CEDIRANIB MALEATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H27FN4O3.C4H4O4
Molecular Weight	566.5774
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.COC1=CC2=C(C=C1OCCCN3CCCC3)N=CN=C2OC4=CC=C5NC(C)=CC5=C4F

InChI

InChIKey=JRMGHBVACUJCRP-BTJKTKAUSA-N

InChI=1S/C25H27FN4O3.C4H4O4/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;5-3(6)1-2-4(7)8/h6-7,12-15,29H,3-5,8-11H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-

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

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Medicine_QA/2016/10/WC500214183.pdf | https://www.ncbi.nlm.nih.gov/pubmed/15899831

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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Vascular endothelial growth factor receptor 2 112 Target ID: CHEMBL279 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15899831	Inhibitor 8504		1.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Ovarian cancer 160 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27025186	Primary	Phase III 665	Unknown Approved Use Unknown
Fallopian tube cancer 17 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25895616	Primary	Phase III 665	Unknown Approved Use Unknown
Primary peritoneal cancer 3 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25895616	Primary	Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.02 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21120480/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21120480/	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

Value	Dose	Analyte	Population
15.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17458505/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21120480/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21120480/	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

T_1/2

Value	Dose	Analyte	Population
16.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/ \| https://pubmed.ncbi.nlm.nih.gov/17634482/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23197081/	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
4.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27943222/			CEDIRANIB plasma	Homo sapiens

Doses

Dose	Population	Adverse 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: https://pubmed.ncbi.nlm.nih.gov/19308410/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/	DLT: Proteinuria, Diarrhea... Dose limiting toxicities: Proteinuria (33.3%) Diarrhea (16.7%) Thrombocytopenia (16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/
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: https://pubmed.ncbi.nlm.nih.gov/19308410/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/	Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/	DLT: Diarrhea... Dose limiting toxicities: Diarrhea (grade 3, 16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/	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: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/	DLT: Nausea, anorexi... Dose limiting toxicities: Nausea (grade 3, 25%) anorexi (grade 2, 25%) Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/

AEs

AE	Significance	Dose	Population
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: https://pubmed.ncbi.nlm.nih.gov/19308410/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/
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: https://pubmed.ncbi.nlm.nih.gov/19308410/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/
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: https://pubmed.ncbi.nlm.nih.gov/19308410/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19308410/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/
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: https://pubmed.ncbi.nlm.nih.gov/21060028/	unhealthy, CHILD\|ADOLESCENT Health Status: unhealthy Age Group: CHILD\|ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21060028/

