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. Author manuscript; available in PMC: 2018 Jul 15.
Published in final edited form as: Clin Cancer Res. 2017 Mar 31;23(14):3489–3498. doi: 10.1158/1078-0432.CCR-16-3083

Table 4.

Key human pharmacokinetic parameters for selected small-molecule drugs NOT approved for oncology indications

Generic Name Brand Name Dose Dose Unit Route infusion Cmax (uM) Cmax (ng/ml) AUC (ng•hr/ml) Tmax (hr) T1/2 (hr) Protein binding
Alfuzosin UroXatral 10 mg PO - 0.035 14 194 8.0 10 82–90%
Aminoglutethimide Cytadren 500 mg PO - 25.4 5900 - 1.5 12.5 21–25%
Celecoxib Celebrex 400 mg PO - 4.60 1752 13049 - 8.8 97%
Chloroquine Aralen 750 mg PO - 0.725 232 8385 3.7 - 55%
Dutasteride Avodart 0.5 mg PO - 0.076 40 - 2–3 840 99%
Finasteride Proscar 5 mg PO - 0.124 46 389 1.8 6 90%
Histrelin acetate Supprelin 0.0567 mg/day SC 0.00083 1.1 2318 12 - 70%
Hydroxychloroquine Plaquenil 200 mg PO - 0.35000 117.4 12015 3.8 564 45%
Ibandronate Boniva 6 mg IV 30 min 1.02 327 942 0.63 12 86%
Medroxyprogesterone acetate Provera 20 mg PO - 0.0026 1.0 6.95 2.7 12.1 90%
Metformin Glucophage 1500 mg PO - 24.0 3100 18400 1.5 5.98 negligible
Quinacrine Acrichine 100 mg PO - 0.300 120 - - - 80–90%
Sildenafil Viagra 100 mg PO - 0.794 377 1295 1.0 2.76 96%
Sirolimus (Rapamycin) Rapamune 2 mg PO - 0.016 15 230 3.5 62 92%
Tacrolimus Prograf 5 mg PO - 0.037 30 243 1.6 34.8 99%
Zalcitabine (Dideoxycytidine) Hivid 1.5 mg PO - 0.119 25 72 0.80 - <4%

Abbreviations: Cmax: maximum plasma concentration; AUC: Area Under the time-plasma Concentration curve; : Tmax: Time post-dose of maximum plasma concentration; : T1/2: Plasma half-life