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

Hong, W. David, O’Neill, Paul M., Taylor, Mark ORCID: https://orcid.org/0000-0003-3396-9275, Turner, Joseph ORCID: https://orcid.org/0000-0002-2185-5476, Ward, Steve ORCID: https://orcid.org/0000-0003-2331-3192, Gusovsky, Fabian, Benayoud, Farid, Shibuguchi, Nao, Girish, Dixit, Fang, Francis Gerard, Talabhakthla, Ravi Kumar, Vaddi, Anand, Challa, Chiranjeevi, Reddy, Karri Satya Ammi, Kalla, Vijay, Srinivasa Rao, Sugandham, Nagireddi, Durga Mahesh Kumar, Patel, Jayesh and Khile, Anil Shahaji (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, Vol 27, Issue 1, pp. 42-53.

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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
Subjects:	WC Communicable Diseases > WC 20 Research (General) WC Communicable Diseases > Tropical and Parasitic Diseases > WC 880 Filariasis and related conditions (General)
Faculty: Department:	Biological Sciences > Department of Tropical Disease Biology
Digital Object Identifer (DOI):	https://doi.org/10.1021/acs.oprd.2c00167
SWORD Depositor:	JISC Pubrouter
Depositing User:	JISC Pubrouter
Date Deposited:	27 Mar 2023 13:46
Last Modified:	15 Oct 2024 14:33
URI:	https://archive.lstmed.ac.uk/id/eprint/21863

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