Synthesis of isotopically labeled daclatasvir for use in human clinical studies
John A Easter1, Richard C Burrell1, Samuel J Bonacorsi2
1Bristol-Myers Squibb Research and Development, Discovery Chemistry Platforms-Radiochemistry, 5 Research Parkway, Wallingford, CT, 06424, USA.
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 [(14) C]-daclatasvir was synthesized in eight steps from commercially available [(14) C]-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 [(13) C2 , (15) N4 ]-daclatasvir was synthesized in four steps.
Related Concept Videos
Clinically Relevant Drug Product Specifications: Methods of Establishment
Bioavailability Study Design: Healthy Subjects Versus Patients
Bioavailability Study Design: Single Versus Multiple Dose Studies

![An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F66708.jpg&w=3840&q=50)
