic or with acute overdose. At therapeutic doses

they include: central nervous system toxicity, cardiovascular toxicity, tendon / articular toxicity,

and rarely hepatic toxicity. Events that may occur in acute overdose are rare and include: renal

failure and seizure. Children and the elderly are at greater risk. Tendon damage may manifest

during, as well as up to a year after fluoroquinolone therapy.

The FDA ordered a black box warnings on all fluoroquinolones advising consumers of the

possible toxic effects of fluoroquinolones on tendons.

On August 15th, 2013 the FDA issued a Safety Announcement where they described that they

are requiring the medication guides and drug labels for all fluoroquinolones to be updated and

better describe the risk for peripheral neuropathy. The peripheral neuropathy may occur very

quickly, and may be irreversible. This warning applies to fluoroquinolones taken by mouth

and injection, but does not apply to fluoroquinolones taken topically.

Current findings

One recent study showed that Gemifloxacin possess anti-metastatic activities

against breast cancer in vitro and in vivo (in mice).