Table 2.

Candidate agent preparation, route of administration, half-maximal inhibitory concentration (IC₅₀), maximal and sustained serum concentrations after systemic delivery, and drug half-life in humans

Drug	Efficacy	Route	IC50 (μm)	Maximal serum concentration	Sustained serum concentration	Elimination half-life	Therapeutic category	Mode of action
Bortezomib	−94.38	iv	0.02	0.16–0.31 μm	0.078–0.156 mm	9–15 h	Antineoplastic	Proteasome inhibitor
Bufogenin	−65.83	NA	0.75	NA	NA	NA	Cardiotonic, respiratory stimulants	Steroids
Cantharidin	−69.03	Topical	1.28	NA	NA	NA	Antiviral	PP-1 and PP-2A inhibitor
Carboquone	−81.00	NA	1.5	NA	No available	NA	Antineoplastic	Alkylating agents
Carminomycin	−61.50	iv	0.47	NA	NA	NA	Antineoplastic, anthracycline antibiotics	DNA synthesis inhibitor
Deslanoside	−64.83	NA	0.13	0.16 μm	0.0021 mm	51 h	Cardiotonic	NA+/K+ ATPase inhibition
Floxuridine	−66.83	Arterial	0.6	NA	NA	NA	Antineoplastic	Pyrimidine antagonists
Fluvastatin	−67.78	PO	1.19	0.51–1.07 μm	0.022–0.03 μm	2.5–3 h	Antilipid	Apoptosis inducer
								HMG-CoA reductase inhibitor
Idarubicin	−92.87	iv	0.94	0.04–0.08 μm	0.004–0.01 μm	16–17.5 h	Antineoplastic	DNA polymerase inhibitor, Antimetabolites
Lanatoside A	−62.74	NA	0.09	NA	NA	NA	Cardiotonic	NA+/K+ ATPase inhibition
Lanatoside C	−78.28	NA	0.17	NA	NA	NA	Cardiotonic	NA+/K+ ATPase inhibition
Niclosamide	−64.31	PO/iv	0.27	NA	NA	NA	Anthelmintic	Niclosamide uncouples oxidative phosphorylation
Ouabain	−70.50	iv	0.05	0.128 μm	0.0004 μm	18 h	Cardiotonic	NA+/K+ ATPase inhibition
Proscillaridin A	−60.34	iv/PO	0.01	0.019 μm by iv; 0.0019 μm by PO	NA	23–33 h	Cardiotonic	Cardiac glycoside
Thioinosine	−67.79	NA	1.68	NA	NA	NA	Antineoplastic	Immunosuppressant
Vinblastine sulfate	−64.24	iv	0.21	NA	NA	24–25 h	Antineoplastic	Antimitotic drugs, tubulin polymerization inhibitor

NA, Not available; PO, by mouth; HMG-CoA, 3-hydroxyl-methyl-glutaryl-CoA.