TEPOTINIB

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

Structure Search

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

HIDE SMILES / InChI

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

Description
Sources: http://biopharma.merckgroup.com/en/research_development/pipeline/pipeline.html
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

Targets

Primary Target	Pharmacology	Condition	Potency
Hepatocyte growth factor receptor 56 Target ID: CHEMBL3717 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25736998 \| https://www.ncbi.nlm.nih.gov/pubmed/23553846	Inhibitor 8504		3.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Lung adenocarcinoma 8 Sources: https://clinicaltrials.gov/ct2/show/NCT02864992	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf	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	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf	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

T_1/2

Value	Dose	Co-administered	Analyte	Population
32 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf https://clinicaltrials.gov/ct2/show/NCT01014936?term=NCT+01014936&draw=2&rank=1 https://pubmed.ncbi.nlm.nih.gov/31822497/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf https://clinicaltrials.gov/ct2/show/NCT01014936?term=NCT+01014936&draw=2&rank=1 https://pubmed.ncbi.nlm.nih.gov/31822497/	DLT: fatigue... Dose limiting toxicities: fatigue (grade 3, 14.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf https://clinicaltrials.gov/ct2/show/NCT01014936?term=NCT+01014936&draw=2&rank=1 https://pubmed.ncbi.nlm.nih.gov/31822497/
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	Disc. AE: Edema, Pleural effusion... AEs leading to discontinuation/dose reduction: Edema (5%) 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%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171

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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf https://clinicaltrials.gov/ct2/show/NCT01014936?term=NCT+01014936&draw=2&rank=1 https://pubmed.ncbi.nlm.nih.gov/31822497/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf https://clinicaltrials.gov/ct2/show/NCT01014936?term=NCT+01014936&draw=2&rank=1 https://pubmed.ncbi.nlm.nih.gov/31822497/
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214096s000lbl.pdf#page=5 https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214096Orig1s000MultidisciplineR.pdf#page=171

PubMed

Title	Date	PubMed
EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors.	2013 Jun 1	23553846

Patents

Sample Use Guides

In Vivo Use Guide

500 mg of tepotinib tablet once daily orally during each 21 day cycle

Route of Administration: Oral

In Vitro Use Guide

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 `Mon Mar 31 22:50:08 GMT 2025` Edited by `admin` on `Mon Mar 31 22:50:08 GMT 2025`
Record UNII	1IJV77EI07
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

tepotinib [INN]

Preferred Name

English

TEPOTINIB

Official Name

English

MSC-2156119

Code

English

MSC2156119

Code

English

EMD-1214063

Code

English

Tepotinib [WHO-DD]

Common Name

English

EMD1214063

Code

English

TEPOTINIB [USAN]

Common Name

English

MSC-2156119J

Code

English

BENZONITRILE, 3-(1,6-DIHYDRO-1-((3-(5-((1-METHYL-4-PIPERIDINYL)METHOXY)-2-PYRIMIDINYL)PHENYL)METHYL)-6-OXO-3-PYRIDAZINYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1967