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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
Structure of LAPATINIB DITOSYLATE

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

HIDE SMILES / InChI

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

Description
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

Curator's Comment:: Increased lapatinib uptake was observed in brain metastases but not in normal brain.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TYKERB

Approved Use

TYKERB® 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 Date

1.17374399E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
LAPATINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse 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)
Diarrhea (grade 3, 2 patients)
Hypoxia (grade 3, 1 patient)
Pulmonary embolus (grade 4, 2 patients)
Sources:
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)
Rash (grade 3, 2 patients)
Sources:
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%)
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%)
Sources:
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)
Gamma GT increased (grade 3, 1 patient)
Other AEs:
Stomatitis (grade 1, 1 patient)
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)
Sources:
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)
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%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
yes [EC50 52.5 uM]
yes [IC50 1.86 uM]
yes [IC50 3.91 uM]
yes [IC50 4.02 uM]
yes [Inhibition 30 uM]
yes [Ki 0.6 uM]
yes [Ki 1.1 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
yes (co-administration study)
Comment: Lapatinib exposure were reduced by 72% after CYP3A4 induction by carbamazepine, and increased to 3.6 times control after CYP3A4 inhibition by ketoconazole.
Page: 5.0
minor
minor
unknown (co-administration study)
Comment: Based upon the ability of laptinib to act as a CYP 2C8 inhibitor in vitro, the Applicant agrees to perform an in vivo drug interaction study of the ability of steady-state lapatinib dosing to alter the pharmacokinetics of a single dose of paclitaxel or rosiglitazone.
Page: 5.0
no
no
no
no
no
no
yes
yes
unknown (co-administration study)
Comment: Based upon the ability of laptinib to act as a Pgp inhibitor in vitro, the Applicant agrees to perform an in vivo drug interaction study of the ability of steady-state lapatinib dosing to alter the pharmacokinetics of a single dose of digoxin
Page: 5.0
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
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
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 Sat Jun 26 00:03:09 UTC 2021
Edited
by admin
on Sat Jun 26 00:03:09 UTC 2021
Record UNII
G873GX646R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LAPATINIB DITOSYLATE
ORANGE BOOK   USAN  
USAN  
Official Name English
LAPATINIB DITOLUENESULFONATE MONOHYDRATE
MI  
Common Name English
LAPATINIB TOSILATE HYDRATE
JAN  
Common Name English
LAPATINIB DITOSYLATE MONOHYDRATE
WHO-DD  
Common Name English
LAPATINIB DITOSYLATE [ORANGE BOOK]
Common Name English
LAPATINIB TOSILATE HYDRATE [JAN]
Common Name English
TYVERB
Brand Name English
GW-572016F
Code English
LAPATINIB DITOLUENESULFONATE MONOHYDRATE [MI]
Common Name English
4-QUINAZOLINAMINE, N-(3-CHLORO-4-((3-FLUOROPHENYL)METHOXY)PHENYL)-6-(5-(((2-(METHYLSULPHONYL)ETHYL)AMINO)METHYL)-2-FURANYL)-, BIS(4-METHYLBENZENESULPHONATE), MONOHYDRATE
Common Name English
LAPATINIB TOSILATE [MART.]
Common Name English
LAPATINIB DITOSYLATE [USAN]
Common Name English
GW572016F
Code English
4-QUINAZOLINAMINE, N-(3-CHLORO-4-((3-FLUOROPHENYL)METHOXY)PHENYL)-6-(5-(((2-(METHYLSULFONYL)ETHYL)AMINO)METHYL)-2-FURANYL)-, 4-METHYLBENZENESULFONATE, HYDRATE (1:2:1)
Common Name English
LAPATINIB DITOSYLATE MONOHYDRATE [WHO-DD]
Common Name English
TYKERB
Brand Name English
N-(3-CHLORO-4-((3-FLUOROBENZYL)OXY)PHENYL)-6-(5-(((2-(METHYLSULFONYL)ETHYL)AMINO)METHYL)FURAN-2-YL)QUINAZOLIN-4-AMINE BIS(4-METHYLBENZENESULFONATE) MONOHYDRATE
Common Name English
4-QUINAZOLINAMINE, N-(3-CHLORO-4-((3-FLUOROPHENYL)METHOXY)PHENYL)-6-(5-(((2-(METHYLSULFONYL)ETHYL)AMINO)METHYL)-2-FURANYL)-, BIS(4-METHYLBENZENESULFONATE), MONOHYDRATE
Common Name English
TYCERB
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C2167
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
NCI_THESAURUS C155764
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
FDA ORPHAN DRUG 284309
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
Code System Code Type Description
EVMPD
SUB27753
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
DRUG BANK
DB01259
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
MERCK INDEX
M6688
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C66878
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
RXCUI
481474
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY RxNorm
CAS
388082-78-8
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
FDA UNII
G873GX646R
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
ChEMBL
CHEMBL554
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
PUBCHEM
11557040
Created by admin on Sat Jun 26 00:03:09 UTC 2021 , Edited by admin on Sat Jun 26 00:03:09 UTC 2021
PRIMARY
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PARENT -> SALT/SOLVATE
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