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Table 1 Used drugs, Cmax, AUC levels

From: Cytotoxic drug sensitivity of Epstein-Barr virus transformed lymphoblastoid B-cells

Drug groups

Drug name

Brand name, company

In vitroused concentrations (μg/ml)

Cmax Value (μg/ml)

In vivodose (Cmax)

AUC (μg × h/ml)

In vivodose (AUC)

Reference

anthracyclines

epirubicin

Epirubicin Meda, Meda

0.026–1.66

9

120 mg/m2

2.412

90 mg/m2

(Fogli et al. 2002) [23]

 

daunorubicin

Cerubidin®, Aventis Pharma

0.065–4.166

0.49

0.95 mg/kg in 45 min

1.2786

1.5 mg/kg

(Andersson et al. 1979) [6]

 

doxorubicin

Doxorubicin Teva, Teva

0.026–1.66

0.93

50 mg/m2

0.82464

50 mg/m2

(Toffoli et al. 2004) [24]

epipodophyllotoxin

etoposide

Sigma

0.325–20.833

2.5

53 mg/m2/day

5.06

100 mg/m2/day

(Minami et al. 1995) [25] (Gruber et al.1995) [26]

camptothecins

topotecan

Hycamtin®, GlaxoSmithKline

0.052–3.33

0.0084

2.3 mg/m2/day

0.0196

1.2 mg/m2/day

(Gerrits et al. 1999) [27]

taxanes

paclitaxel

Taxol, Orifarm

0.078–5

3.38

175 mg/m2 by 3 h

13.49

175 mg/m2

(Fogli et al. 2002) [23]

 

docetaxel

Taxotere®, Aventis Pharma

0.52–33.33

2

60 mg/m2

3.326

85 mg/m2

(Rischin et al. 2002) [28]

vinca alkaloids

vincristine

Vincristine Mayne, Mayne Pharma

0.0065–0.416

0.37

1.4 mg/m2

0.182

1.32 mg/m2

(Terashi et al. 2000) [29] (Desai et al. 1982) [30]

 

vinblastine

Velbe®, STADApharm

0.013–0.833

0.005

1.5 mg/m2 by 24 h

0.218

1.7 mg/m2

(Stewart et al. 1983) [31] (Bates et al.) [32]

 

vinorelbine

Navelbine®, Pierre Fabre

0.13–8.33

0.83

200 mg/week

0.899

80 mg/m2/week

(Zhou et al. 1991) [33] (Freyer et al. 2003) [34]

platinum analogs

carboplatin

Carboplatin Mayne, Mayne Pharma

0.13–8.33

0.046

360 mg/m2

348000

360 mg/m2

(Ghazal-Aswad et al. 1996) [35]

 

oxaliplatin

Eloxatin, Sanofi-Synthelabo

0.065–4.166

3.2

130 mg/m2

71.5

130 mg/m2

(Gamelin et al. 1997) [36] (Graham et al. 2000) [37]

antifolate

methotrexate

Methotrexate Pharmacia, Pfizer

0.325–20.833

363

8–12 g/m2

13200000

12 g/m2

(Bacci et al. 2006) [38] (Crews et al. 2004) [39]

purin antagonists

6-mercaptopurine

Sigma

1.085–69.44

2

2.5 mg/kg oral dose

0.2587

85 mg/m2

(Chan et al. 1989) [26]

 

cladribine

Leustatin, Janssen-Cilag

0.013–0.833

0.0356

5 mg/m2

0.1541

5 mg/m2

(Albertioni et al. 1998) [40]

pyrimidine antagonists

fluorouracil

Fluorouracil Mayne, Mayne Pharma

0.65–41.66

55.4

400 mg/m2

11.59

400 mg/m2

(Casale et al. 2004) [41]

 

cytarabine

Cytarabine Pfizer, Pfizer

1.302–83.33

10.8

3 g/m2

523.4

1 g/m2

(DeAngelis et al. 1992) [42] (Gruber et al. 1995) [26]

 

gemcitabine

Gemzar, Orifarm

0.781–50

22.3

1000 mg/m2

9.3

1000 mg/m2

(Fogli et al. 2002) [23]

antitumor antibiotics

bleomycin

Bleomycin Baxter, Baxter

0.39–25*

0.19*

30 IU/day

0.089

8 IU/kg/day

(Broughton et al. 1977) [43] (Peng et al.1980) [44]

 

dactinomycin

Cosmegen®, MSD

0.006–0.416

0.1

1.5 mg/m2

300

1.5 mg/m2

(Veal et al. 2005) [45]

protease inhibitors

bortezomib

Velcade®, Janssen-Cilag

0.013–0.833

0.08

1.45 mg/m2

0.0438

1.45 mg/m2

(Papandreou et al. 2004) [46]

 

MG132

Sigma

0.13–8.33

#

    

alkylating agents

cyclophosphamide

Sendoxan, Baxter

0.52–33.33

37.2

50 mg/kg

367

50 mg/kg

(Xie et al. 2006) [47]

 

ifosphamide

Holoxan®, Baxter

0.52–33.33

56.63

16 g/m2 in 96 h

1827.7

3 g/m2/day

(Wright et al. 1995) [48] (Boddy et al. 1996) [45]

 

chlorambucil

Sigma

1.302–83.33

0.49

0.2 mg/m2

0.883

0.2 mg/m2

(GlaxoSmithKline Research Triangle Park) [49]

 

streptozotocin

Sigma

0.65–41.66

¤

    

miscellaneous

asparaginase

Asparaginase Medac, Medac

0.065–4.166*

4.48*

10000 IU/m2

0.943

30000 IU/m2

(Ho et al. 1981) [50] (Ylikangas et al. 2002) [51]

 

hydroxyurea

Sigma

0.65–41.66

21

18 mg/kg

82.49

15 mg/kg

(Gwilt et al. 2003) [52] (Yan et al. 2005) [46]

 

prednisolone

Di-Adreson F Aquosum, Organon

1.56–100

0.325

1 mg/kg/day

1.33

1 mg/kg/day

(Rostin et al. 1990) [53]

  1. Cmax: maximum plasma level after administration of the clinical dose of the drug
  2. *In case of bleomycin and asparaginase concentrations are in IU/ml
  3. AUC: area under curve
  4. #: not used in the clinical practice
  5. ¤: no data is available