TABLE 2

IC₅₀ values of the selected anti-TB drugs on common human hepatic CYPs and UGTs

	Bedaquiline		Rifabutin		Pyrazinamide		Ethambutol		Rifampicin		Isoniazid
	W^{^a} μM	W/O^{^b} μM	W μM	W/O μM	W μM	W/O μM	W μM	W/O μM	W μM	W/O μM	W μM	W/O μM
CYP1A2	NC^{^c}	NC	NC	NC	NC	NC	NC	NC	—	—	—	—
CYP3A	NC	NC	27.9	31.5	NC	NC	NC	NC	—	—	—	—
CYP2B6	NC	NC	120.8	165.3	NC	NC	NC	NC	—	—	—	—
CYP2C8	NC	NC	64.0	62.6	NC^{^d}	NC	NC^{^e}	NC	—	—	—	—
CYP2C9	NC	NC	75	150.9	NC	NC	NC	NC	—	—	—	—
CYP2C19	NC	NC	NC	NC	NC	NC	NC	NC	—	—	—	—
CYP2D6	NC	NC	147.7	166.5	NC	NC	NC	NC	—	—	—	—
CYP2E1	NC	NC	NC	NC	NC	NC	NC	NC	—	—	—	—
UGT1A1	NC	NC	35	44	NC	NC	NC	NC	70	63	NC	NC
UGT1A4	-^{^f}	NC	10.8	11.3	—	NC	—	NC	—	230	—	NC
UGT1A6	—	NC	—	NC	—	NC	—	NC	—	^{^g}	—	NC
UGT1A9	—	NC	—	NC	—	NC	—	NC	—	NC	—	NC
UGT2B7	—	NC	—	^{^h}	—	NC	—	NC	—	NC	—	NC
UGT2B15	—	NC	—	81.3	—	NC	—	NC	—	357	—	NC
APAP-Glucuronidation	NC	NC	237.2	422.2	NC	NC	NC	NC	860	545	NC	NC

↵^a Incubations with preincubation.
↵^b Incubations without preincubation.
↵^c Not calculated (No IC₅₀ values were obtained due to less than 50% inhibition at the highest tested concentrations: 1000 μM for rifampicin, pyrazinamide, ethambutol, and isoniazid; 600 μM for rifabutin, and 25 μM for bedaquiline).
↵^d 41% inhibition at 1000 μM.
↵^e 37% inhibition at 1000 μM.
↵^f not tested.
↵^g 58% inhibition at 1000 μM.
↵^h 57% inhibition at 600 μM.