Merck Presents Update on Tepotinib in Advanced Lung Cancer at ASCO 2018

Darmstadt, Germany (ots/PRNewswire) -

ASCO Abstract #

Tepotinib (c-Met kinase inhibitor): 9082, 9016; M7824 (TGF-ß
trap/anti-PD-L1): 3007, 9017, 2566; M2698 (dual p70S6k/Akt
inhibitor): 2584; M6620 (ATR inhibitor): 2549; M3814 (DNA-PK): 2518

Not intended for UK- or US-based media

- Data from an ongoing Phase II tepotinib study show anti-tumor
clinical activity in patients with advanced non-small cell lung
cancer harboring MET exon 14 skipping mutations
- Patients with advanced lung cancer harboring MET exon 14 mutations
currently have a poor prognosis and limited treatment options
- Safety data are consistent with data previously reported, with no
new safety signals identified

Merck, a leading science and technology company, today announced
that the investigational, targeted therapy tepotinib[*] has shown
clinical activity in an ongoing Phase II study of patients with
advanced non-small cell lung cancer (NSCLC) harboring MET exon 14
skipping mutations. Data from the VISION trial will be presented
during the American Society of Clinical Oncology (ASCO) 2018 Annual
Meeting in Chicago, June 1-5, 2018.

"Patients living with advanced non-small cell lung cancer
harboring MET exon 14 skipping mutations have limited treatment
options available to them and typically face poor clinical outcomes,"
said investigator Enriqueta Felip, M.D., Medical Oncologist, Vall
d'Hebron Institute of Oncology (VHIO). "More than half of the
patients in the Phase II VISION study had an investigator-assessed
confirmed response, demonstrating the potential of tepotinib and the
need to further evaluate this precision medicine option."

Initial data from the Phase II VISION study of tepotinib in
patients living with advanced NSCLC harboring MET exon 14 skipping
mutations will be presented today at ASCO during the "Lung
Cancer-Non-Small Cell Metastatic" poster discussion session, 11:30
a.m. - 12:45 p.m. CDT. Treatment with tepotinib led to a confirmed
complete response (CR) or confirmed partial response (PR) in 53.6%
(15/28) and stable disease (SD) in 17.9% (5/28) of patients based on
investigator assessment. Based on independent assessment of updated
data from 28 patients (patients with at least 2 post-baseline
assessments or who discontinued for any reason), 42.9% (12/28) had a
PR and 21.4% (6/28) had SD.

In this ongoing study, the safety data are consistent with that
observed in previous studies; no new safety signals have been
identified to date. A total of 26 out of 38 patients with data
available experienced treatment-related adverse events (TRAEs), most
commonly Grade 1/2 peripheral edema (13 patients) and diarrhea (10
patients). Seven patients reported Grade 3 TRAEs, including
asymptomatic amylase increase (2 patients) and one instance each of:
asthenia, generalized edema, aspartate aminotransferase increase,
gamma-glutamyl transferase increase, lipase increase, hyperkalemia,
dizziness and pneumonia. Four patients experienced serious TRAEs,
with one instance of pneumonia, generalized edema, asthenia and
dizziness, and interstitial lung disease. The VISION study is
continuing to enroll patients harboring MET exon 14 skipping
mutations from Europe, United States and Japan.

"These data support our plans to continue with the clinical
development of tepotinib in this particularly aggressive, advanced
lung cancer. Patients with this form of non-small cell lung cancer
currently have a poor prognosis and limited treatment options," said
Luciano Rossetti, M.D., Executive Vice President, Global Head of
Research & Development at the biopharma business of Merck. "Tepotinib
is an important late-stage investigational therapy and a key part of
our strategic focus on innovative precision medicines."

Tepotinib, discovered in-house at Merck, is an investigational
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 has been designed with the potential to improve outcomes in
aggressive tumors that have a poor prognosis and harbor these
specific mutations. In March, the Japanese Ministry of Health, Labour
and Welfare granted SAKIGAKE 'fast-track' designation to tepotinib in
patients with NSCLC harboring MET exon 14 skipping mutations.

