The Pharmaceutical Journal
Vol 269 No 7205 p11
6 July 2002

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Novel antibiotic for targeting resistant pathogens in early stage development

A novel broad-spectrum antibiotic that targets resistant pathogens has been entered into early stage development by Aventis Pharma. Phase I trials of the antibiotic, AVE-6971, are expected to begin next year.

Dr Frank Douglas, executive vice-president for drug innovation and approval, Aventis, speaking at the company's research and development day in London last month, said that AVE-6971 has a different mechanism of action to fluoroquinolones and linezolid and works by inhibiting topoisomerase IV, an enzyme involved in bacterial DNA replication. It is bactericidal against methicillin-resistant Staphylococcus aureus and has good oral efficacy in mouse models.

Several other drugs in early-stage development were also highlighted at the meeting. An orally active immunomodulator for the treatment of multiple sclerosis that blocks pyrimidine synthesis, 1726, has entered phase II trials, and a new, non-hypnotic, serotonin (5-HT_2a) antagonist, 100,907, has been shown in a recently completed phase I trial to be promising for improving sleep quality.

AVE-7688, in development for the treatment of hypertension and congestive heart failure, has also been found, in preclinical trials, to be more potent than ACE inhibitors in preventing renal disease. Dr Douglas commented that this agent may be used for the prevention of diabetic neuropathy as well as treatment.

A colorectal cancer vaccine in the pipeline, ALVAC-CEA, which works by eliciting a tumour-specific response without toxicity, has been shown to stabilise disease in one-third of patients studied over a two-year period. Aventis is currently working on a second vaccine to target multiple antigens.

A new formulation of docetaxel (Taxotere), LIT-976, has an improved safety profile over the current formulation and has the potential to be used in combination with other antineoplastic agents.

At the meeting, Aventis announced that Lantus (insulin glargine), a recombinant basal insulin analogue for once daily delivery, is expected to be launched in the United Kingdom later this year.