Updated Results for Investigational Therapy Tepotinib Presented at WCLC 2019

- 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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Darmstadt, Germany (ots/PRNewswire) - 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.

All Merck Press Releases are distributed by e-mail at the same
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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 EUR 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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