The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

Steven M. Mennen; Carolina Alhambra; C. Liana Allen; Mario Barberis; Simon Berritt; Thomas A. Brandt; Andrew D. Campbell; Jesús Castañón; Alan H. Cherney; Melodie Christensen; David B. Damon; J. Eugenio De Diego; Susana García-Cerrada; Pablo García-Losada; Rubén Haro; Jacob Janey; David C. Leitch; Ling Li; Fangfang Liu; Paul C. Lobben; David W.C. Macmillan; Javier Magano; Emma McInturff; Sebastien Monfette; Ronald J. Post; Danielle Schultz; Barbara J. Sitter; Jason M. Stevens; Iulia I. Strambeanu; Jack Twilton; Ke Wang; Matthew A. Zajac

doi:10.1021/acs.oprd.9b00140

The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

Steven M. Mennen, Carolina Alhambra, C. Liana Allen, Mario Barberis, Simon Berritt, Thomas A. Brandt, Andrew D. Campbell, Jesús Castañón, Alan H. Cherney, Melodie Christensen, David B. Damon, J. Eugenio De Diego, Susana García-Cerrada, Pablo García-Losada, Rubén Haro, Jacob Janey, David C. Leitch, Ling Li, Fangfang Liu, Paul C. LobbenDavid W.C. Macmillan, Javier Magano, Emma McInturff, Sebastien Monfette, Ronald J. Post, Danielle Schultz, Barbara J. Sitter, Jason M. Stevens, Iulia I. Strambeanu, Jack Twilton, Ke Wang, Matthew A. Zajac

Research output: Contribution to journal › Article › peer-review

316 Scopus citations

Abstract

High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. Today, most major pharmaceutical companies have created dedicated HTE groups within their process development teams, invested in automation technology to accelerate screening, or both. The industry's commitment to accelerating process development has led to rapid innovations in the HTE space. This review will deliver an overview of the latest best practices currently taking place within our teams in process chemistry by sharing frequently studied transformations, our perspective for the next several years in the field, and manual and automated tools to enable experimentation. A series of case studies are presented to exemplify state-of-the-art workflows developed within our laboratories.

Original language	English (US)
Pages (from-to)	1213-1242
Number of pages	30
Journal	Organic Process Research and Development
Volume	23
Issue number	6
DOIs	https://doi.org/10.1021/acs.oprd.9b00140
State	Published - Jun 21 2019

All Science Journal Classification (ASJC) codes

Physical and Theoretical Chemistry
Organic Chemistry

Keywords

automation
catalysis
high-throughput experimentation
screening

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10.1021/acs.oprd.9b00140

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Mennen, S. M., Alhambra, C., Allen, C. L., Barberis, M., Berritt, S., Brandt, T. A., Campbell, A. D., Castañón, J., Cherney, A. H., Christensen, M., Damon, D. B., Eugenio De Diego, J., García-Cerrada, S., García-Losada, P., Haro, R., Janey, J., Leitch, D. C., Li, L., Liu, F., ... Zajac, M. A. (2019). The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future. Organic Process Research and Development, 23(6), 1213-1242. https://doi.org/10.1021/acs.oprd.9b00140

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abstract = "High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. Today, most major pharmaceutical companies have created dedicated HTE groups within their process development teams, invested in automation technology to accelerate screening, or both. The industry's commitment to accelerating process development has led to rapid innovations in the HTE space. This review will deliver an overview of the latest best practices currently taking place within our teams in process chemistry by sharing frequently studied transformations, our perspective for the next several years in the field, and manual and automated tools to enable experimentation. A series of case studies are presented to exemplify state-of-the-art workflows developed within our laboratories.",

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author = "Mennen, {Steven M.} and Carolina Alhambra and Allen, {C. Liana} and Mario Barberis and Simon Berritt and Brandt, {Thomas A.} and Campbell, {Andrew D.} and Jes{\'u}s Casta{\~n}{\'o}n and Cherney, {Alan H.} and Melodie Christensen and Damon, {David B.} and {Eugenio De Diego}, J. and Susana Garc{\'i}a-Cerrada and Pablo Garc{\'i}a-Losada and Rub{\'e}n Haro and Jacob Janey and Leitch, {David C.} and Ling Li and Fangfang Liu and Lobben, {Paul C.} and Macmillan, {David W.C.} and Javier Magano and Emma McInturff and Sebastien Monfette and Post, {Ronald J.} and Danielle Schultz and Sitter, {Barbara J.} and Stevens, {Jason M.} and Strambeanu, {Iulia I.} and Jack Twilton and Ke Wang and Zajac, {Matthew A.}",

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month = jun,

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doi = "10.1021/acs.oprd.9b00140",

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Mennen, SM, Alhambra, C, Allen, CL, Barberis, M, Berritt, S, Brandt, TA, Campbell, AD, Castañón, J, Cherney, AH, Christensen, M, Damon, DB, Eugenio De Diego, J, García-Cerrada, S, García-Losada, P, Haro, R, Janey, J, Leitch, DC, Li, L, Liu, F, Lobben, PC, Macmillan, DWC, Magano, J, McInturff, E, Monfette, S, Post, RJ, Schultz, D, Sitter, BJ, Stevens, JM, Strambeanu, II, Twilton, J, Wang, K & Zajac, MA 2019, 'The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future', Organic Process Research and Development, vol. 23, no. 6, pp. 1213-1242. https://doi.org/10.1021/acs.oprd.9b00140

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AU - Berritt, Simon

AU - Brandt, Thomas A.

AU - Campbell, Andrew D.

AU - Castañón, Jesús

AU - Cherney, Alan H.

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AU - Damon, David B.

AU - Eugenio De Diego, J.

AU - García-Cerrada, Susana

AU - García-Losada, Pablo

AU - Haro, Rubén

AU - Janey, Jacob

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AU - Li, Ling

AU - Liu, Fangfang

AU - Lobben, Paul C.

AU - Macmillan, David W.C.

AU - Magano, Javier

AU - McInturff, Emma

AU - Monfette, Sebastien

AU - Post, Ronald J.

AU - Schultz, Danielle

AU - Sitter, Barbara J.

AU - Stevens, Jason M.

AU - Strambeanu, Iulia I.

AU - Twilton, Jack

AU - Wang, Ke

AU - Zajac, Matthew A.

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KW - catalysis

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The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

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All Science Journal Classification (ASJC) codes

Keywords

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