METHOD FOR THE SELECTIVE AND QUANTITATIVE FUNCTIONALIZATION OF IMMUNOGLOBULIN FAB FRAGMENTS, CONJUGATE COMPOUNDS OBTAINED WITH THE SAME AND COMPOSITIONS THEREOF

摘要

The invention provides chemical conjugates between an immunoglobulin Fabfragment and molecular entities imparting diagnostic or therapeutic utility,whereby the only sites of conjugation on the Fab fragment are one s or both ofthe sulfhydryl groups deriving from the selective and quantitative reductionof the inter-chain disulfide bond of said Fab fragment and whereby saidmolecular entities imparting diagnostic or therapeutic utility have at leastone free sulfllydryl-reactive group, characterized in that the conjugationstoichiometric molar ratio molecular entity to Fab fragment is in the rangefrom 0.95 to 1.05 or in the range from 1.95 to 2.05. The invention alsoprovides a process for preparing said conjugates and pharmaceuticalcompositions thereof.