Presentation Date
Title Lead Author Abstract # / Time (CDT)
Location

Tepotinib
Poster Sessions
Can duration of
response be used
as a surrogate
endpoint for
overall survival
in advanced
non-small cell Boris M Sun, Jun 03, 8:00
lung cancer? Pfeiffer 9082 a.m. - 11:30 a.m.
Hall A
Poster Discussion
Tepotinib in
patients with
advanced
non-small cell
lung cancer
(NSCLC) harboring
MET exon
14-skipping
mutations: Phase Enriqueta Sun, Jun 03, 11:30
II trial. Felip, M.D. 9016 a.m. - 12:45 p.m.
Arie Crown Theater

In addition to tepotinib, Merck is sharing data from across its
oncology and immuno-oncology pipeline at ASCO 2018, including
investigational immunotherapy M7824 and updates from its DNA Damage
Response portfolio. Merck is committed to exploring an array of
targets and taking creative scientific approaches to developing novel
therapies for hard-to-treat cancers.

*Tepotinib is the recommended International Nonproprietary Name
(INN) for the c-Met kinase inhibitor (MSC 2156119J). Tepotinib is
currently under clinical investigation and not approved for any use
anywhere in the world.

About Non-Small Cell Lung Cancer

Globally, lung cancer is the most common cause of cancer-related
deaths in men and the second most common in women,[1] responsible for
more deaths than colon, breast and prostate cancer combined.[2] NSCLC
is the most common type of lung cancer, accounting for 80 to 85% of
all lung cancers.[3] MET exon 14 skipping mutations occur in 3-4% of
lung cancers.[5],[6] The five-year survival rate for people diagnosed
with lung cancer that has spread (metastasized) to other areas of the
body is 1%.[4]

About Tepotinib

Tepotinib is an investigational, small-molecule inhibitor of the
c-Met receptor tyrosine kinase discovered in-house at Merck.
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 currently being investigated in a
Phase II study in NSCLC.

About SAKIGAKE

SAKIGAKE designation is granted by the Japanese Ministry of
Health, Labour and Welfare, promoting research and development in
Japan and aiming at early practical application for innovative
pharmaceutical products, medical devices and regenerative medicines.
SAKIGAKE designation can reduce a drug's review period down from 12
months to a target of 6 months.

The system's objective is to designate drugs that have the
potential of prominent effectiveness against serious and
life-threatening diseases in order to make them available to patients
in Japan ahead of the rest of the world.

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

Merck is a leading science and technology company in healthcare,
life science and performance materials. Almost 53,000 employees work
to further develop technologies that improve and enhance life - from
biopharmaceutical therapies to treat cancer or multiple sclerosis,
cutting-edge systems for scientific research and production, to
liquid crystals for smartphones and LCD televisions. In 2017, Merck
generated sales of EUR 15.3 billion in 66 countries.

Founded in 1668, Merck is the world's oldest pharmaceutical and
chemical company. The founding family remains the majority owner of
the publicly listed corporate group. Merck holds the global rights to
the Merck name and brand. The only exceptions are the United States
and Canada, where the company operates as EMD Serono, MilliporeSigma
and EMD Performance Materials.

References

1. American Cancer Society (2015) Global facts & figures third
edition. Available from: http://www.cancer.org/acs/groups/content/
@research/documents/document/acspc-044738.pdf. Accessed February
2018
2. American Cancer Society (2017) Key statistics for lung cancer.
Available from: https://www.cancer.org/cancer/non-small-cell-lung-
cancer/about/key-statistics.html. Accessed February 2018.
3. American Cancer Society (2016) What is non-small cell lung cancer?
Available from: https://www.cancer.org/cancer/non-small-cell-lung-
cancer/about/what-is-non-small-cell-lung-cancer.html. Accessed
February 2018.
4. Cancer.net. Lung cancer - non-small cell: statistics. Available
from: http://www.cancer.net/cancer-types/lung-cancer-non-small-cel
l/statistics. Accessed February 2018.
5. Lutterbach B et al. Lung cancer cell lines harboring MET gene
amplification are dependent on Met for growth and survival. Cancer
Res. (2007) 67(5):2081-8.
6. Wong MCS, et al. Incidence and mortality of lung cancer: global
trends and association with socioeconomic status. Sci. Rep. (2017)
7:143000: doi: 10.1038/s41598-017-14513-7.
(https://www.nature.com/articles/s41598-017-14513-7)

Contact: Brenda Mulligan +978-821-5345

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