Research & Development Programs

MaxThera’s product driven drug discovery and development strategy is focused on designing and optimizing new structures to inhibit new targets, in new biochemical pathways, that are distinct from those broadly used in pharmaceutical R&D. MaxThera has established a product development platform comprised of novel, validated antibacterial targets and the tools needed to identify and develop new antibacterial therapeutic products.

With a singular focus on the science of antibacterial drug discovery - beginning with a thorough understanding of New Target enzymology - MaxThera has achieved remarkable progress on the path to addressing the antibiotic resistance crisis. The Company plans to file its first IND in 2009.

Summary of MaxThera’s Product Development Pipeline

The drug candidates -

• are unique chemically novel substances
• are not related to any existing antibacterial drugs
• are thoroughly screened for drug-like characteristics such as low toxicity, high solubility and favorable pharmacokinetic properties
• are inhibitors of a unique bacterial target and have antibacterial activity

The targets -

• are distinct from targets used for existing drugs
• are derived from comparative genomics tools screening for druggable biochemical pathways and enzymes
• are essential for growth and survival for a broad spectrum of bacteria
• are not orthologous (redundant) to any biochemical activity within the bacterial cell
• are not closely related to any human enzyme activity
• are readily amenable to x-ray crystallography and assay development

The enzyme assays -

• are developed in the context of full kinetic characterization of the catalyzed reaction
• are carried out with substrate concentrations >> K_M - under V_max conditions - to afford highly robust inhibition data
• are designed to measure enzyme inhibition during the initial velocity phase (v₀) of the enzyme reaction - where the measurement of inhibition is most accurate
• are designed to require effective inhibitors to compete with a large excess of the natural substrate
• are capable of identifying and characterizing enzyme inhibitors having a very wide range of target inhibition activities

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