Table 1. IC 50 and possible targets of... | American Society of Hematology

Table 1.

IC₅₀and possible targets of the 9 top-hit drugs on vitamin K–dependent carboxylation

Drugs	IC₅₀ ± SD, nM		Potential target*	Increased INR or bleeding risks†
Drugs	KO reduction	K reduction	Potential target*	Increased INR or bleeding risks†
Warfarin	8 ± 1	>10 000	KO reduction	Yes
Nitazoxanide	124 ± 9	>10 000	KO reduction	Yes
Lansoprazole	967 ± 49	>10 000	KO reduction	Yes
Itraconazole	1 161 ± 157	258 ± 21	Vitamin K availability	Yes
Clofazimine	789 ± 91	2 964 ± 669	Vitamin K reduction	Yes
Idebenone	1 858 ± 408	2 196 ± 621	Vitamin K reduction	—
AM404	1 976 ± 590	2 864 ± 621	Vitamin K reduction	—
Nelfinavir	8 305 ± 1 574	9 418 ± 1 234	Vitamin K availability	Yes
Orlistat	>10 000	>10 000	Vitamin K availability	Yes

Drugs	IC₅₀ ± SD, nM		Potential target*	Increased INR or bleeding risks†
Drugs	KO reduction	K reduction	Potential target*	Increased INR or bleeding risks†
Warfarin	8 ± 1	>10 000	KO reduction	Yes
Nitazoxanide	124 ± 9	>10 000	KO reduction	Yes
Lansoprazole	967 ± 49	>10 000	KO reduction	Yes
Itraconazole	1 161 ± 157	258 ± 21	Vitamin K availability	Yes
Clofazimine	789 ± 91	2 964 ± 669	Vitamin K reduction	Yes
Idebenone	1 858 ± 408	2 196 ± 621	Vitamin K reduction	—
AM404	1 976 ± 590	2 864 ± 621	Vitamin K reduction	—
Nelfinavir	8 305 ± 1 574	9 418 ± 1 234	Vitamin K availability	Yes
Orlistat	>10 000	>10 000	Vitamin K availability	Yes

If a drug targets multiple steps in the vitamin K redox cycle, the most severe inhibition is listed.

References for increased INR and bleeding risks associated with each drug are listed in supplemental Table 2.