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The magic of small structure differences in a sodium‐glucose cotransporter drug discovery project— 14 C‐labelled drug candidates in a key‐differentiating study
Author(s) -
Schudok Manfred,
Glombik Heiner,
Derdau Volker
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3869
Subject(s) - chemistry , drug , drug discovery , sodium , cotransporter , in vivo , pharmacology , radiochemistry , biochemistry , organic chemistry , medicine , microbiology and biotechnology , biology
We describe the dramatic differences in the synthesis and physiological and pharmacokinetical profiling of two sodium‐glucose cotransporter (SGLT) drug candidates AVE2268 and AVE8887 with very similar chemical structures. It is a classic example of how a radioactive study was able to spare resources in preclinical development prior to entering a costly clinical program. It also demonstrated that radioactive compounds can be used to study differences between two very similar compounds in vivo.