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Details

Stereochemistry ACHIRAL
Molecular Formula C30H29ClN6O3
Molecular Weight 557.0437
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of NERATINIB

SMILES

CCOc1cc2c(cc1N=C(/C(/[H])=C(\[H])/CN(C)C)O)c(=Nc3ccc(c(c3)Cl)OCc4ccccn4)c(C#N)c[nH]2

InChI

InChIKey=JWNPDZNEKVCWMY-VQHVLOKHSA-N
InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+

HIDE SMILES / InChI

Molecular Formula C30H29ClN6O3
Molecular Weight 557.0437
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26089701 | https://www.ncbi.nlm.nih.gov/pubmed/15715478

Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours.

Originator

Curator's Comment:: # Wyeth (now Pfizer)

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
59.0 nM [IC50]
92.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
NERLYNX

Approved Use

NERLYNX is indicated for the extended adjuvant treatment of adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab based therapy.

Launch Date

1.50016321E12
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
73.1 ng/mL
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
81.5 ng/mL
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
76.3 ng/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
71.8 ng/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1060 ng × h/mL
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
1110 ng × h/mL
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
1640 ng × h/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
891 ng × h/mL
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
14.6 h
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
22.7 h
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
14.3 h
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
12.6 h
240 mg single, oral
dose: 240 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
NERATINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Funbound

