Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H26ClFN4O4S.2C7H8O3S.H2O |
Molecular Weight | 943.4809 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(=O)(=O)CCNCc1ccc(-c2ccc3c(c2)c(ncn3)Nc4ccc(c(c4)Cl)OCc5cccc(c5)F)o1.Cc1ccc(cc1)S(=O)(=O)O.Cc1ccc(cc1)S(=O)(=O)O.O
InChI
InChIKey=XNRVGTHNYCNCFF-UHFFFAOYSA-N
InChI=1S/C29H26ClFN4O4S.2C7H8O3S.H2O/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19;2*1-6-2-4-7(5-3-6)11(8,9)10;/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*2-5H,1H3,(H,8,9,10);1H2
Molecular Formula | C29H26ClFN4O4S |
Molecular Weight | 581.0597 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C7H8O3S |
Molecular Weight | 172.203 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment:: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800015425
Curator's Comment:: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800015425
Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. It is present as the monohydrate of the ditosylate salt (trade name TYKERB). Lapatinib is dual inhibitor of the EGFR (epidermal growth factor receptor; also called HER1 or ErbB1) and HER2 receptor tyrosine kinases. Lapatinib was developed by GlaxoSmithKline, however, Novartis subsequently acquired all the rights to the drug from GlaxoSmithKline. TYKERB is indicated in combination therapy for the treatment of metastatic breast cancer that overexpresses the HER2 receptor.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25977884
Curator's Comment:: Increased lapatinib uptake was observed in brain metastases but not in normal brain.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL203 |
3.0 nM [Ki] | ||
Target ID: CHEMBL1824 |
13.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | TYKERB Approved UseTYKERB® is indicated in combination with: •capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. Limitation of Use: Patients should have disease progression on trastuzumab prior to initiation of treatment with TYKERB in combination with capecitabine. •letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. TYKERB in combination with an aromatase inhibitor has not been compared to a trastuzumab-containing chemotherapy regimen for the treatment of metastatic breast cancer. TYKERB, a kinase inhibitor, is indicated in combination with: (1) •capecitabine, for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. Limitation of Use: Patients should have disease progression on trastuzumab prior to initiation of treatment with TYKERB in combination with capecitabine. •letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. TYKERB in combination with an aromatase inhibitor has not been compared to a trastuzumab-containing chemotherapy regimen for the treatment of metastatic breast cancer. Launch Date1.17374399E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.43 μg/mL |
1250 mg 1 times / day steady-state, oral dose: 1250 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LAPATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36.2 μg × h/mL |
1250 mg 1 times / day steady-state, oral dose: 1250 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LAPATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
24 h |
1250 mg 1 times / day steady-state, oral dose: 1250 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LAPATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
LAPATINIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1250 mg 1 times / day steady, oral MTD Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 27 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 27 Sources: |
DLT: Rash, Diarrhea... Dose limiting toxicities: Rash (grade 3, 2 patients) Sources: Diarrhea (grade 3, 2 patients) Hypoxia (grade 3, 1 patient) Pulmonary embolus (grade 4, 2 patients) |
1500 mg 1 times / day steady, oral Dose: 1500 mg, 1 times / day Route: oral Route: steady Dose: 1500 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 5 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 5 Sources: |
DLT: Mucositis, Rash... Dose limiting toxicities: Mucositis (grade 3, 2 patients) Sources: Rash (grade 3, 2 patients) |
1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Disc. AE: Diarrhea... Other AEs: Diarrhea, Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (grade 4, 1%) Other AEs:Diarrhea (all grades, 65%) Sources: Diarrhea (grade 3, 13%) Nausea (all grades, 44%) Nausea (grade 3, 2%) Vomiting (all grades, 26%) Vomiting (grade 3, 2%) Stomatitis (all grades, 14%) Dyspepsia (all grades, 11%) Dyspepsia (grade 3, <1%) Palmar-plantar erythrodysesthesia syndrome (all grades, 53%) Palmar-plantar erythrodysesthesia syndrome (grade 3, 12%) Rash (all grades, 28%) Rash (grade 3, 2%) Dermatitis acneiform (grade 3, <1%) Dry skin (all grades, 10%) Mucosal inflammation (all grades, 15%) Pain in extremity (all grades, 12%) Pain in extremity (grade 3, 1%) Back pain (all grades, 11%) Back pain (grade 3, 1%) Dyspnea (all grades, 12%) Dyspnea (grade 3, 3%) Insomnia (all grades, 10%) Insomnia (grade 3, <1%) Hepatotoxicity (severe|grade 5) Bilirubin total increased (grade 3, 4%) Bilirubin total increased (grade 1-2, 41%) AST increased (grade 3, 2%) AST increased (grade 4, <1%) AST increased (grade 1-2, 46%) ALT increased (grade 3, 2%) ALT increased (grade 1-2, 35%) |
