Table 4.

Summary of results for glucuronidation studies of compound 1 and raltegravir

Compound	Microsome or UGT Isoform	Glucuronide	Reversed-phase HPLC retention time (min), UV detection (nm)	Substrate for UGT? Yes or No
1	-	-	18.6 min, 350 nm
1	pHLM (Xenotech)	Nonea	-	No
1	pHLM (BD Biosciences)	Nonea	-	No
1	UGT1A1 (BD Biosciences)	Nonea	-	No
1	UGT1A3 (BD Biosciences)	Nonea	-	No
Raltegravir	-	-	30.3 min, 300 nm
Raltegravir	pHLM (Xenotech)	Glucuronide	16.4 min, 300 nm	Yes
Raltegravir	pHLM (BD Biosciences)	Glucuronide	16.4 min, 300 nm	Yes
Raltegravir	UGT1A1 (BD Biosciences)	Glucuronide	16.4 min, 300 nm	Yes
Estradiol	-	-	27.9 min, 280 nm
Estradiolb	pHLM (BD Biosciences)	Glucuronides (two)	9.7 min, 11.2 min, 280 nm	Yes
Estradiolb	UGT1A1 (BD Biosciences)	Glucuronide	9.6 min, 280 nm	Yes
Methylumbelliferone	-	-	21.1 min, 318 nm
Methylumbelliferoneb	pHLM (Xenotech)	Glucuronide	6.1 min, 318 nm	Yes
Trifluoperazine	-	-	19.2, 256 nm
Trifluoperazineb	pHLM (Xenotech)	N-Glucuronide	18.0 min, 256 nm	Yes

^aThe glucuronide of compound 1, if formed, would have been observed at a retention time of approximately 8 min. However, no such peak in the HPLC chromatograms using 254 nm, 300 nm or 350 nm detection wavelengths was observed.

^bEstradiol, 4-methylumbelliferone and trifluoperazine were used as positive control substrates.