# Covalent drugs the ChEMBL 37 approved small-molecule set (2,104 drugs) does not contain, checked by hand on 2026-10-29. Not part of the main counts.
# Not listed: ensitrelvir, icotinib and sevabertinib (non-covalent); simnotrelvir, atilotrelvir and limertinib (covalent mechanism or approval date not verified).
name	first_approval_year	first_approval_detail	definition	warhead_class	bond	reversibility	target	verification	source_url
Rilzabrutinib	2025	FDA 2025-08-29 (UAE June 2025)	strict	Cyanoacrylamide	Protein cysteine	Reversible	BTK Cys481	Regulator approval confirmed for FDA; mechanism from the first-approval review	https://doi.org/10.1007/s40265-025-02259-w
Remibrutinib	2025	FDA 2025-09-30	strict	Acrylamide	Protein cysteine	Irreversible	BTK Cys481	FDA approval confirmed (Novartis release); residue from class knowledge	https://www.novartis.com/us-en/news/media-releases/novartis-receives-fda-approval-rhapsido-remibrutinib-only-oral-targeted-btki-treatment-chronic-spontaneous-urticaria
Sunvozertinib	2023	NMPA August 2023; FDA 2025-07-02	strict	Acrylamide	Protein cysteine	Irreversible	EGFR exon 20 insertions (Cys797)	FDA approval confirmed; residue from class knowledge	https://www.fda.gov/drugs/resources-information-approved-drugs/fda-grants-accelerated-approval-sunvozertinib-metastatic-non-small-cell-lung-cancer-egfr-exon-20
Zongertinib	2025	FDA 2025-08-08	strict	Acrylamide	Protein cysteine	Irreversible	HER2 Cys805	FDA approval and covalent mechanism confirmed	https://doi.org/10.1158/2159-8290.CD-24-0306
Lirafugratinib	2026	FDA 2026-09-23	strict	Acrylamide	Protein cysteine	Irreversible	FGFR2 Cys491	FDA approval and covalent mechanism confirmed	https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-lirafugratinib-previously-treated-unresectable-locally-advanced-or-metastatic
Firmonertinib	2021	NMPA 2021-03-03	strict	Acrylamide	Protein cysteine	Irreversible	EGFR Cys797	China only; approval from press; covalent mechanism from class knowledge	https://flcube.com/?p=20016
Aumolertinib	2020	NMPA 2020-03-19	strict	Acrylamide	Protein cysteine	Irreversible	EGFR Cys797	China only; approval from press; covalent mechanism from class knowledge	https://www.businesswire.com/news/home/20200319005185/en/%C2%A0Hansoh-Pharma%E2%80%99s-AMEILE-almonertinib-Receives-Marketing-Authorization
Befotertinib	2023	NMPA 2023-05-29	strict	Acrylamide	Protein cysteine	Irreversible	EGFR Cys797	China only; approval on NMPA page; covalent mechanism from class knowledge	https://english.nmpa.gov.cn/2023-05/31/c_923522.htm
Pyrotinib	2018	NMPA August 2018	strict	Acrylamide	Protein cysteine	Irreversible	HER2 and EGFR	China only; abstract calls it an irreversible inhibitor; residue not verified	https://doi.org/10.1038/s41401-018-0176-6
Orelabrutinib	2020	NMPA about 2020-12-25	strict	Acrylamide	Protein cysteine	Irreversible	BTK Cys481	China only; review states covalent binding	https://doi.org/10.1080/14656566.2022.2144218
Garsorasib	2024	NMPA about November 2024	strict	Acrylamide	Protein cysteine	Irreversible	KRAS G12C	China only; approval on NMPA page; covalent mechanism from class knowledge	https://english.nmpa.gov.cn/2025-02/19/c_1073662.htm
Fulzerasib	2024	NMPA 2024-08-21	strict	Acrylamide	Protein cysteine	Irreversible	KRAS G12C	China only; approval on NMPA notice; covalent mechanism from class knowledge	https://subsites.chinadaily.com.cn/nmpa/2025-02/19/c_1073526.htm
Glecirasib	2025	NMPA reported 2025-05-22	strict	Acrylamide	Protein cysteine	Irreversible	KRAS G12C	China only; approval from company announcement; covalent mechanism from class knowledge	https://www.tipranks.com/news/company-announcements/jacobios-kras-g12c-inhibitor-glecirasib-gains-approval-for-market-launch
Leritrelvir	2023	NMPA March 2023	strict	Ketoamide	Protein cysteine	Reversible	SARS-CoV-2 main protease Cys145	China only; approval on NMPA page; covalent binding stated in abstract	https://doi.org/10.1038/s41564-024-01618-9
Tranylcypromine	1961	ChEMBL first approval 1961	broad	Cyclopropylamine	Prosthetic group (FAD) of target	Irreversible	Monoamine oxidase (FAD cofactor)	In ChEMBL 37 but dropped by the population rules because ChEMBL stores the racemate as two disconnected components	https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL3989843/
Cisplatin	1978	ChEMBL first approval 1978	broad	Platinum(II) complex	DNA	Irreversible	DNA (guanine N7)	In ChEMBL 37 but dropped by the population rules because it contains a metal	https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL11359/
Carboplatin	1989	ChEMBL first approval 1989	broad	Platinum(II) complex	DNA	Irreversible	DNA (guanine N7)	In ChEMBL 37 but dropped by the population rules because it contains a metal	https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1351/
Oxaliplatin	2002	ChEMBL first approval 2002	broad	Platinum(II) complex	DNA	Irreversible	DNA (guanine N7)	In ChEMBL 37 but dropped by the population rules because it contains a metal	https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL414804/