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Details

Stereochemistry ACHIRAL
Molecular Formula C25H27FN4O3
Molecular Weight 450.5053
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CEDIRANIB

SMILES

COC1=CC2=C(C=C1OCCCN3CCCC3)N=CN=C2OC4=CC=C5NC(C)=CC5=C4F

InChI

InChIKey=XXJWYDDUDKYVKI-UHFFFAOYSA-N
InChI=1S/C25H27FN4O3/c1-16-12-17-19(29-16)6-7-21(24(17)26)33-25-18-13-22(31-2)23(14-20(18)27-15-28-25)32-11-5-10-30-8-3-4-9-30/h6-7,12-15,29H,3-5,8-11H2,1-2H3

HIDE SMILES / InChI

Molecular Formula C25H27FN4O3
Molecular Weight 450.5053
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Cediranib (AZD-2171) is a VEGFR-2 kinase inhibitor which was developed by AstraZeneca for the treatment of cancer. The drug reached the final stage of approval by European Medicines Agency in 2008 under the name Zemfirza (it was recommended to be taken in combination with platinum-based chemotherapy), however on 19 September 2016 AstraZeneca decided to withdraw the Marketing Authorisation Application.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.02 ng/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.9 ng/mL
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.1 ng/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.02 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
24.8 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
45.7 ng/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
73.1 ng/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
96.9 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
217 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.39 ng/mL
0.5 mg 1 times / day steady-state, oral
dose: 0.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.79 ng/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9.37 ng/mL
2.5 mg 1 times / day steady-state, oral
dose: 2.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
13.4 ng/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
42.8 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
66.6 ng/mL
20 mg 1 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
69.6 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
73.9 ng/mL
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
170 ng/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.36 ng/mL
1 mg 1 times / day multiple, oral
dose: 1 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3.02 ng/mL
2.5 mg 1 times / day multiple, oral
dose: 2.5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
6.78 ng/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
25.8 ng/mL
10 mg 1 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
25.7 ng/mL
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
52.6 ng/mL
30 mg 1 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.33 ng/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5.28 ng/mL
2.5 mg 1 times / day steady-state, oral
dose: 2.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
17.3 ng/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
18.8 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
40.4 ng/mL
20 mg 1 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
118 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
113 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
115 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
138 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
47 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
96 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
64.2 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
88.9 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
72 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
42.2 ng/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
87.3 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
127.9 ng/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
15.6 ng × h/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
32.3 ng × h/mL
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
87.1 ng × h/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
117 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
457 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
865 ng × h/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1190 ng × h/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2190 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3590 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
17.3 ng × h/mL
0.5 mg 1 times / day steady-state, oral
dose: 0.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
24.3 ng × h/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
102 ng × h/mL
2.5 mg 1 times / day steady-state, oral
dose: 2.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
196 ng × h/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
502 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
774 ng × h/mL
20 mg 1 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
741 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1060 ng × h/mL
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1860 ng × h/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
15.5 ng × h/mL
1 mg 1 times / day multiple, oral
dose: 1 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
34.9 ng × h/mL
2.5 mg 1 times / day multiple, oral
dose: 2.5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
97.4 ng × h/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
302 ng × h/mL
10 mg 1 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
309 ng × h/mL
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
565 ng × h/mL
30 mg 1 times / day multiple, oral
dose: 30 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
25.1 ng × h/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
95.3 ng × h/mL
2.5 mg 1 times / day steady-state, oral
dose: 2.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
226 ng × h/mL
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
316 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
559 ng × h/mL
20 mg 1 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2005 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2238 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1857 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3427 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1248 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1213 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
877 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1106 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
958.1 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
805 ng × h/mL
30 mg 1 times / day steady-state, oral
dose: 30 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1920 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
2392 ng × h/mL
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
16.6 h
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
22.2 h
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
16.5 h
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.6 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
18.8 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
21.7 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
19.7 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.7 h
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
27.2 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
19.7 h
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
25.6 h
45 mg single, oral
dose: 45 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CEDIRANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
4.6%
CEDIRANIB plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
45 mg 1 times / day multiple, oral
Highest studied dose
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
DLT: Proteinuria, Diarrhea...
Dose limiting toxicities:
Proteinuria (33.3%)
Diarrhea (16.7%)
Thrombocytopenia (16.7%)
Sources:
30 mg 1 times / day multiple, oral
MTD
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
12 mg/m2 1 times / day multiple, oral
MTD
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
DLT: Diarrhea...
Dose limiting toxicities:
Diarrhea (grade 3, 16.7%)
Sources:
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
DLT: Lethargy, Nausea...
Dose limiting toxicities:
Lethargy (grade 3, 50%)
Nausea (grade 3, 50%)
Vomiting (grade 3, 50%)
Hypertension (grade 3, 50%)
QT prolonged (grade 3, 50%)
Sources:
17 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 17 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 17 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
DLT: Nausea, anorexi...
Dose limiting toxicities:
Nausea (grade 3, 25%)
anorexi (grade 2, 25%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhea 16.7%
DLT
45 mg 1 times / day multiple, oral
Highest studied dose
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Thrombocytopenia 16.7%
DLT
45 mg 1 times / day multiple, oral
Highest studied dose
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Proteinuria 33.3%
DLT
45 mg 1 times / day multiple, oral
Highest studied dose
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Diarrhea grade 3, 16.7%
DLT
12 mg/m2 1 times / day multiple, oral
MTD
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
Nausea grade 3, 50%
DLT
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
Vomiting grade 3, 50%
DLT
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
Hypertension grade 3, 50%
DLT, Disc. AE
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
Lethargy grade 3, 50%
DLT, Disc. AE
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
QT prolonged grade 3, 50%
DLT, Disc. AE
12 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 12 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
anorexi grade 2, 25%
DLT
17 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 17 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 17 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
Nausea grade 3, 25%
DLT
17 mg/m2 1 times / day multiple, oral
Studied dose
Dose: 17 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 17 mg/m2, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT
Sex: M+F
Food Status: UNKNOWN
Sources:
PubMed

