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. Author manuscript; available in PMC: 2013 May 28.
Published in final edited form as: Nat Rev Drug Discov. 2012 Jan 3;11(1):52–68. doi: 10.1038/nrd3620

Table 1.

Human serine hydrolase inhibitors approved for clinical use.

Target Compound Structure Company Ref(s) Indication
ACHE Rivastigmine (Exelon) graphic file with name nihms466655t1.jpg Novartis 29 Alzheimer’s - associated dementia
Donepezil (Aricept) graphic file with name nihms466655t2.jpg Eisai 69
Galantamine (Razadyne) graphic file with name nihms466655t3.jpg Ortho-McNeil Janssen 72
Tacrine (Cognex) graphic file with name nihms466655t4.jpg Shionogi 66
DPP4 Sitagliptin (Januvia) graphic file with name nihms466655t5.jpg Merck 93 Type II diabetes
Saxagliptin (Onglyza) graphic file with name nihms466655t6.jpg Bristol Myers Squibb 92
Linagliptin (Tradjenta) graphic file with name nihms466655t7.jpg Boehringer Ingelheim 94
Vildagliptin* (Zomelis) graphic file with name nihms466655t8.jpg Novartis 31
Alogliptin* (Nesina) graphic file with name nihms466655t9.jpg Takeda 86
Pancreatic/ gastric lipases Orlistat (Xenical;Alli) graphic file with name nihms466655t10.jpg Roche; GlaxoSmithKline 19, 32 Obesity
Thrombin Dabigatran etexilate (Pradaxa) graphic file with name nihms466655t11.jpg Boehringer Ingelheim 46, 47 Thrombosis
Argatroban (Novastan) graphic file with name nihms466655t12.jpg GlaxoSmithKline Mitsubishi Pharma 42
Factor Xa Rivaroxaban (Xarelto) graphic file with name nihms466655t13.jpg Bayer 54, 59 Thrombosis
Human neutrophil elastase Sivelestat* (Elaspol) graphic file with name nihms466655t14.jpg Ono 33 Respiratory disease

The electrophilic moieties of each compound, if applicable, are colored red. The prodrug portions of dabigatran etexilate are colored blue.

*

Not yet approved in the United States.