Updated Results for Investigational Therapy Tepotinib Presented at WCLC 2019

PR80430

DARMSTADT, Germany, Sept. 9, 2019 /PRNewswire=KYODO JBN/--

- Results include progression-free survival and overall survival data from

Phase Ib/II INSIGHT study

- Phase II INSIGHT 2 study now open for enrollment for patients with locally

advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth

factor receptor (EGFR) mutation and select MET dysregulations

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or the UK

Merck, a leading science and technology company, announced today important

milestones for two combination studies of the investigational therapy

tepotinib* in locally advanced or metastatic non-small cell lung cancer (NSCLC)

with epidermal growth factor receptor (EGFR) mutation and select MET

dysregulations. These include progression-free survival (PFS) and overall

survival (OS) data from the Phase Ib/II INSIGHT study of tepotinib plus the

EGFR inhibitor gefitinib, and an update that the Phase II INSIGHT 2 study of

tepotinib plus tyrosine kinase inhibitor (TKI) osimertinib is now open for

enrollment. Tepotinib, discovered in-house at Merck, is an investigational oral

MET inhibitor that underscores Merck's strategic focus on delivering innovative

precision medicines to patients with cancer.

"The consistency of results across the clinical development program for

tepotinib continues to highlight the potential for this investigational therapy

in targeting select NSCLC mutations and alterations that are associated with

aggressive tumor behavior and poor clinical prognosis," said Luciano Rossetti,

Global Head of Research & Development for the Biopharma business of Merck. "We

are committed to progressing tepotinib as part of our precision medicine

strategy and our work to deliver new therapeutic options for people living with

difficult-to-treat cancers, including NSCLC."

Data were presented on September 8 at the 2019 World Conference on Lung Cancer

hosted by the International Association for the Study of Lung Cancer (#WCLC19),

including 18-month follow-up data from the Phase Ib/II INSIGHT study evaluating

tepotinib in combination with the EGFR inhibitor gefitinib compared with

standard chemotherapy in patients with EGFR-mutant locally advanced or

metastatic NSCLC with MET protein overexpression or MET gene amplification who

had disease progression after receiving an EGFR TKI. These results include

updated PFS data as well as the first OS data for patients in both the MET

overexpression and MET amplification cohorts of this study. These data will be

submitted for future publication in a medical journal.

Additionally, Merck today announced it is now enrolling patients in the Phase

II INSIGHT 2 study investigating tepotinib in combination with the TKI

osimertinib in patients with EGFR-mutated, MET-amplified, locally advanced or

metastatic NSCLC with acquired resistance to prior EGFR TKI therapy. The

decision to initiate the INSIGHT 2 study is based on the encouraging findings

seen in the Phase Ib/II INSIGHT study. Early data from this study presented at

the 2019 American Association for Cancer Research Annual Meeting demonstrated

clinical anti-tumor activity for the combination of tepotinib plus gefitinib

compared with chemotherapy in patients with EGFR-mutant locally advanced or

metastatic NSCLC with MET gene amplification who had disease progression after

receiving an EGFR TKI, based on both investigator assessment and independent

review committee assessment. Related grade ≥3 treatment-emergent adverse

events (TEAEs) were reported in 6 (50.0%) patients treated with tepotinib plus

gefitinib and 5 (71.4%) patients receiving chemotherapy. The most common

related TEAEs in the tepotinib plus gefitinib arm were diarrhea (50.0%) and

amylase increased (41.7%) and in the chemotherapy arm were anemia (57.1%),

white blood cell count decreased (57.1%), neutrophil count decreased (57.1%)

and nausea (42.9%). No new safety signals were observed.1 These data also

indicate that MET amplification may be a biomarker predictive of response to

tepotinib.

Tepotinib is also being investigated in the ongoing Phase II VISION study,

evaluating tepotinib in advanced or metastatic NSCLC patients harboring MET

alterations (MET exon 14 skipping alterations and MET amplifications) as

monotherapy. Results from this study were presented in an oral presentation at

the 2019 American Society of Clinical Oncology (ASCO) Annual Meeting.2 In March

2018, tepotinib's potential was recognized by the Japanese Ministry of Health,

Labour and Welfare (MHLW), which granted SAKIGAKE 'fast-track' designation for

tepotinib in advanced NSCLC harboring MET exon 14 skipping alterations.

For more information on these studies, visit ClinicalTrials.gov and search

identifier NCT01982955 for the Phase Ib/II INSIGHT study, NCT03940703 for the

Phase II INSIGHT 2 study or NCT02864992 for the Phase II VISION study.

*Tepotinib is the recommended International Nonproprietary Name (INN) for the

MET kinase inhibitor (MSC2156119J). Tepotinib is currently under clinical

investigation and not approved for any use anywhere in the world.

About Non-Small Cell Lung Cancer

With 2 million cases diagnosed annually, lung cancer (including trachea,

bronchus and lung) is the most common type of cancer worldwide, and the leading

cause of cancer-related death, with 1.7 million mortality cases worldwide.3

Alterations of the MET signaling pathway, including MET exon 14 skipping

alterations and MET amplifications, occur in 3-5% of NSCLC cases.4-6

About Tepotinib

Tepotinib, discovered in-house at Merck, is an investigational oral MET

inhibitor that is designed to inhibit the oncogenic MET receptor signaling

caused by MET (gene) alterations, including both MET exon 14 skipping

alterations and MET amplifications, or MET protein overexpression. It has been

designed to have a highly selective mechanism of action, with the potential to

improve outcomes in aggressive tumors that have a poor prognosis and harbor

these specific alterations.

Tepotinib is currently being investigated in NSCLC and Merck is actively

assessing the potential of investigating tepotinib in combination with novel

therapies and in other tumor indications.

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About Merck

Merck, a leading science and technology company, operates across healthcare,

life science and performance materials. Around 52,000 employees work to make a

positive difference to millions of people's lives every day by creating more

joyful and sustainable ways to live. From advancing gene editing technologies

and discovering unique ways to treat the most challenging diseases to enabling

the intelligence of devices – the company is everywhere. In 2018, Merck

generated sales of € 14.8 billion in 66 countries.

Scientific exploration and responsible entrepreneurship have been key to

Merck's technological and scientific advances. This is how Merck has thrived

since its founding in 1668. The founding family remains the majority owner of

the publicly listed company. Merck holds the global rights to the Merck name

and brand. The only exceptions are the United States and Canada, where the

business sectors of Merck operate as EMD Serono in healthcare, MilliporeSigma

in life science, and EMD Performance Materials.

References

1. Yang J, et al. AACR 2019 abstract CT193; NCT01982955.

2. Paik P, et al. J Clin Oncol 2019;37: (suppl; abstr 9005).

3. Bray F, et al. CA Cancer J Clin. Global cancer statistics 2018: GLOBOCAN

estimates of incidence and mortality worldwide for 36 cancers in 185 countries.

2018;68(6):394–424. https://doi.org/10.3322/caac.21492 PMID:30207593

4. Reungwetwattana T, et al. Lung Cancer 2017;103:27-37.

5. Mo HN, et al. Chronic Dis Transl Med 2017; 3(3):148-153.

6. Lutterbach B, et al. Cancer Res 2007;67:2081–8.

Contact:

Media Relations

Annemarie.Eckhardt@merckgroup.com  

+49-6151-72-26560

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Source: Merck