Details
Stereochemistry | ACHIRAL |
Molecular Formula | C34H34F2N4O6 |
Molecular Weight | 632.6538 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(C=C1OCCCN3CCOCC3)N=CC=C2OC4=C(F)C=C(NC(=O)C5(CC5)C(=O)NC6=CC=C(F)C=C6)C=C4
InChI
InChIKey=CXQHYVUVSFXTMY-UHFFFAOYSA-N
InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)
DescriptionCurator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022245 | https://www.ncbi.nlm.nih.gov/pubmed/23213094 | http://www.exelixis.com/pipeline/xl880 | https://en.wikipedia.org/wiki/Foretinib
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022245 | https://www.ncbi.nlm.nih.gov/pubmed/23213094 | http://www.exelixis.com/pipeline/xl880 | https://en.wikipedia.org/wiki/Foretinib
Foretinib is an orally available multikinase inhibitor that targets c-MET and VEGFR2 with high affinity, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib is an experimental drug candidate for the treatment of cancer. It was in Phase II trials for the treatment breast cancer, non-small cell lung cancer, gastric cancer, head and neck cancer and papillary renal-cell carcinoma. The most frequent adverse events of any grade associated with foretinib were fatigue, hypertension, gastrointestinal toxicities, and nonfatal pulmonary emboli.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL279 Sources: http://www.exelixis.com/pipeline/xl880 |
0.86 nM [IC50] | ||
Target ID: CHEMBL3717 Sources: http://www.exelixis.com/pipeline/xl880 |
0.4 nM [IC50] | ||
Target ID: CHEMBL4128 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19808973 |
1.1 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Doses
Dose | Population | Adverse events |
---|---|---|
120 mg 1 times / day multiple, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: Page: p.745 |
unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: Page: p.745 |
DLT: Hypertension, Dehydration... Dose limiting toxicities: Hypertension (grade 3, 33.3%) Sources: Page: p.745Dehydration (grade 3, 33.3%) |
80 mg 1 times / day multiple, oral MTD Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.745 |
unhealthy, ADULT n = 25 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 25 Sources: Page: p.745 |
Disc. AE: Left ventricular dysfunction... AEs leading to discontinuation/dose reduction: Left ventricular dysfunction (grade 3, 4%) Sources: Page: p.745 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dehydration | grade 3, 33.3% DLT |
120 mg 1 times / day multiple, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: Page: p.745 |
unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: Page: p.745 |
Hypertension | grade 3, 33.3% DLT |
120 mg 1 times / day multiple, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: Page: p.745 |
unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: Page: p.745 |
Left ventricular dysfunction | grade 3, 4% Disc. AE |
80 mg 1 times / day multiple, oral MTD Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.745 |
unhealthy, ADULT n = 25 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 25 Sources: Page: p.745 |
PubMed
Title | Date | PubMed |
---|---|---|
Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. | 2009 Oct 15 |
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Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | 2010 Nov 24 |
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Comprehensive analysis of kinase inhibitor selectivity. | 2011 Oct 30 |
|
Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety. | 2013 Jun |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23516391
240 mg/day, for 5 days every 2 weeks or daily - 80 mg per day.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21655918
Gastric cancer cell lines MKN-45 and KATO-III, were found to be sensitive to foretinib (IC50 for MKN-45 and KATOIII, 8 nM and 30 nM, respectively).
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1967
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NCI_THESAURUS |
C129825
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42642645
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WW-14
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DB12307
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CHEMBL1230609
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SUB178744
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C80058
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849217-64-7
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FORETINIB
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81FH7VK1C4
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100000164345
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9202
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)