Funbound

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

Doses

DosePopulationAdverse events​
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 49.5 years (range: 42-63 years)
n = 6
Health Status: unhealthy
Condition: Non–small cell lung cancer | breast cancer
Age Group: 49.5 years (range: 42-63 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Diarrhea...
Disc. AE: Fatigue...
Dose limiting toxicities:
Diarrhea (grade 3, 3 patients)
AEs leading to
discontinuation/dose reduction:
Fatigue (all grades, 5 patients)
Sources:
240 mg 1 times / day steady, oral
Recommended
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
DLT: Diarrhea, Diarrhea...
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Disc. AE: Nausea, Abdominal pain...
Other AEs: Nausea, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Nausea (grade 3, 2%)
Abdominal pain (grade 3, 2%)
Abdominal pain upper (grade 3, 2%)
Abdominal pain lower (grade 3, 2%)
Vomiting (grade 3, 3%)
Fatigue (grade 3, 2%)
Alanine aminotransferase increased (grade 3, 1%)
Alanine aminotransferase increased (grade 4, 0.2%)
Other AEs:
Nausea (all grades, 43%)
Abdominal pain (all grades, 36%)
Abdominal pain upper (all grades, 36%)
Abdominal pain lower (all grades, 36%)
Vomiting (all grades, 26%)
Stomatitis (all grades, 14%)
Aphthous stomatitis (all grades, 14%)
Mouth ulceration (all grades, 14%)
Oral mucosal blistering (all grades, 14%)
Mucosal inflammation (all grades, 14%)
Oropharyngeal pain (all grades, 14%)
Oral pain (all grades, 14%)
Glossodynia (all grades, 14%)
Glossitis (all grades, 14%)
Cheilitis (all grades, 14%)
Stomatitis (grade 3, 0.3%)
Aphthous stomatitis (grade 3, 0.3%)
Mouth ulceration (grade 3, 0.3%)
Oral mucosal blistering (grade 3, 0.3%)
Mucosal inflammation (grade 3, 0.3%)
Oropharyngeal pain (grade 3, 0.3%)
Oral pain (grade 3, 0.3%)
Glossodynia (grade 3, 0.3%)
Glossitis (grade 3, 0.3%)
Cheilitis (grade 3, 0.3%)
Dyspepsia (all grades, 10%)
Dyspepsia (grade 3, 0.4%)
Abdominal distension (all grades, 5%)
Abdominal distension (grade 3, 0.3%)
Dry mouth (all grades, 3%)
Dry mouth (grade 3, 0.1%)
Fatigue (all grades, 27%)
Alanine aminotransferase increased (all grades, 9%)
Aspartate aminotransferase increased (all grades, 7%)
Aspartate aminotransferase increased (grade 3, 0.5%)
Aspartate aminotransferase increased (grade 4, 0.2%)
Urinary tract infection (all grades, 5%)
Urinary tract infection (grade 3, 0.1%)
Weight decreased (all grades, 5%)
Weight decreased (grade 3, 0.1%)
Decreased appetite (all grades, 12%)
Decreased appetite (grade 3, 0.2%)
Dehydration (all grades, 4%)
Dehydration (grade 3, 0.9%)
Dehydration (grade 4, 0.1%)
Muscle spasms (all grades, 11%)
Muscle spasms (grade 3, 0.1%)
Epistaxis (all grades, 5%)
Rash (all grades, 18%)
Rash erythematous (all grades, 18%)
Rash follicular (all grades, 18%)
Generalized rash (all grades, 18%)
Rash pruritic (all grades, 18%)
Rash pustular (all grades, 18%)
Maculopapular rash (all grades, 18%)
Rash papular (all grades, 18%)
Dermatitis (all grades, 18%)
Dermatitis acneiform (all grades, 18%)
Toxic skin eruption (all grades, 18%)
Rash (grade 3, 0.6%)
Rash erythematous (grade 3, 0.6%)
Rash follicular (grade 3, 0.6%)
Generalized rash (grade 3, 0.6%)
Rash pruritic (grade 3, 0.6%)
Rash pustular (grade 3, 0.6%)
Maculopapular rash (grade 3, 0.6%)
Rash papular (grade 3, 0.6%)
Dermatitis (grade 3, 0.6%)
Dermatitis acneiform (grade 3, 0.6%)
Toxic skin eruption (grade 3, 0.6%)
Dry skin (all grades, 6%)
Nail disorder (all grades, 8%)
Paronychia (all grades, 8%)
Onychoclasis (all grades, 8%)
Nail discoloration (all grades, 8%)
Nail toxicity (all grades, 8%)
Nail growth abnormal (all grades, 8%)
Nail dystrophy (all grades, 8%)
Nail disorder (grade 3, 0.3%)
Paronychia (grade 3, 0.3%)
Onychoclasis (grade 3, 0.3%)
Nail discoloration (grade 3, 0.3%)
Nail toxicity (grade 3, 0.3%)
Nail growth abnormal (grade 3, 0.3%)
Nail dystrophy (grade 3, 0.3%)
Skin fissures (all grades, 2%)
Skin fissures (grade 3, 0.1%)
Sources:
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Other AEs: Bilirubin increased, Bilirubin increased...
Other AEs:
Bilirubin increased (all grades, 11.1%)
Bilirubin increased (grade 3, 0.1%)
Alkaline phosphatase (all grades, 22.7%)
Creatinine increased (all grades, 12.5%)
Creatinine increased (grade 4, 0.1%)
Creatinine increased (grade 3, 0.1%)
Hypercalcemia (all grades, 11.2%)
Hypercalcemia (grade 4, 0.2%)
Hypercalcemia (grade 3, 0.4%)
Hypermagnesemia (all grades, 5.2%)
Hypermagnesemia (grade 4, 0.1%)
Hypermagnesemia (grade 3, 0.9%)
Hypernatremia (all grades, 10.3%)
Hypernatremia (grade 4, 0.1%)
Hypernatremia (grade 3, 0.1%)
Hypoalbuminemia (all grades, 8.4%)
Hypoalbuminemia (grade 3, 0.1%)
Hypocalcemia (all grades, 48.9%)
Hypocalcemia (grade 4, 0.9%)
Hypocalcemia (grade 3, 0.1%)
Hypokalemia (all grades, 7.5%)
Hypokalemia (grade 4, 0.1%)
Hypokalemia (grade 3, 0.3%)
Hypomagnesemia (all grades, 7.2%)
Hypomagnesemia (grade 4, 0.2%)
Hypomagnesemia (grade 3, 0.4%)
Hyponatremia (all grades, 11.6%)
Hyponatremia (grade 3, 0.9%)
Sources: Page: p. 117
180 mg 1 times / day steady, oral
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, 56.5 years (range: 46-90 years)
n = 6
Health Status: unhealthy
Condition: Breast cancer
Age Group: 56.5 years (range: 46-90 years)
Sex: F
Population Size: 6
Sources:
DLT: Diarrhea...
Disc. AE: Fatigue...
Dose limiting toxicities:
Diarrhea (grade 3, 1 patient)
AEs leading to
discontinuation/dose reduction:
Fatigue (all grades, 1 patient)
Sources:
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Disc. AE: Diarrhea, Fatigue...
Other AEs: Abdominal pain, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (all grades, 92%)
Fatigue (all grades, 49%)
Other AEs:
Abdominal pain (all grades, 21%)
Nausea (all grades, 54%)
Vomiting (all grades, 49%)
Anorexia (all grades, 33%)
Rash (all grades, 8%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fatigue all grades, 5 patients
Disc. AE
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 49.5 years (range: 42-63 years)
n = 6
Health Status: unhealthy
Condition: Non–small cell lung cancer | breast cancer
Age Group: 49.5 years (range: 42-63 years)
Sex: M+F
Population Size: 6
Sources:
Diarrhea grade 3, 3 patients
DLT, Disc. AE
400 mg 1 times / day steady, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 49.5 years (range: 42-63 years)
n = 6
Health Status: unhealthy
Condition: Non–small cell lung cancer | breast cancer
Age Group: 49.5 years (range: 42-63 years)
Sex: M+F
Population Size: 6
Sources:
Diarrhea all grades, 95%
DLT, Disc. AE
240 mg 1 times / day steady, oral
Recommended
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Diarrhea grade 3, 40%
DLT, Disc. AE
240 mg 1 times / day steady, oral
Recommended
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Diarrhea grade 4, 0.1%
DLT, Disc. AE
240 mg 1 times / day steady, oral
Recommended
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dyspepsia all grades, 10%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Muscle spasms all grades, 11%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Decreased appetite all grades, 12%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Aphthous stomatitis all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Cheilitis all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Glossitis all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Glossodynia all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Mouth ulceration all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Mucosal inflammation all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oral mucosal blistering all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oral pain all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oropharyngeal pain all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Stomatitis all grades, 14%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dermatitis acneiform all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dermatitis all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Generalized rash all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Maculopapular rash all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash erythematous all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash follicular all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash papular all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash pruritic all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash pustular all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Toxic skin eruption all grades, 18%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Skin fissures all grades, 2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Vomiting all grades, 26%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Fatigue all grades, 27%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dry mouth all grades, 3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain lower all grades, 36%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain upper all grades, 36%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain all grades, 36%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dehydration all grades, 4%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nausea all grades, 43%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal distension all grades, 5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Epistaxis all grades, 5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Urinary tract infection all grades, 5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Weight decreased all grades, 5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dry skin all grades, 6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Aspartate aminotransferase increased all grades, 7%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail discoloration all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail disorder all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail dystrophy all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail growth abnormal all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail toxicity all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Onychoclasis all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Paronychia all grades, 8%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Alanine aminotransferase increased all grades, 9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dry mouth grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Muscle spasms grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Skin fissures grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Urinary tract infection grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Weight decreased grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Decreased appetite grade 3, 0.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal distension grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Aphthous stomatitis grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Cheilitis grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Glossitis grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Glossodynia grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Mouth ulceration grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Mucosal inflammation grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail discoloration grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail disorder grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail dystrophy grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail growth abnormal grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nail toxicity grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Onychoclasis grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oral mucosal blistering grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oral pain grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Oropharyngeal