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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H22F2N6O2.ClH
Molecular Weight 464.896
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Larotrectinib hydrochloride

SMILES

Cl.[H][C@@]1(CCCN1C2=NC3=C(NC(=O)N4CC[C@H](O)C4)C=NN3C=C2)C5=C(F)C=CC(F)=C5

InChI

InChIKey=UIHKJNYGFOAQDS-QLOBERJESA-N
InChI=1S/C21H22F2N6O2.ClH/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27;/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);1H/t14-,18+;/m0./s1

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C21H22F2N6O2
Molecular Weight 428.4352
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Larotrectinib (previously known as ARRY-470 and LOXO-101) is a potent, oral and selective investigational new drug in clinical development for the treatment of patients with cancers that harbor abnormalities involving the tropomyosin receptor kinases (TRKs). Larotrectinib is in phase II clinical trials for the treatment patients with solid tumors, non-Hodgkin lymphoma and for the pediatric patients with advanced solid or primary CNS tumors.

CNS Activity

Curator's Comment: Known to be CNS non-penetrant in mouse. Human data not available

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VITRAKVI

Approved Use

Vitrakvi is specifically indicated for the treatment of adult and pediatric patients with solid tumors that: • have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, • are metastatic or where surgical resection is likely to result in severe morbidity, and • have no satisfactory alternative treatments or that have progressed following treatment.