1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
DLT: Diarrhea, Gamma GT increased... Other AEs: Stomatitis, Rash... Dose limiting toxicities: Diarrhea (grade 3, 2 patients) Other AEs:Gamma GT increased (grade 3, 1 patient) Stomatitis (grade 1, 1 patient) Sources: Rash (grade 2, 2 patients) Seborrheic dermatitis (grade 1, 1 patient) Paronychia (grade 1, 1 patient) Anorexia (grade 1, 3 patients) Lymphocyte count decreased (grade 1, 1 patient) |
1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
Other AEs: Hepatotoxicity, Bilirubin total increased... Other AEs: Hepatotoxicity (severe|grade 5) Sources: Bilirubin total increased (grade 3, <1%) Bilirubin total increased (grade 4, <1%) Bilirubin total increased (grade 1-2, 20%) AST increased (grade 3, 6%) AST increased (grade 1-2, 47%) ALT increased (grade 3, 5%) ALT increased (grade 4, <1%) ALT increased (grade 1-2, 40%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hypoxia | grade 3, 1 patient DLT |
1250 mg 1 times / day steady, oral MTD Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 27 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 27 Sources: |
Diarrhea | grade 3, 2 patients DLT |
1250 mg 1 times / day steady, oral MTD Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 27 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 27 Sources: |
Rash | grade 3, 2 patients DLT |
1250 mg 1 times / day steady, oral MTD Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 27 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 27 Sources: |
Pulmonary embolus | grade 4, 2 patients DLT |
1250 mg 1 times / day steady, oral MTD Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 27 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 27 Sources: |
Mucositis | grade 3, 2 patients DLT |
1500 mg 1 times / day steady, oral Dose: 1500 mg, 1 times / day Route: oral Route: steady Dose: 1500 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 5 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 5 Sources: |
Rash | grade 3, 2 patients DLT |
1500 mg 1 times / day steady, oral Dose: 1500 mg, 1 times / day Route: oral Route: steady Dose: 1500 mg, 1 times / day Co-administed with:: whole brain radiotherapy Sources: |
unhealthy, 50 years (range: 30–78 years) n = 5 Health Status: unhealthy Condition: (HER2)-positive breast cancer Age Group: 50 years (range: 30–78 years) Sex: F Population Size: 5 Sources: |
Dry skin | all grades, 10% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Insomnia | all grades, 10% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Back pain | all grades, 11% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Dyspepsia | all grades, 11% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Dyspnea | all grades, 12% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Pain in extremity | all grades, 12% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Stomatitis | all grades, 14% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Mucosal inflammation | all grades, 15% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Vomiting | all grades, 26% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Rash | all grades, 28% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Nausea | all grades, 44% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Palmar-plantar erythrodysesthesia syndrome | all grades, 53% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Diarrhea | all grades, 65% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
ALT increased | grade 1-2, 35% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Bilirubin total increased | grade 1-2, 41% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
AST increased | grade 1-2, 46% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Back pain | grade 3, 1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Pain in extremity | grade 3, 1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Palmar-plantar erythrodysesthesia syndrome | grade 3, 12% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Diarrhea | grade 3, 13% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
ALT increased | grade 3, 2% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
AST increased | grade 3, 2% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Nausea | grade 3, 2% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Rash | grade 3, 2% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Vomiting | grade 3, 2% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Dyspnea | grade 3, 3% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Bilirubin total increased | grade 3, 4% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Dermatitis acneiform | grade 3, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Dyspepsia | grade 3, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Insomnia | grade 3, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Diarrhea | grade 4, 1% Disc. AE |
1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
AST increased | grade 4, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Hepatotoxicity | severe|grade 5 | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: capecitabine(2000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle) Sources: |
unhealthy, 53 years n = 198 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 53 years Sex: F Population Size: 198 Sources: |
Lymphocyte count decreased | grade 1, 1 patient | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Paronychia | grade 1, 1 patient | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Seborrheic dermatitis | grade 1, 1 patient | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Stomatitis | grade 1, 1 patient | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Anorexia | grade 1, 3 patients | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Rash | grade 2, 2 patients | 1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Gamma GT increased | grade 3, 1 patient DLT |
1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Diarrhea | grade 3, 2 patients DLT, Disc. AE |
1800 mg 1 times / day steady, oral MTD Dose: 1800 mg, 1 times / day Route: oral Route: steady Dose: 1800 mg, 1 times / day Sources: |
unhealthy, 60 years (range: 37 – 73 years) n = 6 Health Status: unhealthy Condition: Solid Tumors Age Group: 60 years (range: 37 – 73 years) Sex: M+F Population Size: 6 Sources: |
Bilirubin total increased | grade 1-2, 20% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
ALT increased | grade 1-2, 40% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
AST increased | grade 1-2, 47% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
ALT increased | grade 3, 5% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
AST increased | grade 3, 6% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
Bilirubin total increased | grade 3, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
ALT increased | grade 4, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
Bilirubin total increased | grade 4, <1% | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
Hepatotoxicity | severe|grade 5 | 1250 mg 1 times / day steady, oral Recommended Dose: 1250 mg, 1 times / day Route: oral Route: steady Dose: 1250 mg, 1 times / day Co-administed with:: Letrozole(2.5 mg/day) Sources: |
unhealthy, 63 years n = 111 Health Status: unhealthy Condition: stage IV breast cancer | estrogen receptor+ |progesterone receptor+ Age Group: 63 years Sex: F Population Size: 111 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. | 2004 |
|
Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance. | 2004 Feb 1 |
|
Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. | 2004 Jan 22 |
|
Gateways to clinical trials. | 2004 Jan-Feb |
|
Early success of combined EGFR and Her2 receptor blockade as a clinical strategy in breast cancer. | 2004 Jun |
|
Gateways to clinical trials. | 2004 Nov |
|
A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. | 2004 Sep 15 |
|
Therapeutic targeting of multiple signaling pathways in malignant pleural mesothelioma. | 2005 |
|
Study of the biologic effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. | 2005 Apr 10 |
|
Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. | 2005 Aug 10 |
|
GlaxoSmithKline cancer drug threatens Herceptin market. | 2005 Dec |
|
Role of tyrosine kinase inhibitors in cancer therapy. | 2005 Dec |
|
Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. | 2005 Jan |
|
The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. | 2005 Jan 1 |
|
Gateways to clinical trials. | 2005 Jan-Feb |
|
Clinical trials of intracellular signal transductions inhibitors for breast cancer--a strategy to overcome endocrine resistance. | 2005 Jul |
|
Gateways to clinical trials. | 2005 Jun |
|
Small molecules with EGFR-TK inhibitor activity. | 2005 May |
|
Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. | 2005 Sep 15 |
|
Antitumor activity of HER-2 inhibitors. | 2005 Sep 8 |
|
Lessons from the drug discovery of lapatinib, a dual ErbB1/2 tyrosine kinase inhibitor. | 2006 |
|
Gateways to clinical trials. | 2006 Dec |
|
Targeted therapy for metastatic breast cancer. | 2006 Dec 28 |
|
Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. | 2006 Feb |
|
Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers. | 2006 Feb 1 |
|
Determination of lapatinib (GW572016) in human plasma by liquid chromatography electrospray tandem mass spectrometry (LC-ESI-MS/MS). | 2006 Feb 2 |
|
Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. | 2006 Jan 1 |
|
Epidermal growth factor receptor dimerization status determines skin toxicity to HER-kinase targeted therapies. | 2006 Jan 16 |
|
Gateways to clinical trials. | 2006 Jan-Feb |
|
Trials probe new agents for kidney cancer. | 2006 Jul 12 |
|
Canonical WNT signaling pathway and human AREG. | 2006 Jun |
|
Gateways to clinical trials. | 2006 Mar |
|
Her-2 targeted therapy: beyond breast cancer and trastuzumab. | 2006 Mar |
|
Lapatinib: current status and future directions in breast cancer. | 2006 Nov-Dec |
|
[Molecular diagnostic and targeted therapy--"Barking dogs are going to bite": presentations from the 42nd Annual Meeting of the American Society of Clinical Oncology, Atlanta 2006]. | 2006 Oct |
|
HER-2-positive breast cancer: hope beyond trastuzumab. | 2007 |
|
relocating job wise? A mathematical model separates quantitatively the cytostatic and cytotoxic effects of a HER2 tyrosine kinase inhibitor. | 2007 Apr 3 |
|
Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy. | 2007 Feb |
|
European Society for Medical Oncology 2006: meeting highlights on targeted therapies. Istanbul, Turkey, 29 September-3 October 2006. | 2007 Feb |
|
Recent advances in the therapy of renal cancer. | 2007 Feb |
|
Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). | 2007 Feb |
|
Synergistic inhibition of breast cancer cell lines with a dual inhibitor of EGFR-HER-2/neu and a Bcl-2 inhibitor. | 2007 Feb |
|
Targeting EGF-receptor-signalling in squamous cell carcinomas of the head and neck. | 2007 Feb 12 |
|
Prospective study of positron emission tomography for evaluation of the activity of lapatinib, a dual inhibitor of the ErbB1 and ErbB2 tyrosine kinases, in patients with advanced tumors. | 2007 Jan |
|
Proteomic identification of secreted proteins as surrogate markers for signal transduction inhibitor activity. | 2007 Jan 29 |
|
Gateways to clinical trials. | 2007 Jan-Feb |
|
Trastuzumab: mechanism of action, resistance and future perspectives in HER2-overexpressing breast cancer. | 2007 Jun |
|
The EGF receptor Hokey-Cokey. | 2007 Mar |
|
Lapatinib moves forward in inflammatory and early HER2-positive breast cancer trials. | 2007 Mar 7 |
|
Recent advances in the treatment of salivary gland cancers: emphasis on molecular targeted therapy. | 2007 Sep |
Patents
Sample Use Guides
The recommended dosage of TYKERB for advanced or metastatic breast cancer is 1,250 mg (5 tablets) given orally once daily on Days 1-21 continuously in combination with capecitabine 2,000 mg/m2 /day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle. The recommended dose of TYKERB for hormone receptor positive, HER2 positive metastatic breast cancer is 1500 mg (6 tablets) given orally once daily continuously in combination with letrozole. When TYKERB is coadministered with letrozole, the recommended dose of letrozole is 2.5 mg once daily. • TYKERB should be taken at least one hour before or one hour after a meal. However, capecitabine should be taken with food or within 30 minutes after food. • TYKERB should be taken once daily. Do not divide daily doses of TYKERB. • Modify dose for cardiac and other toxicities, severe hepatic impairment, and CYP3A4 drug interactions.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22964224
lapatinib-induced time- and dose-dependent phosphorylation dynamics in SKBR3 breast cancer cells. Among 4953 identified phosphopeptides from 1548 proteins, a small proportion (5-7%) was regulated at least twofold by 1-10 μm lapatinib.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 00:03:09 UTC 2021
by
admin
on
Sat Jun 26 00:03:09 UTC 2021
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Record UNII |
G873GX646R
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C2167
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NCI_THESAURUS |
C129825
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NCI_THESAURUS |
C155764
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FDA ORPHAN DRUG |
284309
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SUB27753
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DB01259
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M6688
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C66878
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481474
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388082-78-8
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G873GX646R
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CHEMBL554
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11557040
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ACTIVE MOIETY |