PubMed

TitleDatePubMed
Acoustic radiation force and optical spectroscopy for assessing tumor vessel normalization during anti-angiogenic therapy.
2009
Current available therapies and future directions in the treatment of malignant gliomas.
2009
PDGF-C induces maturation of blood vessels in a model of glioblastoma and attenuates the response to anti-VEGF treatment.
2009
Noninvasive imaging of the functional effects of anti-VEGF therapy on tumor cell extravasation and regional blood volume in an experimental brain metastasis model.
2009
VEGF inhibitors in the treatment of cerebral edema in patients with brain cancer.
2009 Apr
Antitumor and antiangiogenic activity of cediranib in a preclinical model of renal cell carcinoma.
2009 Dec
Increase in tumour permeability following TGF-beta type I receptor-inhibitor treatment observed by dynamic contrast-enhanced MRI.
2009 Dec 1
Concerns about anti-angiogenic treatment in patients with glioblastoma multiforme.
2009 Dec 16
Effective strategies for management of hypertension after vascular endothelial growth factor signaling inhibition therapy: results from a phase II randomized, factorial, double-blind study of Cediranib in patients with advanced solid tumors.
2009 Dec 20
Phase I study of cediranib in combination with oxaliplatin and infusional 5-Fluorouracil in patients with advanced colorectal cancer.
2009 Feb 15
Phase III trial of FOLFOX plus bevacizumab or cediranib (AZD2171) as first-line treatment of patients with metastatic colorectal cancer: HORIZON III.
2009 Jan
Investigational agents in the management of non-small cell lung cancer.
2009 Jul
A "vascular normalization index" as potential mechanistic biomarker to predict survival after a single dose of cediranib in recurrent glioblastoma patients.
2009 Jul 1
VEGF inhibitors and prostate cancer therapy.
2009 Jun
Treatment in advanced colorectal cancer: what, when and how?
2009 Jun 2
Gateways to clinical trials.
2009 Mar
A phase I and pharmacokinetic study of daily oral cediranib, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with cisplatin and gemcitabine in patients with advanced non-small cell lung cancer: a study of the National Cancer Institute of Canada Clinical Trials Group.
2009 Mar
The vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor cediranib (Recentin; AZD2171) inhibits endothelial cell function and growth of human renal tumor xenografts.
2009 Mar 1
[Second-line treatment using novel chemotherapeutic and biologic agents].
2009 May
Current status of cediranib: the rapid development of a novel anti-angiogenic therapy.
2009 May
Edema control by cediranib, a vascular endothelial growth factor receptor-targeted kinase inhibitor, prolongs survival despite persistent brain tumor growth in mice.
2009 May 20
Gateways to clinical trials.
2009 Nov
Phase I, dose escalation and pharmacokinetic study of cediranib (RECENTIN), a highly potent and selective VEGFR signaling inhibitor, in Japanese patients with advanced solid tumors.
2009 Nov
Cediranib, an oral inhibitor of vascular endothelial growth factor receptor kinases, is an active drug in recurrent epithelial ovarian, fallopian tube, and peritoneal cancer.
2009 Nov 20
Cediranib: profile of a novel anti-angiogenic agent in patients with glioblastoma.
2009 Oct
Cediranib (recentin, AZD2171) reverses ABCB1- and ABCC1-mediated multidrug resistance by inhibition of their transport function.
2009 Oct
Targeting vascular endothelial growth factor receptor-1 and -3 with cediranib (AZD2171): effects on migration and invasion of gastrointestinal cancer cell lines.
2009 Sep
VEGFR1 activity modulates myeloid cell infiltration in growing lung metastases but is not required for spontaneous metastasis formation.
2009 Sep 18
DCE-MRI assessment of the effect of vandetanib on tumor vasculature in patients with advanced colorectal cancer and liver metastases: a randomized phase I study.
2009 Sep 21
Angiogenesis inhibition in prostate cancer: current uses and future promises.
2010
Targeted therapy in ovarian cancer.
2010
Targeted therapies in epithelial ovarian cancer.
2010
Antivascular therapy for epithelial ovarian cancer.
2010
A current review of targeted therapeutics for ovarian cancer.
2010
An open-label, Phase I study of cediranib (RECENTIN) in patients with acute myeloid leukemia.
2010 Feb
Treatment options for small cell lung cancer - do we have more choice?
2010 Feb 16
CT response assessment combining reduction in both size and arterial phase density correlates with time to progression in metastatic renal cancer patients treated with targeted therapies.
2010 Jan
Randomized, double-blind trial of carboplatin and paclitaxel with either daily oral cediranib or placebo in advanced non-small-cell lung cancer: NCIC clinical trials group BR24 study.
2010 Jan 1
Changes in vascular permeability and expression of different angiogenic factors following anti-angiogenic treatment in rat glioma.
2010 Jan 15
CD133+ circulating haematopoietic progenitor cells predict for response to sorafenib plus erlotinib in non-small cell lung cancer patients.
2010 Jan 19
Sorafenib in patients with advanced biliary tract carcinoma: a phase II trial.
2010 Jan 5
Recent advances and future directions in the management of metastatic renal cell carcinoma.
2010 Mar
Tumor invasion after treatment of glioblastoma with bevacizumab: radiographic and pathologic correlation in humans and mice.
2010 Mar
Tyrosine kinase inhibitors to treat liver cancer.
2010 Mar
Phase I evaluation of cediranib, a selective VEGFR signalling inhibitor, in combination with gefitinib in patients with advanced tumours.
2010 Mar
Rapid development of hypertension and proteinuria with cediranib, an oral vascular endothelial growth factor receptor inhibitor.
2010 Mar
Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?
2010 Mar
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.
2010 May 5
Sunitinib in combination with docetaxel in patients with advanced solid tumors: a phase I dose-escalation study.
2010 Sep
Molecularly targeted therapy in hepatocellular carcinoma.
2010 Sep 1
Patents

