Table 1.

Key human pharmacokinetic parameters for small-molecule drugs approved for oncology indications

Generic nameBrand nameDoseDose unitRouteInfusionCmax (μmol/L)Cmax (ng/mL)AUC (ng•hr/mL)Tmax (hr)T1/2 (hr)Protein binding
AbarelixPlenaxis100mgIM0.03143.412,00072316.896%–99%
AfatinibGilotrif40mgPO0.052253244.026.995%
AlectinibAlecensa600mgPO1.386657,4304.033>99%
AlfuzosinUroXatral10mgPO0.035141948.01082%–90%
AllopurinolZyloprim300mgPO14.31,9404,8141.41.4Negligible
AltretamineHexalen200mgPO3.767900.5–34.7–10.294%
AmifostineEthyol200mg/m2IV7.5 min10522,4724,2380.26Negligible
AminoglutethimideCytadren500mgPO25.45,9001.512.521%–25%
Aminolevulinic acidLevulan Kerastick100mgIV*1 min12916,90013,7000.83
AnastrozoleArimidex1mgPO0.0351053641.340%
Arsenic trioxideTrisenox0.1mg/kgIV2 h0.910180*75%
AxitinibInlyta5mgPO0.163634661.83.1>99%
AzacitidineVidaza75mg/m2SC3.077509600.500.68
AzacitidineVidaza75mg/m2IV10–40 min11.32,7501,0440.36
BelinostatBeleodaq1,000mg/m2IV30 min13442,65729,005194%
BendamustineTreanda120mg/m2IV60 min16.35,84013,6350.794%–96%
BexaroteneTargretin300mg/m2PO3.391,1805,9802.53.4>99%
BicalutamideCasodex50mgPO1.78768230,8383113996%
BleomycinBlenoxane15mg/m2IVBolus7061,000,0004.99E+0641%
BortezomibVelcade1.3mg/m2IVBolus0.3121201960.0848.783%
BosutinibBosulif500mgPO0.3772003,6504–622.596%
BusulfanBusulflex0.8mg/kgIV2 h4.961,2224,79032%
CabazitaxelJevtana25mg/m2IV1 h0.2702269911.09589%–92%
CabozantinibCometriq140mgPO4.612,31041,6002–55599.7%
CapecitabineXeloda1,250mg/m2PO21.17,5708,4500.820.43Approx 35%
CarboplatinParaplatin400mg/m2IV30 min13550,00083,3330.5030%
CarfilzomibKyprolis27mg/m2IV5 min5.884,232379<197%
CarmustineBiCNU600mg/m2IV2 h19.44,15080%
CeritinibZykadia750mgPO1.2167414,0005.04197%
ChlorambucilLeukeran0.2mg/kgPO1.624928830.831.399%
CisplatinPlatinol80mg/m2IV1 h14.44,32142,9210.44n/a*
CladribineLeustatin0.09mg/kg/dayIV24 h0.0205.720%
CladribineLeustatin0.12mg/kgIV2 h0.168485.420%
ClofarabineClolar40mg/m2IV2 h0.7442269314.947%
CobimetinibCotellic60mgPO0.5142734,3402.44495%
CrizotinibXalkori250mgPO0.9134113,8804.034.991%
CyclophosphamideCytoxan600mg/m2IVBolus12833,408226,0823–1220%
CytarabineCytosar-U3,000mg/m2IV3 h54.413,21938,9283.8213%
DabrafenibTafinlar150mgPO4.862,52710,7512.04.899.7%
DacarbazineDTIC-Dome200mg/m2IV30 min34.46,2704,8605<5%
DactinomycinCosmegen0.70–1.50mg/m2IVBolus0.0202544.50.2514–435%
DasatinibSprycel100mgPO0.2641294782.06.296%
DaunorubicinDaunoxome50mg/m2IV1 h0.3101755751197%
DecitabineDacogen15mg/m2IV3 h0.323741632.50.62<1%
DegarelixFirmagon240mgSC0.0162625,2964890%
DexrazoxaneZinecard500mg/m2IV15 min13636,5002.5<2%
