TABLE 4.
In vitro and in vivo data for small-molecule therapeutics against Ebolaa
Compound (reference) | EC50 (μM) | Drug class | Dose (mg/kg) and dosage regimenb | % survival (treatment) in mice | % survival (control) in mice |
---|---|---|---|---|---|
Amodiaquine (10) | 34†, 2.6* | Antimalarial | 60, i.p., BID | 0 | 0 |
Benztropine (10) | 9.2†, 14* | Antihistamine/anticholinergic | 13, p.o., QD | 10 | 0 |
5, i.p., BID | 10 | 0 | |||
Chloroquine (36, 57) | 16†, 4.7* | Antimalarial antirheumatic | 90, i.p., BID | 80 | 0 |
90, i.p., BID | 0 | 0 | |||
Chlorotetracycline (10) | 24†, >50* | Antibiotic | 200, p.o., QD | 0 | 0 |
50, i.p., BID | 0 | 0 | |||
Clomiphene (10) | 11†, 1.3* | Selective estrogen modulator | 60, i.p., BID | 10 | 0 |
21, p.o., QD | 0 | 0 | |||
Favipiravir (58, 59) | 31–67† | Purine nucleic acid analogue | 150, p.o., BID | 100 | 0 |
300, p.o., BID | 100 | 0 | |||
FGI-106 (60) | 0.1† | Antiviral | 2, i.p., QD | 100 | 10 |
5, i.p., QD | 100 | 10 | |||
Galidesivir (61) | 3.1† | Nucleoside analog | 25, i.m., BID | 100‡ | 0 |
GS-5734 (7) | 1.5† | Nucleoside analog | 10 (day 0) and 3 (day 3), i.p. | 100‡ | 0 |
10, i.v., QD | 100‡ | 0 | |||
NSC 62914 (62) | 5.2† | Antioxidant | 2, i.p., QD | 90 | 0 |
Prochlorperazine (10) | 11†, 1.9* | Phenothiazine antipsychotic | 10, i.p., QD | 10 | 20 |
Tetrandrine (9) | 0.055† | Two-pore channel blocker | 30, i.p., QD (days 0, 1, 3, 5, 7) | 70 | 0 |
30, i.p., QD (days 1, 3, 5, 7) | 30 | 0 | |||
90, i.p., QD (days 1, 3, 5, 7) | 40 | 0 | |||
Tilorone | 0.23† | Antiviral | 25, i.p., QD | 90 | 10 |
50, i.p., QD | 90 | 10 | |||
30, i.p., QD | 100 | 10 | |||
60, i.p., QD | 100 | 10 |
Symbols: †, replication; *, entry; ‡, nonhuman primate.
BID, twice a day; QD, once daily; i.m., intramuscular; p.o., per os; i.v., intravenous; i.p., intraperitoneal.