Table 3

CYP Enzyme	Direct IC₅₀ (mM)^a
CYP Enzyme	Remogliflozin^b	GSK279782^b	GSK333081^c	GSK1997711^c	GSK1997714^c	GSK355993^c
1A2	>100	>100	>100	>300	>300	>300
2A6	>100	>100	NT^d	NT	NT	NT
2B6	>100	>100	NT	NT	NT	NT
2C8	>100	>100	NT	NT	NT	NT
2C9	>100	>100	>100	>300	>300	>300
2C19	>100	>100	>100	>300	>300	>300
2D6	>100	>100	>100	>300	>300	>300
3A4	>100	>100	>100	>300	>300	>300

^aDirection inhibition studies added the inhibitor with probe substrate together. Assays were initiated with addition of cofactor. ^bCYP HPLC-LC/MS Inhibition method with probes substrates: CYP 1A2 Phenacetin; 2A6 – Coumarin; 2B6 – Buproprion; 2C8 – Rosiglitazone; 2C9 – Diclofenac; 2C19 – Mephenytoin; 2D6 – Bufuraol; 3A4 – Atorvastatin, Midazolam, and Nifedipine
^cCYP Flourescence Inhibition Method with probe substrates: CYP 1A2- ethoxyresorufin; 2C9 – 7-methoxy-4-trifluromethylcoumarin-3-acetic acid; 2C19 – 3-butyryl-7- methoxycoumarin; 2D6 – 4-methylaminomethyl-7-methoxycoumarin; 3A4 – diethoxyfluorescein and 7-benzyloxyquinoline
^dNT = not tested

Table 3: Inhibition of Cytochrome P450 Enzymes by Remogliflozin etabonate, Remogliflozin and Metabolites.