DocetaxelTaxotere100mg/m2IV1 h5.474,4205,9004197%
DoxorubicinAdriamycin60mg/m2IV5 min6.733,6601,85014.275%
Doxorubicin (liposomal)Doxil20mg/m2IV30 min15.348,340590,0005570%
EnzalutamideXtandi160mgPO35.716,6001.05.898%
EpirubicinEllence120mg/m2IV10 min16.69,0003,40033.777%
Eribulin mesylateHalaven1.4mg/m2IV2–5 min0.5083717570.1740.449%–65%
ErlotinibTarceva150mgPO3.151,23818.65.524.493%
EtoposideVePesid100mg/m2IV60 min33.419,66029,8003.6297%
EverolimusAfinitor10mgPO0.064615141.074%
ExemestaneAromasin25mgPO0.0277.9521.2–2.92490%
Fluorouracil (5-FU)Adrucil400mg/m2IVPush42655,40011,59010%
FlutamideEulexin250mgPO0.4091131.37.894%–96%
FulvestrantFaslodex500mgIM0.0412511,40096099%
GefitinibIressa250mgPO0.3561595,1153.050.590%
GemcitabineGemzar1,250mg/m2IV30 min89.323,50012,5000.23Negligible
Goserelin acetateZoladex10.8mgSC0.0078.91.827%
HydroxyureaDroxia2,000mgPO79560,441299,1811.23.32
IbrutinibImbruvica560mgPO0.2771221,2632.09.298%
IdarubicinIdamycin15mg/m2IV5 min0.1236117321.897%
IdelalisibZydelig150mgPO5.182,1529,5991.85.7584%
IfosfamideIfex3,000mg/m2IV3 h431112,5342,448,8574.1Negligible
ImatinibGleevec600mgPO7.503,70048,8001795%
ImiquimodAldara75mgTopical0.00561.40.029190%–95%
IngenolPicato0.5mgTopicalBLOQBLOQ>99%
IxabepiloneIxempra40mg/m2IV3 h0.4972522,1433567%–77%
IxazomibNinlaro4mgPO0.118611,1601.022899%
LanreotideSomatuline Depot120mgSC0.0077.7
LapatinibTykerb1,250mgPO4.182,43036,2004.014.2>99%
LenalidomideRevlimid25mgPO1.744513,8201.55.330%
LenvatinibLenvima24mgPO0.7613253,0102.02898%–99%
LetrozoleFemara2.5mgPO0.4061162,2461.560%
Leuprolide acetateEligard30mgSC0.1241503.343%–49%
MechlorethamineMustargen0.4mg/kgIVBolusBLOQBLOQ
Megestrol acetateMegace800mgPO1.9675310,4765.0
MelphalanAlkeran20mg/m2IV15–20 min9.172,8001.2560%–90%
MercaptopurinePurinethol75mg/m2PO0.590902741.319%
MercaptopurinePurixan50mgPO0.62595136219%
MethotrexateAbitrexate30mgPO1.315942,4661.22.950%
MethoxsalenUvadex; 8-MOP40mgPO0.6241354402.0290%
Mitomycin CMitozytrex15mg/m2IV30 min2.187296910.8124%
MitoxantroneNovantrone12mg/m2IV30 min0.7153182981778%
Nab-paclitaxelAbraxane260mg/m2IV30 min21.918,74020,3242789–98%
NilotinibTasigna400mgPO0.84044511,9004.01398%
NilutamideNilandron150mgPO2.8490039,0002.85680%–84%
OctreotideSandostatin0.1mgSC0.00384.012.40.642.2565%
OlaparibLynparza400mgPO13.15,70058,0001.311.982%
OmacetaxineSynribo1.25mg/m2SC0.046251360.55750%
OsimertinibTagrisso80mgPO0.126633,1326.06499%
OxaliplatinEloxatin110mg/m2IV2 h4.961,9704,9901.86>90%
PaclitaxelTaxol175mg/m2IV3 h4.273,65015,00720.289%–98%
PalbociclibIbrance125mgPO0.101451,4276.022.285%
PamidronateAredia90mgIV4 h11.12,61017,1204.0
