. 2022 Jan 28;77(4):880–902. doi: 10.1093/jac/dkab505

Table 5.

Overview of pharmacokinetic parameters of delamanid evaluated in various animal studies

Reference	Animal model	Infected	Dose (mg/kg)	Single drug or combination	Treatment duration	Route of drug administration	Sample	Methods	T _max (h)	T_½ (h)	C _max (mg/L)	AUC time span	AUC (μg·h/mL)
Mallikaarjun et al. (2020)⁹²	Mice, SLC:ICR	No	0.625	Single drug	Single-dose	Oral gavage	Plasma	HPLC-MS/MS			0.100	0–24	1.188
	Mice, SLC:ICR	No	2.5	Single drug	Single-dose	Oral gavage	Plasma	HPLC-MS/MS			0.297	0–24	3.581
	Mice, SLC:ICR	No	10	Single drug	Single-dose	Oral gavage	Plasma	HPLC-MS/MS			1.012	0–24	11.547
Matsumoto et al. (2006)¹⁰	Mice	Yes	2.5	Single drug	Single dose	Oral	Plasma	LC-ESI-MS/MS	6	7.6	0.297	0–24	4.13
Pieterman et al. (2021)⁹³	Mice, BALB/c	Yes	2.5	BDQ (25) + LZD (100)	4 weeks	Oral gavage	Plasma	LC-MS/MS	0.75		0.864–1.080	0–24	11.234
Sasahara et al. (2015)⁸⁷	Mice, ICR	No	3	Single drug	Single dose	Oral	Plasma	LC-MS/MS	2	7.2	0.4787	0–480	5.536
												0–∞	6.1508
	Mice, ICR	No	30	Single drug	Single dose	Oral	Plasma	LC-MS/MS			2.3141	0–24	35.8403
	Mice, ICR	No	30	Single drug	13 weeks	Oral	Plasma	LC-MS/MS			2.9209	0–24	36.5094
Ramirez et al. (2021)⁹⁴	Rats, Sprague Dawley	No	10	Single drug	Single-dose	Oral gavage	Plasma	HPLC	3.4		0.256	0–96	5.68
Shibata et al. (2017)⁸⁴	Rats, Sprague-Dawley; males, non-fasted	No	3	Single drug	Single dose	Oral	Blood	Radioactivity of ¹⁴C-labelled delamanid	8	82.3	0.5818	0–168	19.4
												0–∞	22.8
	Rats, Sprague-Dawley; males, fasted	No	3	Single drug	Single dose	Oral	Blood	Radioactivity of ¹⁴C-labelled delamanid	6.3	49.5	0.7351	0–168	19.6
												0–∞	20.9
	Rats, Sprague-Dawley; females, non-fasted	No	3	Single drug	Single dose	Oral	Blood	Radioactivity of ¹⁴C-labelled delamanid	8	57.2	0.643	0–168	20.3
												0–∞	22.3
	Rats, Sprague-Dawley; females, fasted	No	3	Single drug	Single dose	Oral	Blood	Radioactivity of ¹⁴C-labelled delamanid	5	59.8	0.8149	0–168	19.7
												0–∞	21.3
Sasahara et al. (2015)⁸⁷	Rats, Sprague-Dawley	No	3	Single drug	Single dose	Oral	Plasma	LC-MS/MS	4	5.1	0.6005	0–480	7.9418
												0–∞	7.9698
	Rats, Sprague-Dawley	No	30	Single drug	Single dose	Oral	Plasma	LC-MS/MS			2.6953	0–24	36.6397
	Rats, Sprague-Dawley	No	30	Single drug	26 weeks	Oral	Plasma	LC-MS/MS			1.7992	0–24	34.2379
Chen et al. (2017)⁹⁵	Guinea pigs	No	10	Single drug	Single dose	Oral	Plasma	HPLC-ESI-MS/MS			0.21	0–48	2.32
		No	100	Single drug	Single dose	Oral	Plasma	HPLC-ESI-MS/MS			0.53	0–48	9.45
Tucker et al. (2019)⁸⁵	Rabbits, New Zealand White	Yes	5	Single drug	Single-dose	Oral gavage	Plasma	HPLC-MS/MS	12	13.9	0.2558	0–24	3.8112
												0–48	4.229
												0–∞	4.2553
	Rabbits, New Zealand White	No	5	Single drug	Single-dose	Oral gavage	Plasma	HPLC-MS/MS	12	14.1	0.1956	0–24	2.7856
												0–48	3.4613
												0–∞	3.5545
Sasahara et al. (2015)⁸⁷	Dogs	No	10	Single drug	Single dose	Oral	Plasma	LC-MS/MS	8	18.4	0.3578	0–768	10.628
												0–∞	10.9275
	Dogs, beagle	No	30	Single drug	Single dose	Oral	Plasma	LC-MS/MS			0.3831
	Dogs, beagle	No	30	Single drug	39 weeks	Oral	Plasma	LC-MS/MS			1.4007	0–24	21.7692

T _max, time until the highest concentration is reached; T_½, half-life time, time until the initial drug concentration is halved; C_max, highest concentration reached.