pain grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Paronychia grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Stomatitis grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dyspepsia grade 3, 0.4%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Aspartate aminotransferase increased grade 3, 0.5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dermatitis acneiform grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dermatitis grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Generalized rash grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Maculopapular rash grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash erythematous grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash follicular grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash papular grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash pruritic grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash pustular grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Rash grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Toxic skin eruption grade 3, 0.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dehydration grade 3, 0.9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Alanine aminotransferase increased grade 3, 1%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain lower grade 3, 2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain upper grade 3, 2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Abdominal pain grade 3, 2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Fatigue grade 3, 2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Nausea grade 3, 2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Vomiting grade 3, 3%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Dehydration grade 4, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Aspartate aminotransferase increased grade 4, 0.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Alanine aminotransferase increased grade 4, 0.2%
Disc. AE
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources:
Hypernatremia all grades, 10.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Bilirubin increased all grades, 11.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypercalcemia all grades, 11.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hyponatremia all grades, 11.6%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Creatinine increased all grades, 12.5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Alkaline phosphatase all grades, 22.7%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypocalcemia all grades, 48.9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypermagnesemia all grades, 5.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypomagnesemia all grades, 7.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypokalemia all grades, 7.5%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypoalbuminemia all grades, 8.4%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Bilirubin increased grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Creatinine increased grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypernatremia grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypoalbuminemia grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypocalcemia grade 3, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypokalemia grade 3, 0.3%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypercalcemia grade 3, 0.4%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypomagnesemia grade 3, 0.4%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypermagnesemia grade 3, 0.9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hyponatremia grade 3, 0.9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Creatinine increased grade 4, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypermagnesemia grade 4, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypernatremia grade 4, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypokalemia grade 4, 0.1%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypercalcemia grade 4, 0.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypomagnesemia grade 4, 0.2%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Hypocalcemia grade 4, 0.9%
240 mg 1 times / day steady, oral
Recommended
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources: Page: p. 117
unhealthy, 52 years
n = 1408
Health Status: unhealthy
Condition: HER2-positive early-stage breast cancer
Age Group: 52 years
Sex: F
Population Size: 1408
Sources: Page: p. 117
Fatigue all grades, 1 patient
Disc. AE
180 mg 1 times / day steady, oral
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, 56.5 years (range: 46-90 years)
n = 6
Health Status: unhealthy
Condition: Breast cancer
Age Group: 56.5 years (range: 46-90 years)
Sex: F
Population Size: 6
Sources:
Diarrhea grade 3, 1 patient
DLT, Disc. AE
180 mg 1 times / day steady, oral
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, 56.5 years (range: 46-90 years)
n = 6
Health Status: unhealthy
Condition: Breast cancer
Age Group: 56.5 years (range: 46-90 years)
Sex: F
Population Size: 6
Sources:
Abdominal pain all grades, 21%
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Anorexia all grades, 33%
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Vomiting all grades, 49%
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Fatigue all grades, 49%
Disc. AE
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Nausea all grades, 54%
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Rash all grades, 8%
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Diarrhea all grades, 92%
Disc. AE
320 mg 1 times / day steady, oral
MTD
Dose: 320 mg, 1 times / day
Route: oral
Route: steady
Dose: 320 mg, 1 times / day
Sources:
unhealthy, 57 years (range: 34-80 years)
n = 39
Health Status: unhealthy
Condition: cancers
Age Group: 57 years (range: 34-80 years)
Sex: M+F
Population Size: 39
Sources:
Overview

OverviewOther

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
yes [IC50 1 uM]
yes (co-administration study)
yes [Inhibition 10 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: ketoconazole increased Cmax and AUC by 3.2- and 4.8-fold respectively, rifampin (a strong CYP3A4 inducer) decreased the Cmax and AUC of neratinib by 76% and 87%, respectively
Page: -
minor
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
2004 Jun 1
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma.
2011
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
2011 Mar 10
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
2013 Nov
Patents

Sample Use Guides

Patients who received 40, 80, or 120 mg experienced no dose-limiting toxicities. The study determined the maximum tolerated dose at 320 mg, with 240 mg being the therapeutic dose.
Route of Administration: Oral
both very low (10 nM) and physiologically attainable concentrations of neratinib (133 nM) significantly inhibited the autophosphorylation of HER2/neu and activation of S6 in primary carcinosarcoma cells
Substance Class Chemical
Created
by admin
on Sat Jun 26 10:01:48 UTC 2021
Edited
by admin
on Sat Jun 26 10:01:48 UTC 2021
Record UNII
JJH94R3PWB
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
NERATINIB
INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
2-BUTENAMIDE, N-(4-((3-CHLORO-4-(2-PYRIDINYLMETHOXY)PHENYL)AMINO)-3-CYANO-7-ETHOXY-6-QUINOLINYL)-4-(DIMETHYLAMINO)-, (2E)-
Systematic Name English
HKI-272
Code English
CDP-820
Code English
NERATINIB [WHO-DD]
Common Name English
NERATINIB [MART.]
Common Name English
NERATINIB [MI]
Common Name English
NERATINIB [USAN]
Common Name English
NERATINIB [INN]
Common Name English
(2E)-N-(4-((3-CHLORO-4-((PYRIDIN-2-YL)METHOXY)PHENYL)AMINO)-3-CYANO-7-ETHOXYQUINOLIN-6-YL)-4-(DIMETHYLAMINO)BUT-2-ENAMIDE
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 699119
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
WHO-ATC L01XE45
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
Code System Code Type Description
WIKIPEDIA
NERATINIB
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
ChEMBL
CHEMBL180022
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
PUBCHEM
9915743
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
DRUG CENTRAL
5252
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
EVMPD
SUB32232
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
EPA CompTox
698387-09-6
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
DRUG BANK
DB11828
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
INN
8878
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
FDA UNII
JJH94R3PWB
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
RXCUI
1940643
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
CAS
698387-09-6
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
NCI_THESAURUS
C49094
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
MERCK INDEX
M7827
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY Merck Index
LACTMED
Neratanib
Created by admin on Sat Jun 26 10:01:49 UTC 2021 , Edited by admin on Sat Jun 26 10:01:49 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
SALT/SOLVATE -> PARENT
CELL->INHIBITOR
CELL PROLIFERATION
IC50
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
BINDER->LIGAND
ex vivo protein binding of neratinib in human plasma samples from clinical study in healthy subjects as determined using ult racentrifugation was 88%
BINDING
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
OFF-TARGET->INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TRANSPORTER -> SUBSTRATE
OFF-TARGET->INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
CUMULATIVE EXCRETION
URINE
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
Percent inhibition of specific binding
TARGET -> INHIBITOR
OFF-TARGET->INHIBITOR
Radioligand binding assay
BINDING
IC50
TARGET -> INHIBITOR
Cyclin D1 expression in BT474 cells
INHIBITOR
IC50
CELL->INHIBITOR
CELL PROLIFERATION
IC50
TARGET -> INHIBITOR
HER2 ligand-independent receptor phosphorylation in BT474
IRREVERSIBLE INHIBITOR
IC50
OFF-TARGET->INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
TARGET -> INHIBITOR
EGFR-dependent receptor phosphorylation in A431 cells
IC50
OFF-TARGET->INHIBITOR
Radioligand binding assay
BINDING
IC50
METABOLIC ENZYME -> NON-INDUCER
TRANSPORTER -> INHIBITOR
IC50
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
METABOLIC ENZYME -> NON-INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
CUMULATIVE EXCRETION
FECAL
BINDER->LIGAND
In vitro, neratinib was highly bound (N 99 %) to human plasma proteins at cl inica l exposures. click to edit
BINDING
TARGET -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TRANSPORTER -> INHIBITOR
Neratinib concentration at 10 microM
INHIBITOR
Percent inhibition of specific binding
TARGET -> INHIBITOR
Radioligand binding assay
BINDING
IC50
Related Record Type Details
METABOLITE LESS ACTIVE -> PARENT
METABOLITE ACTIVE -> PARENT
Inhibition of HER2 kinase activity (Neratinib IC50 = 17 nM)
INHIBITOR
IC50
METABOLITE LESS ACTIVE -> PARENT
IC50 for HER2 kinase activity was up to 19 fold higher when compared to neratinib.
INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC Dose
PHARMACOKINETIC
Route of Administration
PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC Route of Administration
PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC Dose
PHARMACOKINETIC
Route of Administration
PHARMACOKINETIC
Cmax PHARMACOKINETIC Dose
PHARMACOKINETIC
Route of Administration
PHARMACOKINETIC