Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H22FN3O3 |
| Molecular Weight | 407.4375 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C=CN=C2C=C1OCC5(N)CC5
InChI
InChIKey=KSMZEXLVHXZPEF-UHFFFAOYSA-N
InChI=1S/C23H22FN3O3/c1-13-9-15-16(27-13)3-4-19(22(15)24)30-18-5-8-26-17-11-21(20(28-2)10-14(17)18)29-12-23(25)6-7-23/h3-5,8-11,27H,6-7,12,25H2,1-2H3
| Molecular Formula | C23H22FN3O3 |
| Molecular Weight | 407.4375 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
AL3818 (anlotinib) is a receptor tyrosine kinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR1, VEGFR2/KDR, and VEGFR3), stem cell factor receptor (C-kit), platelet-derived growth factor (PDGFβ), and fibroblast growth factor receptors (FGFR1, FGFR2, and FGFR3). Anlotibib is a kind of innovative medicines approved by State Food and Drug Administration(SFDA:2011L00661) which was researched by Jiangsu Chia-tai Tianqing Pharmaceutical Co., Ltd. Phase III development is underway for the treatment of thyroid cancer, gastric cancer, leiomyosarcoma; non-small cell lung cancer; synovial sarcoma; thyroid cancer etc.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 0.2 nM [IC50] | |||
| 1.0 nM [IC50] | |||
| 7.7 null [pIC50] | |||
Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27716285 |
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 |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
5.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
10.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
15.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
687 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
562 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1066 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1585 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
102 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
95 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
116 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
98 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27716285/ |
16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANLOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
7.9% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29620050/ |
ANLOTINIB plasma | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Hemoptysis, Pneumonia... Other AEs: Hemoptysis (7 patients) Sources: Pneumonia (3 patients) Venous thromboembolism (3 patients) Interstitial lung disease (2 patients) Pneumothorax (2 patients) Proteinuria (2 patients) Respiratory failure (2 patients) Hypertension (1 pt) Abdominal pain (1 pt) Gastrointestinal hemorrhage (1 pt) Hypophosphatemia (1 pt) Oral mucositis (1 pt) Fatigue (1 pt) Hand foot syndrome (1 pt) Low density lipoprotein increased (1 pt) Appendicitis (1 pt) Hand-foot syndrome (7 patients) Hypertension (3 patients) Hypertriglyceridemia (2 patients) Diarrhea (1 pt) Liver dysfunction (1 pt) Anorexia (2 patients) Oral mucositis (2 patients) Arrhythmia (2 patients) Fatigue (1 pt) Dyspnea (1 pt) Hypertension (all grades, 67.7%) Fatigue (all grades, 52%) Anorexia (all grades, 45.9%) Hypertriglyceridemia (all grades, 44.6%) Hand-foot syndrome (all grades, 43.9%) Hypercholesteremia (all grades, 41.8%) Cough (all grades, 41.5%) Diarrhea (all grades, 35.4%) Low density lipoprotein increased (all grades, 31.3%) Proteinuria (all grades, 28.9%) Pharyngalgia (all grades, 28.2%) Blood bilirubin increased (all grades, 26.2%) Hyponatremia (all grades, 23.5%) Weight loss (all grades, 23.1%) Mucositis oral (all grades, 23.1%) Dysphonia (all grades, 23.1%) Low density lipoprotein increased (all grades, 21.1%) Hemoptysis (all grades, 20.4%) Hematuria (all grades, 15%) Upper respiratory infection (all grades, 12.6%) Urinary tract infection (all grades, 11.6%) Headache (all grades, 11.2%) Decreased platelet count (all grades, 10.5%) Hypertension (grade 3-4, 13.6%) Fatigue (grade 3-4, 1 pt) Anorexia (grade 3-4, 3 patients) Hypertriglyceridemia (grade 3-4, 9 patients) Hand-foot syndrome (grade 3-4, 11 patient) Cough (grade 3-4, 3 patients) Diarrhea (grade 3-4, 3 patients) GGT increased (grade 3-4, 16 patients) Proteinuria (grade 3-4, 7 patients) Pharyngalgia (grade 3-4, 2 patients) Pharyngalgia (grade 3-4, 5 patients) Hyponatremia (grade 3-4, 24 patients) Mucositis oral (grade 3-4, 3 patients) Dysphonia (grade 3-4, 3 patients) GGT elevation (grade 3-4, 2 patients) Hemoptysis (grade 3-4, 9 patients) Decreased platelet count (grade 3-4, 3 patients) |
12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Fatigue, Hypertension... Other AEs: Fatigue (all grades, 57%) Sources: Hypertension (all grades, 54%) Decreased appetite (all grades, 43%) Hypothyroidism (all grades, 36%) Palmar-plantar erythrodysesthesia (all grades, 27%) Proteinuria (all grades, 26%) Weight loss (all grades, 19%) Diarrhea (all grades, 17%) Leukopenia (all grades, 17%) Aspartate aminotransferase increased (all grades, 17%) Hypercholesterolemia (all grades, 15%) Hypertriglyceridemia (all grades, 14%) Gamma-glutamyltransferase increased (all grades, 14%) Alanine aminotransferase increased (all grades, 14%) Dysphonia (all grades, 14%) Low density lipoprotein increased (all grades, 13%) Lymphocytopenia (all grades, 13%) Oropharyngeal pain (all grades, 12%) Abdominal pain (all grades, 12%) Globulin urine present (all grades, 11%) Neutrophil count decreased (all grades, 11%) Rash (all grades, 10%) Nausea (all grades, 10%) Hyperglycemia (all grades, 5%) Insomnia (all grades, 1 pt) Fatigue (grade 3, 2%) Hypertension (grade 3, 16%) Decreased appetite (grade 3, 6%) Hypothyroidism (grade 3, 1 pt) Palmar-plantar erythrodysesthesia (grade 3, 2 patients) Proteinuria (grade 3, 1 pt) Electrocardiogram QTc interval prolonged (grade 3, 1 pt) Weight loss (grade 3, 3 patients) Electrocardiogram QTc interval prolonged (grade 3, 2 patients) Gamma-glutamyltransferase increased (grade 3, 3 patients) Alanine aminotransferase increased (grade 3, 1 pt) Increased low density lipoprotein (grade 3, 1 pt) Lymphocytopenia (grade 3, 2 patients) Oropharyngeal pain (grade 4, 1 pt) death (grade 5, 3 patients) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abdominal pain | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Appendicitis | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Diarrhea | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Dyspnea | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Gastrointestinal hemorrhage | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hand foot syndrome | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypophosphatemia | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Liver dysfunction | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Low density lipoprotein increased | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Oral mucositis | 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Anorexia | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Arrhythmia | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertriglyceridemia | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Interstitial lung disease | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Oral mucositis | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Pneumothorax | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Proteinuria | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Respiratory failure | 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Pneumonia | 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Venous thromboembolism | 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hand-foot syndrome | 7 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hemoptysis | 7 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Decreased platelet count | all grades, 10.5% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Headache | all grades, 11.2% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Urinary tract infection | all grades, 11.6% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Upper respiratory infection | all grades, 12.6% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hematuria | all grades, 15% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hemoptysis | all grades, 20.4% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Low density lipoprotein increased | all grades, 21.1% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Dysphonia | all grades, 23.1% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Mucositis oral | all grades, 23.1% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Weight loss | all grades, 23.1% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hyponatremia | all grades, 23.5% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Blood bilirubin increased | all grades, 26.2% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Pharyngalgia | all grades, 28.2% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Proteinuria | all grades, 28.9% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Low density lipoprotein increased | all grades, 31.3% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Diarrhea | all grades, 35.4% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Cough | all grades, 41.5% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypercholesteremia | all grades, 41.8% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hand-foot syndrome | all grades, 43.9% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertriglyceridemia | all grades, 44.6% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Anorexia | all grades, 45.9% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | all grades, 52% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | all grades, 67.7% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | grade 3-4, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hand-foot syndrome | grade 3-4, 11 patient | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | grade 3-4, 13.6% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| GGT increased | grade 3-4, 16 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| GGT elevation | grade 3-4, 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Pharyngalgia | grade 3-4, 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hyponatremia | grade 3-4, 24 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Anorexia | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Cough | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Decreased platelet count | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Diarrhea | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Dysphonia | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Mucositis oral | grade 3-4, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Pharyngalgia | grade 3-4, 5 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Proteinuria | grade 3-4, 7 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hemoptysis | grade 3-4, 9 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertriglyceridemia | grade 3-4, 9 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Insomnia | all grades, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Nausea | all grades, 10% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Rash | all grades, 10% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Globulin urine present | all grades, 11% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Neutrophil count decreased | all grades, 11% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Abdominal pain | all grades, 12% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Oropharyngeal pain | all grades, 12% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Low density lipoprotein increased | all grades, 13% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Lymphocytopenia | all grades, 13% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Alanine aminotransferase increased | all grades, 14% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Dysphonia | all grades, 14% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Gamma-glutamyltransferase increased | all grades, 14% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertriglyceridemia | all grades, 14% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypercholesterolemia | all grades, 15% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Aspartate aminotransferase increased | all grades, 17% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Diarrhea | all grades, 17% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Leukopenia | all grades, 17% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Weight loss | all grades, 19% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Proteinuria | all grades, 26% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Palmar-plantar