Table 2

Excretion of delavirdine and its metabolites after single and multiple oral dose administration of [¹⁴C]delavirdine mesylate^2-a

Dose mg/kg/day	Sex/N	Dose Freq.	Matrix	[¹⁴C-carboxamide]Delavirdine Mesylate
Dose mg/kg/day	Sex/N	Dose Freq.	Matrix	MET-2 Despyridinyl DLV	MET-9^2-b Indole Carboxylic Acid conj.	MET-10 Indole Carboxylic Acid	MET-3^2-cDesalkyl DLV conjugate	MET-4a N-Sulf Desalkyl DLV	MET-5 Desalkyl DLV	MET-6 6′-OGluc DLV	MET-7 6′-OH DLV	DLV
10	M /4	Single dose	Urine	1.8 ± 0.2	ND	8.2 ± 2.3	1.6 ± 1.1	0.5 ± 0.3	9.4 ± 0.4	0.3 ± 0.4	0.3 ± 0.4	ND
	F /4			2.4 ± 0.5	ND	7.8 ± 2.1	1.3 ± 0.9	ND	9.4 ± 0.2	0.3 ± 0.6	ND	ND
250	M /4	Single dose	Urine	1.6 ± 0.2	ND	14.8 ± 2.4	1.5 ± 0.9	0.1 ± 0.1	11.1 ± 3.0	1.1 ± 0.3	0.4 ± 0.1	ND
	F /4			1.9 ± 0.2	ND	15.0 ± 2.6	2.4 ± 1.3	ND	11.4 ± 0.6	1.2 ± 0.1	ND	ND
200	M /2	Multiple dose	Urine	1.3 ± 0.3	5.5 ± 3.1	11.4 ± 0.4	0.3 ± 0.1	ND	8.9 ± 1.0	1.0 ± 0.2	0.1 ± 0.1	ND
			Feces	24.0 ± 0.4	ND	3.1 ± 0.7	2.3 ± 0.2	0.3 ± 0.0	7.9 ± 0.2	ND	2.2 ± 0.1	3.1 ± 0.6
			Total	25.4 ± 0.7	5.5 ± 3.1	14.4 ± 1.1	2.6 ± 0.3	0.3 ± 0.0	16.8 ± 1.2	1.0 ± 0.2	2.3 ± 0.2	3.1 ± 0.6

				[2-¹⁴C-Pyridine]Delavirdine Mesylate
				MET-13 Desalkyl Pyridine Piperazine	MET-14 Pyridine Ring Opened	MET-12 N-IsoPr Pyridine Piperazine	MET-3^2-c Desalkyl DLV Conjugate	MET-4a N-Sulf Desalkyl DLV	MET-5 Desalkyl DLV	MET-6 6′-OGluc DLV	MET-7 6′-OH DLV	DLV
250	M /2	Single-dose	Urine	5.0 ± 1.5	1.1 ± 0.2	13.0 ± 3.5	4.6 ± 1.2	ND	9.9 ± 0.3	0.7 ± 0.3	ND	ND
			Feces	ND	ND	0.8 ± 1.1	1.3 ± 0.0	ND	8.3 ± 1.1	ND	3.3 ± 0.3	25.9 ± 2.0
			Total	5.0 ± 1.5	1.1 ± 0.2	13.7 ± 4.6	5.8 ± 1.3	ND	18.2 ± 0.8	0.7 ± 0.3	3.3 ± 0.3	25.9 ± 2.0

↵2-a Mean ± SD in percent of administered dose; values for feces were corrected for extraction recovery. Other minor metabolites are not listed. ND, not detected.
↵2-b MET-9 was tentatively characterized as a labile conjugate of the indole carboxylic acid metabolite (U-96364).
↵2-c MET-3 was tentatively characterized as a thermally labile conjugate of desalkyl delavirdine (U-96183).