Sample Use Guides

The recommended dose is 20 mg taken orally, once daily.
Route of Administration: Oral
NCI-H526 cells were treated with Cediranib for 72 hours (0.001 nM, 0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM). Cediranib inhibited SCF-stimulated proliferation of cells with an IC50 value of 0.013 nmol/L.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:28:13 GMT 2025
Edited
by admin
on Mon Mar 31 18:28:13 GMT 2025
Record UNII
NQU9IPY4K9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AZD-2171
Preferred Name English
CEDIRANIB
INN   MART.   USAN   WHO-DD  
INN   USAN  
Official Name English
CEDIRANIB [USAN]
Common Name English
cediranib [INN]
Common Name English
Cediranib [WHO-DD]
Common Name English
Quinazoline, 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-
Systematic Name English
4-((4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY)-6-METHOXY-7-(3-PYRROLIDIN-1-YLPROPOXY)QUINAZOLINE
Systematic Name English
CEDIRANIB [MART.]
Common Name English
AZD2171
Code English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
NCI_THESAURUS C1742
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
FDA ORPHAN DRUG 310510
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
WHO-ATC L01XE32
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
EU-Orphan Drug EU/3/14/1303
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
Code System Code Type Description
CAS
288383-20-0
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
INN
8764
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
USAN
TT-141
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
NCI_THESAURUS
C80867
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
EPA CompTox
DTXSID10183035
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
FDA UNII
NQU9IPY4K9
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
EVMPD
SUB26524
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
SMS_ID
100000090090
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
DRUG BANK
DB04849
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
ChEMBL
CHEMBL491473
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
WIKIPEDIA
CEDIRANIB
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
PUBCHEM
9933475
Created by admin on Mon Mar 31 18:28:13 GMT 2025 , Edited by admin on Mon Mar 31 18:28:13 GMT 2025
PRIMARY
Related Record Type Details
ACTIVE MOIETY