PanobinostatFarydak20mgPO0.082292801.015.590%
PazopanibVotrient800mgPO13358,1001,037,0002–430.9>99%
PemetrexedAlimta500mg/m2IV10 min306131,000188,0004.481%
PentostatinNipent4mg/m2IV15 min1.824891,2325.34%
PlerixaforMozobil0.24mg/kgSC1.849264,7410.505.158%
PomalidomidePomalyst4mgPO0.274754002–39.512%–44%
PonatinibIclusig45mgPO0.137731,25324>99%
PorfimerPhotofrin2mg/kgIV3–5 min33.940,0002,400,00041590%
PralatrexateFolotyn40mg/m2IV5 min10.34,9004,9001.867%
PrednisoneDeltasone50mgPO0.14552Extensive
ProcarbazineMatulane300mgPO3.136922170.210.154
RaloxifeneEvista60mgPO0.00110.527.2 (ng•hr/mL)/(mg/kg)27.795%
RegorafenibStivarga160mgPO8.083,90058,3004.02899.5%
RomidepsinIstodax14mg/m2IV4 h0.6973771,549392%–94%
RucaparibRubraca600mgPO6.0001,94016,9001.91770%
RuxolitinibJakafi25mgPO1.093359790.632.397%
SonidegibOdomzo200mgPO2.121,03022,0002–4672>97%
SorafenibNexavar400mgPO20.19,350107,0002.523.899.5%
StreptozocinZanosar1,500mg/m2IVPush1,438381,40072,1500.22
Sunitinib malateSutent50mgPO0.181721,2968.541–8695%
Tamoxifen citrateNolvadex20mgPO0.108405.0120–168>99%
TegafurUtefos50mg/m2PO19.03,80326,4801.07.88
TemsirolimusTorisel25mgIV30–60 min0.5685851,6271787%
TeniposideVumon300–750mg/m2IV72 h23.115,200>99%
ThalidomideThalomid200mgPO8.912,30023,3005.84.1255% (+)-(R); 66% (-)-(S)
ThioguanineTabloid40mg/m2PO0.313520.09791.5
TopotecanHycamtin2.3mg/m2PO0.0156.322.73.4935%
ToremifeneFareston120mgPO4.561,850115,1002.956.5>99.5%
TrabectedinYondelis1.5mg/m2IV24 hr0.00241.856.817597%
TrametinibMekinist2mgPO0.0211369.72.03.9–4.897%
TretinoinVesanoid45mg/m2PO1.153476822.2>95%
TriptorelinTrelstar Depot22.5mgIM0.034441–30%
ValrubicinValstar800mgIntra-cisternal0.011856.42–6>99%
VandetanibCaprelsa300mgPO2.161,02520,460545690%
VemurafenibZelboraf960mgPO12762,000601,0003.057>99%
VenetoclaxVenclexta400mgPO4.4821,00032,8005–826>99%
VinblastineVelban1**mg/m2IVBolus0.03528450.1226.2098%–99%
VincristineVincasar PFS1mg/m2IVBolus0.0075.475%
Vincristine (liposomal)Marqibo2.25mg/m2IV60 min1.4791,22014,5667.6675%
VinorelbineNavelbine25mg/m2IV20 min0.81163258521.4089%
VismodegibErivedge150mgPO33.914,2822,283,44696>99%
VorinostatZolinza400mgPO1.203171,1101.5271%
Zoledronic acidZometa4mgIV15 min0.97126442014633%–40%
  • NOTE: A single (*) or double (**) asterisk refers readers to notes in Supplementary Table S1.

  • Abbreviations: Approx, approximately; BLOQ, below the limit of quantitation; hr, hours; IM, intramuscular; IV, intravenous; min, minute(s); n/a, not applicable; PO, per os; SC, subcutaneous; Tmax: time post-dose of maximum plasma concentration; T1/2: plasma half-life.