TABLE 2.
Reported human pharmacokinetic properties of FDA-approved top hits.
| Sample name | Cmax (ng/ml) | MW (g/mol) | Cmax (µM) | Elimination T1/2 | Dosing regimen | References |
|---|---|---|---|---|---|---|
| (+/-) -Fluoxetine | 15–55 | 309.33 | 0.05–0.18 | 1–3 days | Single dose 40 mg PO | Eli Lilly and Company (1987) |
| Amiodarone hydrochloride | 5,000–41,000 | 681.78 | 7.33–60.14 | 9–36 days | Single dose 5 mg/kg IV | Hospira (1995) |
| Amodiaquine dihydrochloride | 32 ± 3 | 464.8 | 0.069 | 5.2 ± 1.7 h | Single dose 600 mg PO | Winstanley et al. (1987) |
| Chlorprothixene | 430 ± 81 | 315.9 | 1.36 | 25.8 ± 13.6 h | Single dose 100 mg IV | Bagli et al. (1996) |
| Clemastine fumarate | 0.577 ± 0.252 | 460 | 0.0013 | 21.3 ± 11.6 h | Single dose 1.34 mg PO | Schran et al. (1996) |
| Deserpidine | 0.172 | 578.66 | 0.0003 | 42.9 ± 17.8 h | Single dose 0.25 mg PO | Zhang et al. (2009) |
| Duloxetine hydrochloride | 110 | 333.88 | 0.33 | 6.96–14.9 h | 60 mg BID PO | Knadler et al. (2011) |
| Imatinib | 3,395 ± 2,409 | 493.6 | 6.88 | 10–18.9 h | Single dose 600 mg PO | Peng et al. (2005) |
| Loperamide hydrochloride | 2 | 477 | 0.0042 | 9.1–14.4 h | Single dose 2 mg PO | Janssen Pharmaceutica Inc. (1998) |
| Maprotiline hydrochloride | 25 | 313.87 | 0.080 | 45 h | Single dose 75 mg PO | Maguire et al. (1980) |
| a Methdilazine hydrochloride | 332.9 | |||||
| Methotrimeprazine maleate | 3.44 | 444.6 | 0.0077 | 10.8 h | Single dose 25 mg PO | AA Pharma Inc. (2012) |
| a Piperacetazine | 410.6 | |||||
| Remdesivir | 4,420 | 602.58 | 7.34 | 1.05 h | Single dose 225 mg IV | Humeniuk et al. (2020) |
Discontinued drugs. No PK data available.
Cmax: maximum serum/plasma concentration; MW: molecular weight; Elimination T1/2: elimination half life; PO: per os (oral dosing); IV: intravenous.