Greener peptide manufacture is a fast-growing area of interest for the pharmaceutical industry and many companies have invested heavily in developing increased capabilities for peptide synthesis in-house and at contract manufacturing organizations. In recent years, there has been a growing interest in therapeutic peptides within the pharmaceutical industry with more than 50 peptide drugs on the market, approximately 170 in clinical trials, and more than 200 in preclinical development. The synthesis of peptides is associated with the use of comparatively high volumes of hazardous solvent and reagents and little focus on green chemistry and engineering.
In 2016, the ACS Green Chemistry Institute Pharmaceutical Roundtable identified development of greener processes for peptide API as a critical unmet need, and as a result, a new Roundtable team formed to address this important area. In a recent perspective (see below; DOI: 10.1021/acs.joc.8b03001), the greener peptide team summarizes the current challenges of peptide synthesis and purification in terms of sustainability; highlights possible solutions; and encourages synergies between academia, the pharmaceutical industry, and contract research organizations and/or contract manufacturing organizations. The team is organizing around benchmarking, best practice sharing, and the identification of new synthetic methodologies in an attempt to reduce the environmental impacts associated with these processes.
Amgen, AZ, Asymchem, Bachem, BI, BMS, Enzytag, Genentech, GSK, Gilead, JNJ, Ipsen, Lilly, Pfizer, Roche, Polypeptide, Takeda, WuXi, Novonordisk, Novartis
Greener peptide design and development.
Sustainability Challenges in Peptide Synthesis and Purification: From R&D to Production; Albert Isidro-Llobet, Martin N. Kenworthy, Subha Mukherjee, Michael E. Kopach, Katarzyna Wegner, Fabrice Gallou, Austin G. Smith, Frank Rrochangar. J. Org. Chem. 2019, 84(8), 4615-4628. DOI: 10.1021/acs.joc.8b03001
ACS Webinar: Slimming the Waste-line in Large Molecule Syntheses
Presented by Michael Kopach and David Constable
Updated: October 2021
- Collect PMI data for PMI perspective article
- Organize and held Peptide section at 2021 GC&E
- Submitted Session Request for 2022 GC&E
- 2019 Perspectives Article Remains one of JOC’s most read papers now approaching 100 citations (https://doi.org/10.1021/acs.joc.8b03001)
- Albericio 2019 Ignition Grant Completed leading to 2021 paper (Amide Formation: Choosing the Safer Carbodiimide in Combination with OxymaPure to Avoid HCN Release (acs.org)
- Meeting time (west US vs Europe)
- ACS GCIPR Grant 2021: Prof Gosia Chwatko – Improvement of peptide yield and solvent reuse via membrane enhanced peptide synthesis;Points of Contact: Nick Ki (Lilly), Kasia Wegner (Ipsen)
- ACS GCIPR Grant 2020 wrapping up:
- Prof. Matthew Hostetler CUPS: An Atom Efficient and Low Waste Producing Method of Inverse Solid-Phase Peptide Synthesis. Points of Contact: Josh Bolger (AsymChem); Albert Isidro Llobet (GSK)
- Drafting PMI publication – draft for approval by the end of 2021
- Submit 2022 grant proposal
- Compete & Submit PMI publication to JOC
- Optimization of Articles of Interest Interface