Hong, W David, O'Neill, Paul M 
ORCID: 0000-0003-4338-0317, Taylor, Mark J, Turner, Joseph D, Ward, Stephen A, Gusovsky, Fabian, Benayoud, Farid, Shibuguchi, Nao, Girish, Dixit, Fang, Francis Gerard et al (show 9 more authors)
(2023)
Transformation of the Manufacturing Process from Discovery to Kilogram Scale for AWZ1066S: A Highly Specific Anti-Wolbachia Drug Candidate for a Short-Course Treatment of Filariasis.
ORGANIC PROCESS RESEARCH & DEVELOPMENT, 27 (1).
pp. 42-53.
ISSN 1083-6160, 1520-586X
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AWZ1066S Process Development_OPRD_Main_Final (preaccepted revised version).pdf - Author Accepted Manuscript Download (1MB) | Preview |
Abstract
Anti-Wolbachia therapy has been clinically proven to be a safe approach for the treatment of onchocerciasis and lymphatic filariasis. AWZ1066S, a first-in-class highly specific anti-Wolbachia drug candidate developed for a short-course treatment of human filariasis, has advanced into clinical development. An improved, cost-efficient, and scalable process for the manufacture of this clinical candidate is described. Presented herein is the process development work for the active pharmaceutical ingredient (API) and its two key starting materials [2-(trifluoromethyl)-3-pyridyl]methanamine and (S)-3-methylmorpholine, starting from 2,4-dichloropyrido[2,3-d]pyrimidine, which is capable of delivering high-purity (>99%) API consistently. The optimized production route was used in the manufacture of the clinical candidate at the kilogram scale to support the ongoing clinical development.
| Item Type: | Article |
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| Uncontrolled Keywords: | anti-Wolbachia, AWZ1066S, chiral morpholine analogue, filariasis, trifluoromethyl pyridine derivative |
| Divisions: | Faculty of Science and Engineering > School of Physical Sciences |
| Depositing User: | Symplectic Admin |
| Date Deposited: | 15 May 2023 07:32 |
| Last Modified: | 07 Dec 2024 23:11 |
| DOI: | 10.1021/acs.oprd.2c00167 |
| Related URLs: | |
| URI: | https://livrepository.liverpool.ac.uk/id/eprint/3170326 |
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