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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H19FN6O2.C2H4O2
Molecular Weight 466.4649
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LORLATINIB ACETATE

SMILES

CC(O)=O.C[C@H]1OC2=CC(=CN=C2N)C3=C(C#N)N(C)N=C3CN(C)C(=O)C4=CC=C(F)C=C14

InChI

InChIKey=BLNAIBLTPYGILH-RFVHGSKJSA-N
InChI=1S/C21H19FN6O2.C2H4O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12;1-2(3)4/h4-7,9,11H,10H2,1-3H3,(H2,24,25);1H3,(H,3,4)/t11-;/m1./s1

HIDE SMILES / InChI

Molecular Formula C21H19FN6O2
Molecular Weight 406.413
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula C2H4O2
Molecular Weight 60.052
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including: http://adisinsight.springer.com/drugs/800039198 | http://meetinglibrary.asco.org/content/143329-156

Lorlatinib is an investigational medicine that inhibits the anaplastic lymphoma kinase (ALK) and ROS1 proto-oncogene. Lorlatinib was specifically designed to inhibit tumor mutations that drive resistance to other ALK inhibitors. Lorlatinib has in vitro activity against ALK and number of other tyrosine kinase receptor related targets including ROS1, TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK. Lorlatinib demonstrated in vitro activity against multiple mutant forms of the ALK enzyme, including some mutations detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors. Moreover, lorlatinib possesses the capability to cross the blood-brain barrier, allowing it to reach and treat progressive or worsening brain metastases as well. Lorlatinib is a third-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) indicated for the treatment of patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on a) the prior use of crizotinib and at least one other ALK inhibitor for metastatic disease, or b) the prior use of alectinib as the first ALK inhibitor therapy for metastatic disease, or c) the prior use of certinib as the first ALK inhibitor therapy for metastatic disease.

Originator

Curator's Comment: # Pfizer

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Lorbrena

Approved Use

LORBRENA is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on crizotinib and at least one other ALK inhibitor for metastatic disease; or alectinib as the first ALK inhibitor therapy for metastatic disease; or ceritinib as the first ALK inhibitor therapy for metastatic disease .

Launch Date

1.54111679E12
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
577 ng/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORLATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5650 ng × h/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORLATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
24 h
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORLATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
34%
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORLATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 51 years
n = 3
Health Status: unhealthy
Age Group: 51 years
Sex: M+F
Population Size: 3
Sources:
Disc. AE: Cognitive disorder, Aphasia...
AEs leading to
discontinuation/dose reduction:
Cognitive disorder (2 patients)
Aphasia (2 patients)
Irritability (2 patients)
Sources:
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Disc. AE: Respiratory failure, Dyspnea...
AEs leading to
discontinuation/dose reduction:
Respiratory failure (1.4%)
Dyspnea (0.7%)
Myocardial infarction (0.7%)
Cognitive disorder NEC (0.7%)
Mood disorder (0.7%)
Edema (7%)
Hypertriglyceridemia (6%)
Peripheral neuropathy (5%)
Cognitive disorder NEC (4.4%)
Lipase increased (3.7%)
Hypercholesterolemia (3.4%)
Mood disorder (3.1%)
Dyspnea (2.7%)
Pneumonia (2.7%)
Hypertension (2%)
Edema (6%)
Peripheral neuropathy (4.7%)
Cognitive disorder NEC (4.1%)
Mood disorder (3.1%)
Sources:
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Disc. AE: Acute leukemia, Brain compression...
AEs leading to
discontinuation/dose reduction:
Acute leukemia (0.3%)
Brain compression (0.3%)
Embolism (0.3%)
Hallucinations (0.3%)
Headache (0.3%)
Hydrocephalus (0.3%)
Hypoxia (0.3%)
Leukocytosis (0.3%)
Loss of consciousness (0.3%)
Lung infection (0.3%)
Mental status changes (0.3%)
Parkinsonian gait (0.3%)
Peripheral swelling (0.3%)
Thrombocytopenia (0.3%)
Tinnitus (0.3%)
Vomiting (0.3%)
Hypertriglyceridemia (1.7%)
Arthralgia (1%)
Dizziness (1%)
Hallucinations (1%)
Weight increased (1%)
Blood amylase increased (1.7%)
Diarrhea (1.7%)
Fatigue (1.7%)
Asthenia (1.7%)
Dizziness (1.4%)
Fall (1.4%)
Hyperglycemia (1.4%)
Pyrexia (1.4%)
ALT increased (1%)
Anemia (1%)
Arthralgia (1%)
Atrial fibrillation (1%)
Back pain (1%)
Ejection fraction decreased (1%)
Mental status changes (1%)
Pericardial effusion (1%)
Pleural effusion (1%)
Acute respiratory failure (1%)
Respiratory failure (1%)
Vomiting (1%)
Weight increased (1%)
Sources: Page: p. 164
AEs

