Table 2.

Key human pharmacokinetic parameters for small-molecule prodrugs and their active metabolites approved for oncology indications

Generic nameBrand nameDoseDose unitRouteInfusionCmax (μmol/L)Cmax (ng/mL)AUC (ng•hr/mL)Tmax (hr)T1/2 (hr)Protein binding
Abiraterone acetateZytiga1,000mgPOBLOQBLOQ
Abirateronea(Zytiga)As abovePO0.6472261,17312>99%
Estramustine phosphateEmcyt2,000mg/m2IV60 min797414,700889,8842.5
Estramustinea(Emcyt)As aboveIV10.44,42037,60599
Estramustronea(Emcyt)As aboveIV15.66,620211,351129
FloxuridineFUDR30mg/kgIV8 h1.052591,3650.22
5-FUa(FUDR)As above0.88115
Fludarabine phosphateFludara25mg/m2IV30 minBLOQBLOQ19%–29%
2-F-araAa(Fludara)As aboveIV3.008083,28511.3
IrinotecanCamptosar340mg/m2IV90 min5.783,39220,60411.730%–68%
SN-38a(Camptosar)As aboveIV0.143564742195%
Irinotecan (liposomal)Onivyde70mg/m2IV90 min63.437,2001,364,00025.8<0.44%
SN-38 (liposomal)a(Onivyde)As aboveIV0.0145.462067.895%
Lomustine (CCNU)Gleostine130mg/m2POBLOQBLOQ50%
cis+trans 4-OH-CCNUa(Gleostine)As abovePO3.398473,4002–41.8
NelarabineArranon1,500mg/m2IV2 h16.85,0004,4000.3<25%
Ara-Ga(Arranon)As aboveIV11131,400162,0003.2<25%
TemozolomideTemodar150mg/m2IV90 min37.67,30024,6001.01.815%
MTICa(Temodar)As aboveIV1.64276891
Testosterone enanthateDelatestryl200mgIMn.d.n.d.
Testosteronea(Delatestryl)As aboveIM0.051155598%
ThiotepaThioplex80mgIVPush9.661,8284,1272.310%
TEPAa(Thioplex)As aboveIV2.043537,45215.7
  • Abbreviations: BLOQ, below the limit of quantitation; hr, hours; IM, intramuscular; IV, intravenous; min, minutes; n.d., not determined; PO, per os; Tmax: time post-dose of maximum plasma concentration; T1/2: plasma half-life.

  • aKey human pharmacokinetic parameters for active metabolites (of small-molecule prodrugs) approved for oncology indications.