Antibiotic – nemonoxacin

Published: 5-May-2010
Research & Development Pharmaceutical

Quinolone antibiotics prevent the bacteria’s DNA from unwinding, thus stopping them replicating

Quinolone antibiotics first reached the market in the 1960s, and work by preventing the bacteria’s DNA from unwinding, and thus stopping them replicating. The key target is the enzyme topoisomerase II, or DNA gyrase, and more recently introduced quinolone antibiotics such as ciprofloxacin and moxifloxacin have increased activity againt this enzyme.

However, there is a growing incidence of resistance against these key antibacterial agents; notably, the majority of strains of methicillin-resistant Streptococcus aureus are resistant to marketed quinolones. There is also significant resistance from several other bacteria, including Streptococcus pneumoniae and Pneumococcus influenzae. Therefore, there is a need for analogues of these otherwise potent antibiotics that retain activity against these resistant strains.

One such molecule that is under development is TaiGen Biotechnology’s nemonoxacin, which licensed the non-fluorinated quinolone drug from Procter & Gamble for development in a variety of Asian markets.1 It shows good activity against MRSA, multidrug resistant S. pneumoniae, vancomycin-resistant S. aureus and a wide range of other bacteria, both Gram positive and Gram negative.

Results of two Phase I trials have recently been published. In one 56 healthy subjects were enrolled in a double blind, ascending single dose study and randomised to one of seven dose cohorts.2 In each of these, two subjects were given placebo, and six single oral doses of between 25 and 1500mg nemonoxacin. It was well tolerated up to the maximum dose, and no serious adverse events were seen, with the most common being contact dermatitis, erythema and pruritis. Its peak time was 1 to 2 hours, and half-life between 9 and 16 hours.

In the second, 46 healthy volunteers were given oral doses of 75 to 1000mg once a day for 10 days.3 It was generally safe and well tolerated, with the most common side-effects being headache, contact dermatitis and rash. It was rapidly absorbed within 2 hours of dosing, and a steady state was achieved after 3 days in most subjects. The pharmacokinetics were affected by food, causing a decrease in plasma concentration, but free drug levels were good whether the subjects were fasting or fed.

A randomised, double blind Phase II trial has also been reported.4 Its efficacy was compared with that of levofloxacin in patients with community acquired pneumonia at once daily doses of 500 or 750mg for seven days. The most common pathogens involved were H. influenzae, S. pneumoniae and S. aureus. Clinical cure rates were 92% for the higher dose of nemonoxacin, 88% for the lower dose, and 94% for 500mg of levofloxacin. In addition, the company has recently announced by press release that it had shown promising clinical efficacy and good tolerability in a Phase II trial in patients with diabetic foot infections.

References

1. G.G. Zhanel et al. 48th Ann. Intersci. Conf. Antimicrob. Agents Chemother. Infect. Dis. Soc. Am. Ann. Meet. (Oct 25-28, Washington DC), 2008, Abst F1-2057; N. Laing et al. ibid. Abst. C1-1957
2. L. Lin et al. Antimicrob Agents Chemother. 2010, 54, 405
3. D.T. Chang et al. Antimicrob Agents Chemother. 2010, 54, 411
4. D.J. van Rensburg et al. 48th Ann. Intersci. Conf. Antimicrob. Agents Chemother. Infect. Dis. Soc. Am. Ann. Meet. (Oct 25-28, Washington DC), 2008, Abst. L-678
See more

You may also like

Research & Development

Quotient Sciences extends partnership for ultra-rare disease treatment

Read more
This collaboration reinforces Quotient Sciences’ commitment to supporting the manufacture of niche and smaller volume commercial products often overlooked by larger CDMOs

Trending Articles

  1. You need to be a subscriber to read this article.
    Click here to find out more.
    Landmark NHS‑Galleri trial cuts Stage IV cancers and boosts early detection across England NHS‑Galleri trial shows multi‑cancer blood test sharply reduces late‑stage diagnoses and boosts early detection—possibly signalling a structural change in cancer drug demand, supply chain planning and long-term oncology production strategy
  2. Johnson & Johnson files FDA application for IMAAVY in wAIHA Johnson & Johnson has submitted an sBLA to the US Food and Drug Administration seeking approval of IMAAVY as the first-ever treatment for warm autoimmune haemolytic anaemia, supported by Phase II/III ENERGY trial data showing rapid and durable haemoglobin response
  3. Horizon Europe 2025 grant backs Phase II trial of HER-096 for Parkinson’s disease Herantis Pharma has secured selection for €8m in non-dilutive funding under Horizon Europe to advance a Phase II proof-of-concept study of its subcutaneously delivered Parkinson’s therapy candidate HER-096
  4. THX Pharma and Biocodex pair up to advance rare disease research Biocodex has acquired two licences from THX Pharma to develop and commercialise Batten-1 worldwide and TX01 in the US and Canada, with the deal totalling up to $173m
  5. Navigating AI regulation for digital medical devices in global markets New whitepaper outlines regulatory pathways for AI-powered medical technologies in the UK, US and EU

Upcoming event

DCAT Week

23–26 March 2026 | Conference | New York, US See all

You may also like

Research & Development

Quotient Sciences extends partnership for ultra-rare disease treatment

This collaboration reinforces Quotient Sciences’ commitment to supporting the manufacture of niche and smaller volume commercial products often overlooked by larger CDMOs
Research & Development

OSE Immunotherapeutics receives positive IDMC review for Phase III ARTEMIA trial

OSE Immunotherapeutics SA has received a second positive recommendation from the Independent Data Monitoring Committee to continue its Phase III ARTEMIA trial of Tedopi in advanced non-small cell lung cancer
Research & Development

Vilnius University scientists reveal new role for CRISPR-Cas9 in bacterial immunity

The researchers report in Molecular Cell that the CRISPR-Cas9 protein plays a previously unknown role in selecting and integrating viral DNA fragments during bacterial immune memory formation
Research & Development

Lilly’s Orforglipron beats oral semaglutide in Phase III ACHIEVE-3 trial with superior weight loss

Head-to-head data published in The Lancet show Eli Lilly's oral GLP-1 candidate orforglipron delivered significantly greater HbA1c reductions and weight loss than oral semaglutide in adults with type 2 diabetes, supporting global regulatory submissions
Regulatory

Johnson & Johnson files FDA application for IMAAVY in wAIHA

Johnson & Johnson has submitted an sBLA to the US Food and Drug Administration seeking approval of IMAAVY as the first-ever treatment for warm autoimmune haemolytic anaemia, supported by Phase II/III ENERGY trial data showing rapid and durable haemoglobin response
Research & Development

Almirall advances etherna’s mRNA/LNP therapy LAD116 into IND-enabling studies

Almirall has selected LAD116, developed using etherna's intratumoral mRNA/LNP platform, for IND-enabling studies in non-melanoma skin cancer, marking a key milestone toward GMP manufacturing and Phase I clinical trials
Research & Development

SPARK THE MIDLANDS backs Aston University anti-cancer bone paste collaboration

A collaboration between Aston University and Royal Orthopaedic Hospital NHS Foundation Trust has secured support from SPARK THE MIDLANDS to advance a minimally invasive gallium-doped injectable paste for treating primary and metastatic bone cancer
Subscribe now