AEs

AESignificanceDosePopulation
Aphasia 2 patients
Disc. AE
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 51 years
n = 3
Health Status: unhealthy
Age Group: 51 years
Sex: M+F
Population Size: 3
Sources:
Cognitive disorder 2 patients
Disc. AE
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 51 years
n = 3
Health Status: unhealthy
Age Group: 51 years
Sex: M+F
Population Size: 3
Sources:
Irritability 2 patients
Disc. AE
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 51 years
n = 3
Health Status: unhealthy
Age Group: 51 years
Sex: M+F
Population Size: 3
Sources:
Cognitive disorder NEC 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Dyspnea 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Mood disorder 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Myocardial infarction 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Respiratory failure 1.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Hypertension 2%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Dyspnea 2.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Pneumonia 2.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Mood disorder 3.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Mood disorder 3.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Hypercholesterolemia 3.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Lipase increased 3.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Cognitive disorder NEC 4.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Cognitive disorder NEC 4.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Peripheral neuropathy 4.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Peripheral neuropathy 5%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Edema 6%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Hypertriglyceridemia 6%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Edema 7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources:
Acute leukemia 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Brain compression 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Embolism 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hallucinations 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Headache 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hydrocephalus 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hypoxia 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Leukocytosis 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Loss of consciousness 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Lung infection 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Mental status changes 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Parkinsonian gait 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Peripheral swelling 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Thrombocytopenia 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Tinnitus 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Vomiting 0.3%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
ALT increased 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Acute respiratory failure 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Anemia 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Arthralgia 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Arthralgia 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Atrial fibrillation 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Back pain 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Dizziness 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Ejection fraction decreased 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hallucinations 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Mental status changes 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Pericardial effusion 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Pleural effusion 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Respiratory failure 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Vomiting 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Weight increased 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Weight increased 1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Dizziness 1.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Fall 1.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hyperglycemia 1.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Pyrexia 1.4%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Asthenia 1.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Blood amylase increased 1.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Diarrhea 1.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Fatigue 1.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
Hypertriglyceridemia 1.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources: Page: p. 164
unhealthy, 53 years (range: 19 - 85 years)
n = 295
Health Status: unhealthy
Condition: non-small cell lung cancer (NSCLC)
Age Group: 53 years (range: 19 - 85 years)
Sex: M+F
Population Size: 295
Sources: Page: p. 164
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [EC50 2.85 uM]
yes (co-administration study)
Comment: rifampin reduced mean lorlatinib AUC by 85% and Cmax by 76%
Page: 85.0
yes
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: lorlatinib reduced midazolam AUC by 64% and Cmax by 50%
Page: 14.0
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
Tackling ALK in non-small cell lung cancer: the role of novel inhibitors.
2016 Jun
Patents

Sample Use Guides

The recommended dosage is 100 mg orally once daily.
Route of Administration: Oral
Mutant ALKG1128A, ALKF1174L, ALKR1192P, ALKF1245C and ALKR1275Q responded to PF-06463922 with IC50 values similar to that of wild-type, two mutants – ALKI1171N and ALKY1278S – were more resistant, with 4- and 2.8-fold (3.21 nM and 2.27 nM) respectively of the IC50 of wild-type ALK kinase.
Substance Class Chemical
Created
by admin
on Sat Dec 16 15:07:43 UTC 2023
Edited
by admin
on Sat Dec 16 15:07:43 UTC 2023
Record UNII
TE9WI16FEU
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LORLATINIB ACETATE
Common Name English
PF-06463922 ACETATE
Code English
2H-4,8-METHENOPYRAZOLO(4,3-H)(2,5,11)BENZOXADIAZACYCLOTETRADECINE-3-CARBONITRILE, 7-AMINO-12-FLUORO-10,15,16,17-TETRAHYDRO-2,10,16-TRIMETHYL-15-OXO-, (10R)-, ACETATE
Systematic Name English
Code System Code Type Description
FDA UNII
TE9WI16FEU
Created by admin on Sat Dec 16 15:07:43 UTC 2023 , Edited by admin on Sat Dec 16 15:07:43 UTC 2023
PRIMARY
CAS
1924207-18-0
Created by admin on Sat Dec 16 15:07:43 UTC 2023 , Edited by admin on Sat Dec 16 15:07:43 UTC 2023
PRIMARY
PUBCHEM
124203822
Created by admin on Sat Dec 16 15:07:43 UTC 2023 , Edited by admin on Sat Dec 16 15:07:43 UTC 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY