We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis of isotopically labeled daclatasvir for use in human clinical studies.
- Authors
Easter, John A.; Burrell, Richard C.; Bonacorsi, Samuel J.
- Abstract
Daclatasvir is a novel hepatitis C virus NS5A inhibitor developed by Bristol-Myers Squibb and marketed as Daklinza®. The need to support the development of daclatasvir required the synthesis of carbon-14 labeled material for use in human absorption, distribution, metabolism, and excretion studies. A total of 7.53 mCi of [14C]-daclatasvir was synthesized in eight steps from commercially available [14C]-copper cyanide. The radiochemical purity was 99.6%, and specific activity was 3.86 μCi/mg. To support a human absolute bioavailability study, 5.56 g of [13C2, 15N4]-daclatasvir was synthesized in four steps.
- Subjects
VIRUS inhibitors; HEPATITIS C virus; STABLE isotopes; CHEMICAL synthesis; BIOAVAILABILITY; RADIOCHEMICAL research
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2016, Vol 59, Issue 4, p164
- ISSN
0362-4803
- Publication type
Article
- DOI
10.1002/jlcr.3386