Launch Date

1.54310397E12
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
788 ng/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LAROTRECTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4351 ng × h/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LAROTRECTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.9 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LAROTRECTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Disc. AE: Brain edema, Intestinal perforation...
Other AEs: Fatigue, Nausea...
AEs leading to
discontinuation/dose reduction:
Brain edema (1 - 2)
Intestinal perforation (1 - 2)
Pericardial effusion (1 - 2)
Pleural effusion (1 - 2)
Small intestinal obstruction (1 - 2)
Dehydration (1 - 2)
Fatigue (1 - 2)
ALT increased (1 - 2)
AST increased (1 - 2)
Enterocutaneous fistula (1 - 2)
Amylase increased (1 - 2)
Lipase increased (1 - 2)
Muscular weakness (1 - 2)
Abdominal pain (1 - 2)
Asthenia (1 - 2)
Decreased appetite (1 - 2)
Dyspnea (1 - 2)
Hyponatremia (1 - 2)
Jaundice (1 - 2)
Syncope (1 - 2)
Vomiting (1 - 2)
Nausea (1 - 2)
Acute myeloid leukemia (1 - 2)
Other AEs:
Fatigue (>20)
Nausea (>20)
Dizziness (>20)
Vomiting (>20)
Anemia (>20)
AST increased (>20)
Cough (>20)
ALT increased (>20)
Constipation (>20)
Diarrhea (>20)
ALT increased (6%)
AST increased (6%)
Dizziness (3%)
Sources: Page: 6.1
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Other AEs: Fatigue, Pyrexia...
Other AEs:
Fatigue (all grades, 37%)
Pyrexia (all grades, 18%)
Edema peripheral (all grades, 15%)
Nausea (all grades, 29%)
Vomiting (all grades, 26%)
Constipation (all grades, 23%)
Diarrhea (all grades, 22%)
Abdominal pain (all grades, 13%)
Dizziness (all grades, 28%)
Headache (all grades, 14%)
Cough (all grades, 26%)
Dyspnea (all grades, 18%)
Nasal congestion (all grades, 10%)
Fatigue (grade 3-4, 3%)
Pyrexia (grade 3-4, 1%)
Nausea (grade 3-4, 1%)
Vomiting (grade 3-4, 1%)
Constipation (grade 3-4, 1%)
Diarrhea (grade 3-4, 2%)
Abdominal pain (grade 3-4, 2%)
Dizziness (grade 3-4, 1%)
Dyspnea (grade 3-4, 2%)
Weight increased (all grades, 15%)
Arthralgia (all grades, 14%)
Myalgia (all grades, 14%)
Muscular weakness (all grades, 13%)
Back pain (all grades, 12%)
Pain in extremity (all grades, 12%)
Decreased appetite (all grades, 13%)
Decreased appetite (all grades, 11%)
Weight increased (grade 3-4, 4%)
Arthralgia (grade 3-4, 1%)
Myalgia (grade 3-4, 1%)
Back pain (grade 3-4, 1%)
Pain in extremity (grade 3-4, 1%)
Decreased appetite (grade 3-4, 2%)
Decreased appetite (grade 3-4, 2%)
Sources: Page: Table 2
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Other AEs: ALT increased, AST increased...
Other AEs:
ALT increased (all grades, 45%)
AST increased (all grades, 45%)
Hypoalbuminemia (all grades, 35%)
Alkaline phosphatase increased (all grades, 30%)
Anemia (all grades, 42%)
Neutropenia (all grades, 23%)
ALT increased (grade 3-4, 3%)
AST increased (grade 3-4, 3%)
Hypoalbuminemia (grade 3-4, 2%)
Alkaline phosphatase increased (grade 3-4, 3%)
Anemia (grade 3-4, 10%)
Neutropenia (grade 3-4, 7%)
Sources: Page: Table 3
150 mg 2 times / day steady, oral
Higher than recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 7
Sources:
DLT: Alanine aminotransferase increased, Aspartate aminotransferase increased...
Dose limiting toxicities:
Alanine aminotransferase increased (1 patient)
Aspartate aminotransferase increased (1 patient)
Sources:
200 mg 2 times / day steady, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult
n = 6
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 6
Sources:
DLT: Dizziness...
Dose limiting toxicities:
Dizziness (1 patient)
Sources:
200 mg 2 times / day steady, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources: Page: 91
unhealthy, adult
n = 6
Health Status: unhealthy
Condition: solid tumor
Age Group: adult
Sex: unknown
Population Size: 6
Sources: Page: 91
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 6
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 6
Sources:
DLT: Dizziness...
Dose limiting toxicities:
Dizziness (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
ALT increased 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
AST increased 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Abdominal pain 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Acute myeloid leukemia 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Amylase increased 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Asthenia 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Brain edema 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Decreased appetite 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Dehydration 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Dyspnea 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Enterocutaneous fistula 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Fatigue 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Hyponatremia 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Intestinal perforation 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Jaundice 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Lipase increased 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Muscular weakness 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Nausea 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Pericardial effusion 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Pleural effusion 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Small intestinal obstruction 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Syncope 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Vomiting 1 - 2
Disc. AE
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Dizziness 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
ALT increased 6%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
AST increased 6%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
ALT increased >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
AST increased >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Anemia >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Constipation >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Cough >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Diarrhea >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Dizziness >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Fatigue >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Nausea >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Vomiting >20
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: 6.1
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: 6.1
Nasal congestion all grades, 10%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Decreased appetite all grades, 11%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Back pain all grades, 12%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Pain in extremity all grades, 12%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Abdominal pain all grades, 13%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Decreased appetite all grades, 13%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Muscular weakness all grades, 13%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Arthralgia all grades, 14%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Headache all grades, 14%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Myalgia all grades, 14%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Edema peripheral all grades, 15%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Weight increased all grades, 15%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Dyspnea all grades, 18%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Pyrexia all grades, 18%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Diarrhea all grades, 22%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Constipation all grades, 23%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Cough all grades, 26%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Vomiting all grades, 26%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Dizziness all grades, 28%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Nausea all grades, 29%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Fatigue all grades, 37%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Arthralgia grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Back pain grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Constipation grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Dizziness grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Myalgia grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Nausea grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Pain in extremity grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Pyrexia grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Vomiting grade 3-4, 1%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Abdominal pain grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Decreased appetite grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Decreased appetite grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Diarrhea grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Dyspnea grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Fatigue grade 3-4, 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Weight increased grade 3-4, 4%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 2
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 2
Neutropenia all grades, 23%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Alkaline phosphatase increased all grades, 30%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Hypoalbuminemia all grades, 35%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Anemia all grades, 42%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
ALT increased all grades, 45%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
AST increased all grades, 45%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Anemia grade 3-4, 10%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Hypoalbuminemia grade 3-4, 2%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
ALT increased grade 3-4, 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
AST increased grade 3-4, 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Alkaline phosphatase increased grade 3-4, 3%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Neutropenia grade 3-4, 7%
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources: Page: Table 3
unhealthy, 28 - 82 years
n = 176
Health Status: unhealthy
Condition: solid tumor
Age Group: 28 - 82 years
Sex: M+F
Population Size: 176
Sources: Page: Table 3
Alanine aminotransferase increased 1 patient
DLT
150 mg 2 times / day steady, oral
Higher than recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 7
Sources:
Aspartate aminotransferase increased 1 patient
DLT
150 mg 2 times / day steady, oral
Higher than recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 7
Sources:
Dizziness 1 patient
DLT
200 mg 2 times / day steady, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult
n = 6
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 6
Sources:
Dizziness 1 patient
DLT
100 mg 2 times / day steady, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, adult
n = 6
Health Status: unhealthy
Condition: solid tumours
Age Group: adult
Sex: unknown
Population Size: 6
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes (co-administration study)
Comment: larotrectinib increased midazolam both AUC and Cmax by 1.7-fold
Page: 94.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
yes [Km >300 uM]
yes [Km >300 uM]
yes (co-administration study)
Comment: rifampin increased larotrectinib AUC by 1.7-fold and Cmax by 1.8-fold
Page: 93, 94, 106
yes
yes (co-administration study)
Comment: coadministration with midazolam increased midazolam AUC and Cmax by 1.7-fold; itraconazole increased larotrectinib AUC by 4.3-fold and Cmax by 2.8-fold; rifampin decreased larotrectinib AUC by 81% and Cmax by 71%
Page: 95, 104, 105
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Targeting NTRK fusion in non-small cell lung cancer: rationale and clinical evidence.
2017 Jun
Rapid Response to Larotrectinib (LOXO-101) in an Adult Chemotherapy-Naive Patients With Advanced Triple-Negative Secretory Breast Cancer Expressing ETV6-NTRK3 Fusion.
2018 Jun

