Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H28N6O2 |
Molecular Weight | 492.5716 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC(COC2=CN=C(N=C2)C3=CC(CN4N=C(C=CC4=O)C5=CC(=CC=C5)C#N)=CC=C3)CC1
InChI
InChIKey=AHYMHWXQRWRBKT-UHFFFAOYSA-N
InChI=1S/C29H28N6O2/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30/h2-9,14-15,17-18,21H,10-13,19-20H2,1H3
Molecular Formula | C29H28N6O2 |
Molecular Weight | 492.5716 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25736998
https://www.ncbi.nlm.nih.gov/pubmed/23553846
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25736998
https://www.ncbi.nlm.nih.gov/pubmed/23553846
Tepotinib is an investigational small molecule inhibitor of the c-Met receptor tyrosine kinase. Alterations of the c-Met signaling pathway are found in various cancer types and correlate with aggressive tumor behavior and poor clinical prognosis. Tepotinib is a potent and selective c-Met inhibitor, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib is currently in Phase I/II trials in liver cancer and lung cancer.
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
244.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
215 mg single, oral dose: 215 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
301.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
442.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
807.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
215 mg 1 times / day steady-state, oral dose: 215 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
610.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
996.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
500 mg 1 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1291 ng/mL |
450 mg 1 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
57 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
330 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
863 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
1400 mg single, oral dose: 1400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
113 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
30 mg 1 times / day steady-state, oral dose: 30 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
943 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
500 mg 1 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
1805 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
1400 mg 1 times / day steady-state, oral dose: 1400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
89 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
60 mg 3 times / week multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
178 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
130 mg 3 times / week multiple, oral dose: 130 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
722 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
315 mg 3 times / week multiple, oral dose: 315 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4060.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
215 mg single, oral dose: 215 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5412.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
8235 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
16088.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
215 mg 1 times / day steady-state, oral dose: 215 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13313.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
21509 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32328660/ |
500 mg 1 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
27438 ng × h/mL |
450 mg 1 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
849 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
5918 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
15542 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
1400 mg single, oral dose: 1400 mg route of administration: Oral experiment type: SINGLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
2267 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
30 mg 1 times / day steady-state, oral dose: 30 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
20169 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
500 mg 1 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
39284 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
1400 mg 1 times / day steady-state, oral dose: 1400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
3032 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
60 mg 3 times / week multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
5306 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
130 mg 3 times / week multiple, oral dose: 130 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
27760 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31822497/ |
315 mg 3 times / week multiple, oral dose: 315 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TEPOTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
32 h |
450 mg 1 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2% |
450 mg 1 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TEPOTINIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Doses
Dose | Population | Adverse events |
---|---|---|
1400 mg 1 times / day multiple, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: multiple Dose: 1400 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
DLT: fatigue... Dose limiting toxicities: fatigue (grade 3, 14.3%) Sources: |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Edema, Pleural effusion... AEs leading to discontinuation/dose reduction: Edema (5%) Sources: Pleural effusion (2%) Dyspnea (1.6%) General health deterioration (1.6%) Pneumonitis (1.2%) Edema (23%) Increased blood creatinine (6%) Pleural effusion (4.3%) Increased ALT (3.1%) Pneumonia (2.4%) Edema (19%) Pleural effusion (2.7%) Increased blood creatinine (2.7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
fatigue | grade 3, 14.3% DLT |
1400 mg 1 times / day multiple, oral Highest studied dose Dose: 1400 mg, 1 times / day Route: oral Route: multiple Dose: 1400 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Pneumonitis | 1.2% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Dyspnea | 1.6% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
General health deterioration | 1.6% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Edema | 19% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | 2% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pneumonia | 2.4% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Increased blood creatinine | 2.7% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | 2.7% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Edema | 23% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Increased ALT | 3.1% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | 4.3% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Edema | 5% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Increased blood creatinine | 6% Disc. AE |
450 mg 1 times / day multiple, oral Recommended Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02864992
500 mg of tepotinib tablet once daily orally during each 21 day cycle
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23553846
Tepotinib inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with Tepotinib induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. Tepotinib effectively blocks phosphorylation of the major downstream effectors of the c-Met enzyme, such as Grb2, Gab1, Sos, PLCγ, and phosphoinositide 3-kinase, in EBC-1, MKN-45, and Hs746T cells in the range of 1 to 10 nM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:50:08 GMT 2025
by
admin
on
Mon Mar 31 22:50:08 GMT 2025
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Record UNII |
1IJV77EI07
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Record Status |
Validated (UNII)
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Record Version |
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Preferred Name | English | ||
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Code | English | ||
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NCI_THESAURUS |
C1967
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FDA ORPHAN DRUG |
679719
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NCI_THESAURUS |
C129825
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25171648
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DTXSID70149132
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Tepotinib
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DB15133
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CHEMBL3402762
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HI-32
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100000175303
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C88314
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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CUMULATIVE EXCRETION |
URINE
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TARGET -> INHIBITOR |
IC50
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CUMULATIVE EXCRETION |
FECAL
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TRANSPORTER -> INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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BINDER->LIGAND |
Protein binding of tepotinib is 98% and is independent of drug concentration at clinically relevant exposures.
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TARGET -> INHIBITOR |
Tepotinib also inhibited melatonin 2 and
imidazoline 1 receptors at clinically achievable concentrations.
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SALT/SOLVATE -> PARENT |
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EXCRETED UNCHANGED |
FECAL
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EXCRETED UNCHANGED |
URINE
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TRANSPORTER -> SUBSTRATE |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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ORAL ADMINISTRATION PHARMACOKINETIC PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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