Skip to main content
. 2022 Aug 25;21(12):881–898. doi: 10.1038/s41573-022-00542-z

Table 1.

Key examples of covalent drugs

Drug (company; former compound name) Structure Target Approvala Refs.
Osimertinib (AstraZeneca; AZD9291) graphic file with name 41573_2022_542_Taba_HTML.gif Mutant-selective EGFR inhibitor 2015 for treatment of NSCLC 44,45,48,49
Ibrutinib (AbbVie; PCI-32765) graphic file with name 41573_2022_542_Tabb_HTML.gif BTK inhibitor 2013 for treatment of mantle-cell lymphoma and, subsequently, many other B cell malignancies 55,56,60
Sotorasib (Amgen; AMG-510) graphic file with name 41573_2022_542_Tabc_HTML.gif KRAS(G12C) inhibitor 2021 for treatment of NSCLC with KRASG12C mutation 93–95
Nirmatrelvir (Pfizer; PF-07321332) graphic file with name 41573_2022_542_Tabd_HTML.gif SARS-CoV-2 main protease inhibitor Authorized for emergency use by FDA in 2021 for treatment of COVID-19b 103,105
Voxelotor (Global Blood Therapeutics; GBT-440) graphic file with name 41573_2022_542_Tabe_HTML.gif Mutant-haemoglobin modulator 2019 for treatment of sickle cell anaemia 142,143,145

BTK, Bruton’s tyrosine kinase; COVID-19, coronavirus disease 2019; EGFR, epidermal growth factor receptor; NSCLC, non-small-cell lung cancer; SARS-CoV-2, severe acute respiratory syndrome coronavirus 2. aUnless otherwise indicated, the date of the first approval by one of the major regulatory agencies is provided, which was the FDA in each case. bNirmatrelvir is approved for use in combination with ritonavir (Paxlovid). The FDA’s emergency use authorization preceded approval by other agencies, but Paxlovid has not yet been fully approved by the FDA.