Sample Use Guides

Oral capsule of LOXO-101 (ARRY-470 (FREE BASE)) - 100mg BID
Route of Administration: Oral
ARRY-470 is a selective kinase inhibitor with nanomolar activity against TRKA/B/C but no other significant kinase inhibition below 1000nM. Treatment of cells expressing MPRIP- or CD74-NTRK1 with ARRY-470, CEP-701 and, to a lesser extent, crizotinib, inhibited autophosphorylation of RIP-TRKA and CD74-TRKA. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.
Substance Class Chemical
Created
by admin
on Fri Jul 07 00:48:36 UTC 2023
Edited
by admin
on Fri Jul 07 00:48:36 UTC 2023
Record UNII
E4BVS4JUA7
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Larotrectinib hydrochloride
Common Name English
1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, hydrochloride (1:1), (3S)-
Systematic Name English
Code System Code Type Description
FDA UNII
E4BVS4JUA7
Created by admin on Fri Jul 07 00:48:36 UTC 2023 , Edited by admin on Fri Jul 07 00:48:36 UTC 2023
PRIMARY
CAS
1919868-83-9
Created by admin on Fri Jul 07 00:48:36 UTC 2023 , Edited by admin on Fri Jul 07 00:48:36 UTC 2023
PRIMARY
PUBCHEM
121333501
Created by admin on Fri Jul 07 00:48:36 UTC 2023 , Edited by admin on Fri Jul 07 00:48:36 UTC 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE