Principia Biopharma: a University of California, San Francisco, startup offers a reversible twist on covalent drugs
K Garber - Nature Biotechnology, 2013 - go.gale.com
K Garber
Nature Biotechnology, 2013•go.gale.comCovalent drugs, largely ignored for decades, are staging a comeback. Five irreversible
covalent kinase inhibitors have advanced to phase 3 in recent years, with Boehringer
Ingelheim's afatinib now under review by US and European regulatory agencies for treating
lung cancer. Meanwhile, Principia Biopharma, a startup dedicated to covalent drug
development, is offering a unique twist on covalent drugs--reversibility.Covalent drugs
typically bond irreversibly and, consequently, pharma has mostly avoided them because of …
covalent kinase inhibitors have advanced to phase 3 in recent years, with Boehringer
Ingelheim's afatinib now under review by US and European regulatory agencies for treating
lung cancer. Meanwhile, Principia Biopharma, a startup dedicated to covalent drug
development, is offering a unique twist on covalent drugs--reversibility.Covalent drugs
typically bond irreversibly and, consequently, pharma has mostly avoided them because of …
Covalent drugs, largely ignored for decades, are staging a comeback. Five irreversible covalent kinase inhibitors have advanced to phase 3 in recent years, with Boehringer Ingelheim's afatinib now under review by US and European regulatory agencies for treating lung cancer. Meanwhile, Principia Biopharma, a startup dedicated to covalent drug development, is offering a unique twist on covalent drugs--reversibility.
Covalent drugs typically bond irreversibly and, consequently, pharma has mostly avoided them because of the potential for unpredicted toxicities or immune reactions. Of reversible drugs, the vast majority bind noncovalently, relying on ionic bonds, hydrogen bonds, hydrophobic bonds or van der Waals forces--all generally weaker than covalent bonds, in which the drug and target share a pair of electrons.
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