Single Ascending Dose Safety and Pharmacokinetics of CDRI-97/78: First-in-Human Study of a Novel Antimalarial Drug

Table 5

Pharmacokinetic parameters of converted active metabolite 97/63 after oral administration of 97/78 at 200 mg single dose to male healthy human volunteers (𝑁=16).

PK parameter	Converted in  vivo metabolite, 97/63																Mean ± SEM
	Male healthy human volunteers (𝑁=16)
	1	2	3	4	5	6	7	8	9	10	11	12	13	14	15	16
𝐶max (ng/mL)	172	20.1	373	187	149	355	42.6	202	60.9	295	47.4	50.4	65.4	105	55	123	𝟏𝟒𝟑.𝟗𝟑±𝟐𝟖.𝟑𝟐
𝑇max (h)	1.5	4	1	2	1.5	2	4	4	4	2	2	2	1.5	1.5	2	1.5	𝟐.𝟐𝟖±𝟎.𝟐𝟕
𝑇1/2 (h)	13.89	2.17	4.78	2.20	3.88	21.27	3.00	8.94	7.80	11.63	24.26	14.50	10.10	17.73	24.51	18.90	𝟏𝟏.𝟖𝟓±𝟏.𝟗𝟒
AUC0−∞; (ng⋅h/mL)	788.7	104.8	1644	602.6	785	1522.6	207.9	1604.9	511.7	1898.9	935	356.1	583.6	696.8	833.1	984.1	𝟖𝟕𝟖.𝟕𝟒±𝟏𝟑𝟑.𝟏𝟓
MRT (h)	12.57	5.72	13.7	3.53	5.38	14.25	6.42	14.13	9.28	9.76	30.72	14.53	11.26	18.37	32.20	18.52	𝟏𝟑.𝟕𝟕±𝟐.𝟎𝟓