Table 1 The set of drugs used in the screen, their main targets, and clinical information

Regorafenib

(Stivarga®)

VEGFR_2-3, RET, PDGFR

4.3

approved

160 mg/kg

50.26 mg*h/L [25]; 58.3 mg*h/L [26]

Vemurafenib

(Zelboraf®)

BRAF

32.3

approved

960 mg/kg

380 µg*h/mL (EMEA/H/C/002409)

Vatalanib

VEGFR_1-3

6.3

Phase III

1200 mg

69.2 mg*h/L [27]; 52.9 mg*h/L [28]

Erlotinib

(Tarceva®)

EGFR

1.6

approved

15 mg/kg

15.2 mg*h/L (EMEA/H/C/000618)

AZD-4547

FGFR_1-4, VEGFR₂

0.6

Phase II/III

160 mg

2058_(0-12 h) µg*h/L [29]

Lapatinib

(Tyverb®)

HER2, EGFR

1.6

approved

1250 mg/kg

36.2 µg*h/mL (EMEA/H/C/002532)

Trametinib

(Mekinist®)

MEK

14.4

approved

2 mg/kg

370 ng*h/mL (EMEA/H/C/002643)

Palbociclib

(Ibrance®)

CDK_4-6

29.3

approved

100/125 mg/kg

547.5 ng*h/L [30] (EMEA/H/C/003853)

BEZ-235

PI3K,

mTOR

0.1

Phase II/III

400 mg/kg

741.3 ng*h/L [31]; 1404.4 µg*h/L [32]

Nilotinib

(Tasigna®)

BCR/ABL

8.8

approved

300-400 mg

11,217 ng*h/mL [33] (EMEA/H/C/000798)

Olaparib

(Lynparza®)

PARP

58

approved

400 mg

609 µg*h/mL [34] (EMEA/H/C/003726)