Table 1. EC of HU or other RNR... | American Society of Hematology

Table 1.

EC of HU or other RNR inhibitors, and ACT’s partner drugs or active metabolite of ART against Pf3D7, PfNF54, and PfDd2 asexual blood stages in vitro

Molecule	Pf3D7		PfNF54			PfDd2
Molecule	EC₅₀, μM	EC₉₀, μM	EC₅₀, μM	EC₉₀, μM	∗Fold difference	EC₅₀, μM	EC₉₀, μM	†Fold difference
RNR inhibitor
HU	127.6 (105.8-140.8)	471.5 (376.8-592.8)	144.8 (142.3-147.4)	344.1 (302.6-459.3)	1.13	225.9 (201.5-235.6)	759 (499-1043)	1.77
3AP	0.55 (0.54-0.60)	2.30 (1.7-3.0)	0.46 (0.45-0.46)	0.89 (0.81-0.99)	0.84	0.32 (0.28-0.39)	0.50 (0.46-0.78)	0.58
Gem	0.80 (0.67-0.90)	13.1 (10.4-19.7)	0.57 (0.52-0.62)	12.7 (11.1-14.2)	0.71	1.07 (0.77-1.52)	54.96 (34.64-86.25)	1.33
Clof	100.1 (86.8-110)	189.2 (168-227.2)	85.2 (84.4-86.0)	156.4 (148.5-162.1)	0.85	99.8 (96.21-104.08)	259.4 (227.85-289.4)	1.00
Antimalarial drug
LUM × 10-3	13.1 (5.3-26.8)	82.1 (31.7-165.4)	ND	ND	—	15.63 (13.32-17.93)	57.52 (45.12-69.91)	1.19
AQ × 10-3	12.9 (9.3-17.4)	21.6 (15.6-24.1)	ND	ND	—	14.76 (12.54-16.97)	32.14 (19.62-44.66)	1.14
CQ × 10-3	13.6 (11.8-16.7)	20.3 (18.4-23.4)	ND	ND	—	100.8	193.2	7.41
PQ	0.37 (0.29-0.44)	2.2 (1.9-2.7)	ND	ND	—	0.67 (0.55-0.78)	1.58 (1.20-1.95)	1.81
TQ	0.06 (0.04-0.09)	0.61 (0.32-1.84)	ND	ND	—	ND	ND	—
DHA × 10-3	4.1 (3.0-5.2)	17.2 (9.5-25.3)	ND	ND	—	4.94 (3.57-6.30)	11.3 (9.15-13.45)	1.20

Molecule	Pf3D7		PfNF54			PfDd2
Molecule	EC₅₀, μM	EC₉₀, μM	EC₅₀, μM	EC₉₀, μM	∗Fold difference	EC₅₀, μM	EC₉₀, μM	†Fold difference
RNR inhibitor
HU	127.6 (105.8-140.8)	471.5 (376.8-592.8)	144.8 (142.3-147.4)	344.1 (302.6-459.3)	1.13	225.9 (201.5-235.6)	759 (499-1043)	1.77
3AP	0.55 (0.54-0.60)	2.30 (1.7-3.0)	0.46 (0.45-0.46)	0.89 (0.81-0.99)	0.84	0.32 (0.28-0.39)	0.50 (0.46-0.78)	0.58
Gem	0.80 (0.67-0.90)	13.1 (10.4-19.7)	0.57 (0.52-0.62)	12.7 (11.1-14.2)	0.71	1.07 (0.77-1.52)	54.96 (34.64-86.25)	1.33
Clof	100.1 (86.8-110)	189.2 (168-227.2)	85.2 (84.4-86.0)	156.4 (148.5-162.1)	0.85	99.8 (96.21-104.08)	259.4 (227.85-289.4)	1.00
Antimalarial drug
LUM × 10-3	13.1 (5.3-26.8)	82.1 (31.7-165.4)	ND	ND	—	15.63 (13.32-17.93)	57.52 (45.12-69.91)	1.19
AQ × 10-3	12.9 (9.3-17.4)	21.6 (15.6-24.1)	ND	ND	—	14.76 (12.54-16.97)	32.14 (19.62-44.66)	1.14
CQ × 10-3	13.6 (11.8-16.7)	20.3 (18.4-23.4)	ND	ND	—	100.8	193.2	7.41
PQ	0.37 (0.29-0.44)	2.2 (1.9-2.7)	ND	ND	—	0.67 (0.55-0.78)	1.58 (1.20-1.95)	1.81
TQ	0.06 (0.04-0.09)	0.61 (0.32-1.84)	ND	ND	—	ND	ND	—
DHA × 10-3	4.1 (3.0-5.2)	17.2 (9.5-25.3)	ND	ND	—	4.94 (3.57-6.30)	11.3 (9.15-13.45)	1.20

EC data are presented as median (interquartile range).

ART, artemisinin; EC, effective concentration; ND, not done.

∗

PfNF54/Pf3D7 ratio of EC₅₀.

†

PfDd2/Pf3D7 ratio of EC₅₀.

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