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Details

Stereochemistry ACHIRAL
Molecular Formula C29H26ClFN4O4S
Molecular Weight 581.058
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LAPATINIB

SMILES

CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC=C3N=CN=C(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)C3=C2

InChI

InChIKey=BCFGMOOMADDAQU-UHFFFAOYSA-N
InChI=1S/C29H26ClFN4O4S/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/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)

HIDE SMILES / InChI

Molecular Formula C29H26ClFN4O4S
Molecular Weight 581.058
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
Therapeutic targeting of multiple signaling pathways in malignant pleural mesothelioma.
2005
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
Gateways to clinical trials.
2005 Mar
Antitumor activity of HER-2 inhibitors.
2005 Sep 8
HER2 therapy: molecular mechanisms of trastuzumab resistance.
2006
Two targets, one drug for new EGFR inhibitors.
2006 Aug 16
The molecular biology and immunology of glioblastoma multiforme (GBM) with the presentation of an immunotherapy protocol for a clinical trial.
2006 Dec
Targeting growth factor and antiangiogenic pathways in clear-cell renal cell carcinoma: rationale and ongoing trials.
2006 Dec
Gateways to clinical trials.
2006 Dec
A novel mutation in the tyrosine kinase domain of ERBB2 in hepatocellular carcinoma.
2006 Dec 6
Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers.
2006 Feb 1
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
Gateways to clinical trials.
2006 Jan-Feb
Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer.
2006 Jul
Trials probe new agents for kidney cancer.
2006 Jul 12
Old and new perspectives in the pharmacological treatment of advanced or recurrent endometrial cancer: Hormonal therapy, chemotherapy and molecularly targeted therapies.
2006 Jun
Systemic therapy in the palliative management of advanced salivary gland cancers.
2006 Jun 10
Gateways to clinical trials.
2006 Mar
Her-2 targeted therapy: beyond breast cancer and trastuzumab.
2006 Mar
A phase II study of vinflunine in bladder cancer patients progressing after first-line platinum-containing regimen.
2006 May 22
Lapatinib: current status and future directions in breast cancer.
2006 Nov-Dec
Receptor tyrosine kinase (RTK) inhibition is effective in chemosensitising EGFR-expressing drug resistant human ovarian cancer cell lines when used in combination with cytotoxic agents.
2006 Oct 16
Closing in on a cure.
2006 Oct 23
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
2006 Sep 1
Combination therapy with aromatase inhibitors: the next era of breast cancer treatment?
2006 Sep 18
HER-2-positive breast cancer: hope beyond trastuzumab.
2007
Targeted therapy of breast cancer.
2007
HER2 therapy. HER2 (ERBB2): functional diversity from structurally conserved building blocks.
2007
relocating job wise? A mathematical model separates quantitatively the cytostatic and cytotoxic effects of a HER2 tyrosine kinase inhibitor.
2007 Apr 3
Lapatinib plus capecitabine in breast cancer.
2007 Apr 5
TEACH: Tykerb evaluation after chemotherapy.
2007 Feb
Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy.
2007 Feb
Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signaling.
2007 Feb
European Society for Medical Oncology 2006: meeting highlights on targeted therapies. Istanbul, Turkey, 29 September-3 October 2006.
2007 Feb
Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity.
2007 Feb
Recent advances in the therapy of renal cancer.
2007 Feb
Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu).
2007 Feb
Lapatinib antitumor activity is not dependent upon phosphatase and tensin homologue deleted on chromosome 10 in ErbB2-overexpressing breast cancers.
2007 Feb 1
Therapeutic advances in the treatment of brain metastases.
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
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
2007 Mar
The EGF receptor Hokey-Cokey.
2007 Mar
Vinorelbine plus 3-weekly trastuzumab in metastatic breast cancer: a single-centre phase 2 trial.
2007 Mar 20
Chemotherapy in advanced biliary tract carcinoma: a pooled analysis of clinical trials.
2007 Mar 26
Lapatinib moves forward in inflammatory and early HER2-positive breast cancer trials.
2007 Mar 7
Combination treatment with Grb7 peptide and Doxorubicin or Trastuzumab (Herceptin) results in cooperative cell growth inhibition in breast cancer cells.
2007 May 21
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 Wed Jul 05 23:50:52 UTC 2023
Edited
by admin
on Wed Jul 05 23:50:52 UTC 2023
Record UNII
0VUA21238F
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LAPATINIB
EMA EPAR   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
LAPATINIB [EMA EPAR]
Common Name English
lapatinib [INN]
Common Name English
GSK-572016
Code English
GW-572016X
Code English
LAPATINIB [MI]
Common Name English
GW572016
Code English
LAPATINIB [VANDF]
Common Name English
GW-572016
Code English
Lapatinib [WHO-DD]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175605
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
NDF-RT N0000175076
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
WHO-VATC QL01XE07
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
NCI_THESAURUS C155764
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
LIVERTOX NBK547971
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
NCI_THESAURUS C2167
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
NCI_THESAURUS C129825
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
FDA ORPHAN DRUG 284209
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
WHO-ATC L01XE07
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
Code System Code Type Description
SMS_ID
100000089379
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
ChEMBL
CHEMBL554
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
RXCUI
480167
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY RxNorm
LACTMED
Lapatinib
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
DRUG CENTRAL
1548
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
MESH
C490728
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
NSC
727989
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
PUBCHEM
208908
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
NCI_THESAURUS
C26653
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
DAILYMED
0VUA21238F
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
EVMPD
SUB25379
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
IUPHAR
5692
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
HSDB
8209
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
EPA CompTox
DTXSID7046675
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
MERCK INDEX
M6688
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY Merck Index
INN
8378
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
WIKIPEDIA
LAPATINIB
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
CAS
231277-92-2
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
DRUG BANK
DB01259
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
FDA UNII
0VUA21238F
Created by admin on Wed Jul 05 23:50:52 UTC 2023 , Edited by admin on Wed Jul 05 23:50:52 UTC 2023
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
Lapatinib is a mechanism-based inactivator of CYP3A4, most likely via the formation and further oxidation of its O-dealkylated metabolite to a quinoneimine that covalently modifies the CYP3A4 apoprotein and/or heme moiety.
TIME-DEPENDENT INHIBITION
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
SALT/SOLVATE -> PARENT
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
Related Record Type Details
METABOLITE -> PARENT
METABOLITE TOXIC -> PARENT
Specifically, the structure of O-dealkylated lapatinib has the potential to generate a reactive quinoneimine similar to the model hepatotoxin acetaminophen. lapatinib is a mechanism-based inactivator of CYP3A4, most likely via the formation and further oxidation of its O-dealkylated metabolite to a quinoneimine that covalently modifies the CYP3A4 apoprotein and/or heme moiety.
MAJOR
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
MAJOR
FECAL
METABOLITE -> PARENT
METABOLITE -> PARENT
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC