Antibacterial drug discovery
Antibacterial drug discovery based on polyketide leads.
Polyketides are a mainstay of antibacterial therapy
Major anti-bacterial classes based on polyketides include the erythromycins, the tetracyclines, rifamycin and its derivatives and mupirocin. New classes continue to be developed; in 2008, an 18-membered macrolide polyketide therapeutic, fidaxomicin, showed efficacy in a phase III study of Clostridium difficile.
The first generation of naturally produced polyketide antibacterials was followed by a second, in which the parent molecule was semi-synthetically altered to improve activity or overcome resistance. For example, azithromycin and clarithromycin are both semi-synthetic derivatives of erythromycin, and both generated annual peak sales of over $1bn. The newer ketolide class of antibiotics, which includes telithromycin, is also derived semi-synthetically from erythromycin
Biotica’s exploratory programmes
Biotica’s technology allows access to novel chemical space, providing a third generation of antibacterials with further differentiated characteristics. This includes overcoming resistance and improving PK, for example to enhance oral bioavailability.