PubMed

Title	Date	PubMed
Molecularly targeted therapy in hepatocellular carcinoma.	2010-09-01	20371362
Sunitinib in combination with docetaxel in patients with advanced solid tumors: a phase I dose-escalation study.	2010-09	20043166
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.	2010-05-05	20351338
Recent advances and future directions in the management of metastatic renal cell carcinoma.	2010-03	20184547
Tumor invasion after treatment of glioblastoma with bevacizumab: radiographic and pathologic correlation in humans and mice.	2010-03	20167811
Tyrosine kinase inhibitors to treat liver cancer.	2010-03	20128706
Phase I evaluation of cediranib, a selective VEGFR signalling inhibitor, in combination with gefitinib in patients with advanced tumours.	2010-03	20061136
Rapid development of hypertension and proteinuria with cediranib, an oral vascular endothelial growth factor receptor inhibitor.	2010-03	20056761
Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?	2010-03	20012482
Treatment options for small cell lung cancer - do we have more choice?	2010-02-16	20104223
An open-label, Phase I study of cediranib (RECENTIN) in patients with acute myeloid leukemia.	2010-02	19674789
CD133+ circulating haematopoietic progenitor cells predict for response to sorafenib plus erlotinib in non-small cell lung cancer patients.	2010-01-19	20010948
Changes in vascular permeability and expression of different angiogenic factors following anti-angiogenic treatment in rat glioma.	2010-01-15	20090952
Sorafenib in patients with advanced biliary tract carcinoma: a phase II trial.	2010-01-05	19935794
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.	2010-01-01	19917841
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.	2010-01	20009542
Angiogenesis inhibition in prostate cancer: current uses and future promises.	2010	20169138
Targeted therapy in ovarian cancer.	2010	20130818
Targeted therapies in epithelial ovarian cancer.	2010	20111741
Antivascular therapy for epithelial ovarian cancer.	2010	20072701
A current review of targeted therapeutics for ovarian cancer.	2010	20069122
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.	2009-12-20	19901116
Concerns about anti-angiogenic treatment in patients with glioblastoma multiforme.	2009-12-16	20015387
Increase in tumour permeability following TGF-beta type I receptor-inhibitor treatment observed by dynamic contrast-enhanced MRI.	2009-12-01	19888220
Antitumor and antiangiogenic activity of cediranib in a preclinical model of renal cell carcinoma.	2009-12	20044618
Cediranib, an oral inhibitor of vascular endothelial growth factor receptor kinases, is an active drug in recurrent epithelial ovarian, fallopian tube, and peritoneal cancer.	2009-11-20	19826113
Gateways to clinical trials.	2009-11	20094643
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.	2009-11	19308410
Cediranib: profile of a novel anti-angiogenic agent in patients with glioblastoma.	2009-10	19671039
Cediranib (recentin, AZD2171) reverses ABCB1- and ABCC1-mediated multidrug resistance by inhibition of their transport function.	2009-10	19255759
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.	2009-09-21	19946413
VEGFR1 activity modulates myeloid cell infiltration in growing lung metastases but is not required for spontaneous metastasis formation.	2009-09-18	19763275
Targeting vascular endothelial growth factor receptor-1 and -3 with cediranib (AZD2171): effects on migration and invasion of gastrointestinal cancer cell lines.	2009-09	19755510
A "vascular normalization index" as potential mechanistic biomarker to predict survival after a single dose of cediranib in recurrent glioblastoma patients.	2009-07-01	19549889
Investigational agents in the management of non-small cell lung cancer.	2009-07	19508832
Treatment in advanced colorectal cancer: what, when and how?	2009-06-02	19436303
VEGF inhibitors and prostate cancer therapy.	2009-06	19617926
Edema control by cediranib, a vascular endothelial growth factor receptor-targeted kinase inhibitor, prolongs survival despite persistent brain tumor growth in mice.	2009-05-20	19332720
[Second-line treatment using novel chemotherapeutic and biologic agents].	2009-05	19461172
Current status of cediranib: the rapid development of a novel anti-angiogenic therapy.	2009-05	19450171
VEGF inhibitors in the treatment of cerebral edema in patients with brain cancer.	2009-04	19333229
The vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor cediranib (Recentin; AZD2171) inhibits endothelial cell function and growth of human renal tumor xenografts.	2009-03-01	19215823
Gateways to clinical trials.	2009-03	19455266
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.	2009-03	19091548
Phase I study of cediranib in combination with oxaliplatin and infusional 5-Fluorouracil in patients with advanced colorectal cancer.	2009-02-15	19228749
Phase III trial of FOLFOX plus bevacizumab or cediranib (AZD2171) as first-line treatment of patients with metastatic colorectal cancer: HORIZON III.	2009-01	19203899
Acoustic radiation force and optical spectroscopy for assessing tumor vessel normalization during anti-angiogenic therapy.	2009	19964240
Current available therapies and future directions in the treatment of malignant gliomas.	2009	19707392
PDGF-C induces maturation of blood vessels in a model of glioblastoma and attenuates the response to anti-VEGF treatment.	2009	19352490
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	19277878

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose is 20 mg taken orally, once daily.

Route of Administration: Oral

In Vitro Use Guide

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 18:13:32 GMT 2025` Edited by `admin` on `Mon Mar 31 18:13:32 GMT 2025`
Record UNII	68AYS9A614
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CEDIRANIB MALEAT

Preferred Name

English

CEDIRANIB MALEATE

Official Name

English

AZD2171 MALEATE

Code

English

RECENTIN

Brand Name

English

QUINAZOLINE, 4-((4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY)-6-METHOXY-7-(3-(1-PYRROLIDINYL)PROPOXY)-, (2Z)-2-BUTENEDIOATE (1:1)

Systematic Name

English

CEDIRANIB MALEATE [JAN]

Common Name

English

AZD-2171 MALEATE

Code

English

CEDIRANIB MALEATE [USAN]

Common Name

English

CEDIRANIB MALEATE [MART.]

Common Name

English

Cediranib maleat [WHO-DD]

Common Name

English

4-((4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY)-6-METHOXY-7-(3-PYRROLIDIN-1-YLPROPOXY)QUINAZOLINE (2Z)-BUT-2-ENEDIOATE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1967