Synthesis of a Dual Carbon ‐14 Labeled CGRP Receptor Antagonist For Use in a Human ADME Study

Oral calcitonin gene-related peptide (CGRP) receptor antagonists have been shown to be effective in the acute and preventive treatment of migraine. CGRP receptor antagonists offer safety advantages over triptans because they are not active vasoconstrictors, which reduces cardiovascular risks. Bristol Myers Squibb discovered a high affinity CGRP receptor antagonist BMS-927711 for the treatment of migraine now FDA approved as Nurtec ® ODT (rimegepant). Dual labeled [14C]-BMS-927711 was prepared and used in a human absorption-distribution-metabolism-elimination (ADME) study. A dual labeled analog of BMS-927711 was required to fully track the compound ’s metabolic transformation. The carbon-14 labeled synthesis of both right side and left side portions of [14C]-BMS-927711 are described.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research