erythrodysesthesia | all grades, 27% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypothyroidism | all grades, 36% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Decreased appetite | all grades, 43% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hyperglycemia | all grades, 5% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | all grades, 54% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | all grades, 57% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Alanine aminotransferase increased | grade 3, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Electrocardiogram QTc interval prolonged | grade 3, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypothyroidism | grade 3, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Increased low density lipoprotein | grade 3, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Proteinuria | grade 3, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Hypertension | grade 3, 16% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Electrocardiogram QTc interval prolonged | grade 3, 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Lymphocytopenia | grade 3, 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Palmar-plantar erythrodysesthesia | grade 3, 2 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | grade 3, 2% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Gamma-glutamyltransferase increased | grade 3, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Weight loss | grade 3, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Decreased appetite | grade 3, 6% | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Oropharyngeal pain | grade 4, 1 pt | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| death | grade 5, 3 patients | 12 mg 1 times / day multiple, oral Studied dose Dose: 12 mg, 1 times / day Route: oral Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Endometrial Cancers Harboring Mutated Fibroblast Growth Factor Receptor 2 Protein Are Successfully Treated With a New Small Tyrosine Kinase Inhibitor in an Orthotopic Mouse Model. | 2018-01 |
|
| Safety and Efficacy of the S-1/Temozolomide Regimen in Patients with Metastatic Neuroendocrine Tumors. | 2018 |
|
| Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors. | 2016-10-04 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT03016819
Anlotinib (AL3818) 12 mg orally administered once daily in 21-day cycles (14 days on treatment, 7 days off treatment)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28953502
AN3CA cells
appeared the most sensitive to AL3818 with an IC50 value of 84
nM. The other cell lines were approximately 28- to
550-fold less sensitive to AL3818. HEC1B had an IC50 value
of 46 uM, and MFE296 cells were sensitive to AL3818,
with an IC50 value of 2.9 uM compared with 3.2, 28.9, 29,
and 40 uM for Ishikawa, MFE280, KLE, and HEC1A, respectively.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:10:25 GMT 2025
by
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Mon Mar 31 21:10:25 GMT 2025
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| Record UNII |
GKF8S4C432
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Validated (UNII)
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NCI_THESAURUS |
C129825
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FDA ORPHAN DRUG |
576017
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NCI_THESAURUS |
C1742
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DB11885
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SUB192810
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C138997
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100000177425
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GKF8S4C432
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ANLOTINIB
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PRIMARY | Anlotinib (AL3818) - MedKoo CAT NO.: 206058Description: Anlotinib, alos known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (Last update: 7/2/2015). Synonym: AL3818, AL-3818, AL 3818, Anlotinib - IUPAC/Chemical Name: NONE | ||
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LM-10
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1058156-90-3
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CHEMBL3545021
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25017411
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11077
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ACTIVE MOIETY |
Results: Dose-limiting toxicities (DLT) at the 10mg/d for consecutive 4 weeks group was grade 3 hypertension, and significant accumulation of anlotinib was observed. For 2 weeks on/1 week off group, DLT were grade 3 hypertension and grade 3 fatigue at the dose of 16 mg/d, the maximum-tolerated doses (MTD) was 12mg/d, the plasma concentration of anlotinib was well controlled. Anlotinib reached its maximum plasma concentration with Tmax of 411 h after orally administration at 10, 12, or 16 mg/subject. Then it eliminated slowly with t1/2of 64136 h and MRT of 124167 h. 20 patients of the 21 patients at the dose of 12mg/d (2 weeks on/1 week off) were assessable for efficacy, 3 patients had a partial response(include renal cancer(n = 2), and soft tissue tumor),14 patients had stable disease(include medullary carcinoma of thyroid, NSCLC, colon cancer, melanoma, thymic carcinoma, and adenoid cystic carcinoma), with 9 patients lasting > 72 weeks. Official Title: A Phase I Study of Anlotinib on Tolerance and Pharmacokinetics Purpose: Anlotibib (ALTN) is a kind of innovative medicines approved by State Food and Drug AdministrationSFDA which was researched by Jiangsu Chia-tai Tianqing Pharmaceutical Co., Ltd. ALTN is a kinase inhibitor of receptor tyrosine with multi-targets, especially for VEGFR2 and VEGFR3. It has the obvious resistance to new angiogenesis. Drug: Anlotinib(Primary); Indication: Renal cell carcinoma; Focus: Therapeutic Use; Sponsor: Chia Tai Tianqing Pharmaceutical Group; Most Recent Events: 25 Apr 2016 Planned End Date changed from 1 Dec 2015 to 1 Dec 2016., 25 Apr 2016 Planned primary completion date changed from 1 Dec 2015 to 1 Dec 2016., 22 Oct 2015 Status changed from recruiting to active, no longer recruiting, as reported by ClinicalTrials.gov.
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