Tepotinib

Tepotinib, sold under the brand name Tepmetko, is a medication used for the treatment of adults with non-small cell lung cancer (NSCLC).[3][4][6]

Tepotinib
Clinical data
Trade namesTepmetko
Other namesEMD-1214063
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: D[1]
  • Not recommended
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
IUPAC name
  • 3-{1-[(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin2-yl}phenyl)methyl]-6-oxo-1,6-dihydropyridazin3-yl}benzonitrile
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H28N6O2
Molar mass492.583 g·mol−1
3D model (JSmol)
SMILES
  • CN1CCC(COc2cnc(-c3cccc(Cn4nc(-c5cccc(C#N)c5)ccc4=O)c3)nc2)CC1
InChI
  • 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
  • Key:AHYMHWXQRWRBKT-UHFFFAOYSA-N

Tepotinib first received marketing approval in Japan, in March 2020, as a "line-agnostic" drug, meaning it is approved both for treatment-naive patients and for those in whom previous attempts at treatment have failed.[7] U.S. approval followed in February 2021. It is the second therapy approved by the U.S. Food and Drug Administration (FDA) to treat non-small cell lung cancer with these particular mutations, after capmatinib.[8]

Medical uses

Tepotinib is indicated for the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping.[3][4]

Adverse effects

The most common side effects seen in clinical trials were edema, fatigue, nausea, diarrhea, muscle aches, and shortness of breath. Like capmatinib, tepotinib can also cause interstitial lung disease and liver damage, and is toxic to a developing fetus.[4] The most common treatment-related adverse effect in a 2021 study were peripheral edema (54.1%), nausea (20.0%), diarrhea (19.6%), blood creatinine increased (17.6%), and hypoalbuminemia (14.5%), which were 'mostly mild or moderate'.[9]

Society and culture

On 16 December 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Tepmetko, intended for the treatment of patients with advanced non-small cell lung cancer (NSCLC) harboring alterations leading to mesenchymal-epithelial transition factor gene exon 14 (METex14) skipping.[10] The applicant for this medicinal product is Merck Europe B.V.[10] Tepotinib (Tepmetko) was approved for medical use in the European Union in February 2022.[5]

References
  1. "Tepmetko APMDS". Therapeutic Goods Administration (TGA). 27 January 2022. Retrieved 5 February 2022.
  2. "Summary Basis of Decision (SBD) for Tepmetko". Health Canada. Archived from the original on 29 May 2022. Retrieved 29 May 2022.
  3. "Tepmetko- tepotinib hydrochloride tablet". DailyMed. Archived from the original on 27 November 2021. Retrieved 13 February 2021.
  4. "FDA grants accelerated approval to tepotinib for metastatic non-small cell lung cancer". Food and Drug Administration. 3 February 2021. Archived from the original on 3 February 2021. Retrieved 3 February 2021. This article incorporates text from this source, which is in the public domain.
  5. "Tepmetko EPAR". European Medicines Agency (EMA). 14 December 2021. Archived from the original on 5 May 2022. Retrieved 5 May 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. "FDA Approves Tepmetko as the First and Only Once-daily Oral MET Inhibitor for Patients with Metastatic NSCLC with METex14 Skipping Alterations". EMD Serono (Press release). 3 February 2021. Archived from the original on 4 February 2021. Retrieved 3 February 2021.
  7. "Tepmetko (Tepotinib) Approved in Japan for Advanced NSCLC with METex14 Skipping Alterations" (Press release). Merck KGaA. 25 March 2020. Retrieved 3 February 2021.
  8. Mathieu LN, Larkins E, Akinboro O, Roy P, Amatya AK, Fiero MH, et al. (January 2022). "FDA Approval Summary: Capmatinib and Tepotinib for the Treatment of Metastatic NSCLC Harboring MET Exon 14 Skipping Mutations or Alterations". Clin Cancer Res. 28 (2): 249–254. doi:10.1158/1078-0432.CCR-21-1566. PMID 34344795. S2CID 236915283.
  9. Morise, Masahiro; Sakai, Hiroshi; Veillon, Remi; Le, Xiuning; Felip, Enriqueta; Garassino, Marina Chiara; Cortot, Alexis B.; Smit, Egbert; Park, Keunchil; Griesinger, Frank; Britschgi, Christian (July 2021). "O13-4 Tepotinib safety in MET exon 14 (METex14) skipping NSCLC: Updated results from the VISION trial". Annals of Oncology. 32: S291. doi:10.1016/j.annonc.2021.05.541. ISSN 0923-7534. S2CID 237785148. Archived from the original on 30 September 2022. Retrieved 4 October 2021.
  10. "Tepmetko: Pending EC decision". European Medicines Agency. 17 December 2021. Archived from the original on 18 December 2021. Retrieved 18 December 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

Further reading
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