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Shaping Cancer Care Today and Tomorrow: Merck to Present New Data from Rapidly Evolving Pipeline at ASCO 2017

Germany (ots/PRNewswire)

Not intended for UK- or U.S.-based media

ASCO Abstract #

M7824 (anti-PD-L1/TGF-ß trap): 3006; Avelumab: 9086, 9530, 9557, 4528, 3059, 5037, e21070, e21065, e20581; Tepotinib: 4087, 8547, e15676, 20541; M3814 (DNA-PK): 2556, e14048; M7583 (BTKi): e14101

- ASCO data highlights Merck's strong and rapidly accelerating 
  pipeline in oncology, spanning immuno-oncology to DNA damage 
  response 
- New avelumab data in metastatic Merkel cell carcinoma and 
  previously treated metastatic urothelial carcinoma, following 
  recent U.S. FDA accelerated approvals  
- Oral presentation on new immuno-oncology approach anti-PD-L1/TGF-ß 
  trap (M7824); potential first-in-class bifunctional immunotherapy 

Merck, a leading science and technology company, today announced that new research from its growing broad oncology portfolio, from immuno-oncology (IO) to DNA damage response (DDR) approaches, will be presented across a broad range of hard-to-treat cancers at this year's American Society of Clinical Oncology annual meeting (ASCO; June 2-6, Chicago). Over 40 abstracts showcase the impact of Merck's commitment to shaping cancer care today and tomorrow, including data for avelumab*, which is being developed in collaboration with Pfizer, Erbitux® (cetuximab), and pipeline updates on the anti-PD-L1/TGF-ß trap M7824, the DNA-PK inhibitor M3814, the BTK inhibitor M7583, and the c-Met inhibitor tepotinib**.

"We are focused on delivering innovation that matters to patients, as shown in our ASCO data that spans across IO and DDR approaches to tackle some of the hardest-to-treat cancers," said Luciano Rossetti, Executive Vice President, Head of Global Research & Development at the biopharma business of Merck. "Merck was among the first to leverage the potential of the PD1/PDL1 pathway for patients, and we continue to build on that progress with our ASCO presence and the two recent FDA accelerated approvals for avelumab."

Multiple avelumab presentations at ASCO include data in first-line metastatic Merkel cell carcinoma (mMCC) and previously treated metastatic urothelial carcinoma (UC), as well as results from the Phase Ib trial from the avelumab combination trial with axitinib in renal cell carcinoma (RCC). Recently, the U.S. Food and Drug Administration (FDA) granted accelerated approval*** for avelumab for the treatment of mMCC and pretreated patients with locally advanced or metastatic UC. Avelumab is currently being evaluated as both monotherapy and combination therapy in an extensive clinical development program. Beyond mMCC, locally advanced or metastatic UC and RCC, further avelumab abstracts in non-small cell lung cancer and metastatic castrate-resistant prostate cancer, locally advanced squamous cell carcinoma of the head and neck, relapsed or refractory diffuse large B-cell lymphoma will be showcased.

In addition to avelumab data, Merck will also feature new research at ASCO on its investigational bifunctional immunotherapy anti-PD-L1/TGF-ß trap (M7824), which is thought to simultaneously block both PD-L1 and TGF-ß. An oral presentation will showcase dose escalation Phase I clinical data exploring the potential of M7824 in advanced solid tumors.

Pipeline updates at ASCO also include early clinical results for both Tepotinib, an investigational small-molecule inhibitor of the c-Met receptor tyrosine kinase, M7583, an oral, highly selective, covalent inhibitor of Bruton's tyrosine kinase (BTK), and the first clinical data for M3814, an investigational DNA-dependent protein kinase (DNA-PK) inhibitor. Merck is investing significant resources in the promising area of DDR to be a leader in this field. Merck has recently in-licensed two promising clinical-stage programs from Vertex.

This highly focused approach to research and development channels Merck's scientific expertise in areas of high unmet need, a legacy started with Erbitux. Multiple presentations at ASCO reinforce Erbitux as a standard-of-care treatment in squamous cell carcinoma of the head and neck (SCCHN) and metastatic colorectal cancer (mCRC), providing valuable information about biomarkers, disease response, and the importance of tumor location in mCRC, to best target treatment to the right patients.

*Avelumab is under clinical investigation for treatment of NSCLC, RCC, DLBCL, SSCHN and mCRPC and has not been demonstrated to be safe and effective for these indications. There is no guarantee that avelumab will be approved for NSCLC, RCC, DLBCL, SSCHN and mCRPC by any health authority worldwide.

**Tepotinib is the proposed nonproprietary name for the c-Met kinase inhibitor (also known as MSC2156119J).

Tepotinib, M7824 and M3814 are under clinical investigation and have not been proven to be safe and effective. There is no guarantee any product will be approved in the sought-after indication by any health authority worldwide.

Notes to Editors

Accepted Merck-supported key abstracts slated for presentation are listed below. In addition, a number of investigator-sponsored studies have been accepted, including multiple abstracts related to Erbitux and avelumab (not listed).



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

M7824 (TGF-ss trap) JL Gulley      3006             June 5       
Hall D1           
Oral Presentation                                  13:15-16:27
Solid Tumors
Preliminary
results from a
phase 1 trial of
M7824
(MSB0011359C), a
bifunctional
fusion protein                           
targeting PD-L1
and TGF-beta, in
advanced solid
tumors               


Presentation
Date / Time
Title                  Lead Author   Abstract #    (CDT)         
Location
Avelumab                                           June 5
Oral Presentation      TK Choueiri     4504      8:00-11:00     
Arie Crown Theater
Renal Cell
Carcinoma
(JAVELIN Renal
100)
First-line
avelumab +
axitinib therapy
in patients with                            
advanced renal
cell carcinoma:
results from a                                              
phase 1b trial    

Poster Sessions                                     June 3
Non-Small Cell          JL Gulley       9086      8:00-11:30     
Hall A
Lung Cancer
(JAVELIN Solid
Tumor)
Exposure-response
and PD-L1
expression
analysis of
second-line
avelumab in
patients with                          
advanced NSCLC:
Data from the
JAVELIN Solid
Tumor trial       
Merkel Cell                                        June 3
Carcinoma (JAVELIN     S D'Angelo       9530      13:15-16:45    
Hall A
Merkel 200)
First-line
avelumab treatment
in patients with
metastatic Merkel                       
cell carcinoma:
preliminary data
from an ongoing
study                                               June 3
Merkel Cell            I Shapiro        9557      13:15-16:45    
Hall A
Carcinoma (JAVELIN
Merkel 200)
Exploratory
biomarker analysis
in patients with
chemotherapy-refra                      
ctory metastatic
Merkel cell
carcinoma treated
with avelumab                                        June 4
Urothelial              AB Apolo        4528       8:00-11:30    
Hall A
Carcinoma 
Updated efficacy
and safety of
avelumab in
metastatic
urothelial
carcinoma: pooled
analysis from 2
cohorts of the
phase 1b JAVELIN
Solid Tumor study                                    June 4
Renal Cell           TK Choueiri     TPS4594       8:00-11:30    
Hall A
Carcinoma (JAVELIN
Renal 101)
Avelumab plus
axitinib vs
sunitinib as
first-line
treatment of
advanced renal
cell carcinoma:
phase 3 study
(JAVELIN Renal
101)                                                June 5
Pan-Tumor              K Kelly          3059       8:00-11:30    
Hall A
(JAVELIN Solid
Tumor)
Safety profile of
avelumab in
patients with                           
advanced solid
tumors: a JAVELIN
pooled analysis of
phase 1 and 2 data                                    June 5
Lymphoma (TiP)         R Chen         TPS7575        8:00-11:30  
Hall A
(JAVELIN DLBCL)
Phase 1b/3 study
of avelumab-based
combination
regimens in
patients (pts)
with relapsed or                            
refractory diffuse
large B-cell
lymphoma (R/R
DLBCL)                                                June 5
Prostate Cancer    F. Fakhrejahani      5037        13:15-16:45  
Hall A
(JAVELIN Solid
Tumor)
Avelumab in                             
metastatic
castration-resista
nt prostate cancer
(mCRPC)                                               June 5
Head and Neck          NY Lee        TPS6093        13:15-16:45  
Hall A
Cancer (TiP)
(JAVELIN Head and
Neck 100)
JAVELIN Head and
Neck 100: a phase
3 trial of
avelumab in
combination with
chemoradiotherapy
(CRT) vs CRT for
1st-line treatment
of locally                                  
advanced squamous
cell carcinoma of
the head and neck
(LA SCCHN)        


Publications
Merkel Cell            M Bharmal      e21070              N/A    
N/A
Carcinoma (JAVELIN
Merkel 200)
Non-progression
during avelumab
treatment is
associated with
clinically
relevant
improvements in
health-related
quality of life in
patients with
Merkel cell
carcinoma
Merkel Cell            H Kaufman      e21065              N/A    
N/A
Carcinoma (JAVELIN
Merkel 200)
Patient
experiences with
avelumab vs
chemotherapy for
treating Merkel
cell carcinoma:                 
results from
protocol-specified
qualitative
research          
Non-Small Cell        Z Feng        e20581              N/A       
N/A
Lung Cancer
(JAVELIN Solid
Tumor)
Comparative study
of two PD-L1
expression assays
in patients with
non-small cell
lung cancer
(NSCLC)


Presentation
Date / Time
Title              Lead Author     Abstract #          (CDT)     
Location
Tepotinib                                             June 3
Poster Sessions       S Qin             4087         8:00-11:30  
Hall A
Hepatocellular
Carcinoma
Phase Ib trial of 
tepotinib in Asian
patients with
advanced
hepatocellular
carcinoma (HCC):
Final data
including
long-term outcomes                                    June 3
Non-Small Cell        Y-L Wu             8547        8:00-11:30  
Hall A
Lung Cancer
Phase Ib study of
tepotinib in
EGFR-mutant/c-Met-
positive NSCLC:
final data and
long-term
responders        


Publications
Hepatocellular       S Faivre          e15676           N/A      
N/A
Carcinoma
Final phase Ib
data for the oral
c-Met inhibitor
tepotinib in
patients with
previously treated
advanced
hepatocellular
carcinoma         
Advanced Lung         PK Paik           20541            N/A     
N/A
Adenocarcinoma
Phase II trial of
the c-Met
inhibitor
tepotinib in
advanced lung
adenocarcinoma
with MET exon 14
skipping mutations


Presentation
Date / Time
Title                 Lead Author      Abstract #       (CDT)    
Location
M3814 (DNA-PK)
Poster Session                                          June 5
Solid Tumors          M van Bussel       2556         8:00-11:30 
Hall A
A multicenter
phase I trial of
the DNA-dependent
protein kinase
(DNA-PK) inhibitor
M3814 in patients
with solid tumors 
Publication
Solid Tumors          B Van Triest      e14048            N/A    
N/A
A phase Ia/Ib
trial of the
DNA-dependent
protein kinase
inhibitor
(DNA-PKi) M3814 in
combination with
radiotherapy in
patients with
advanced solid
tumors            



Presentation
Date / 
Time
Title                 Lead Author     Abstract #           (CDT) 
Location
M7583 (BTKi)        
Publication
B Cell                  S Rule           e14101            N/A   
N/A
Malignancies
Phase I/II, first
in human trial of
the Bruton's
tyrosine kinase
inhibitor (BTKi)
M7583 in patients
with B cell
malignancies      

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About Avelumab

Avelumab is a human antibody specific for a protein called PD-L1, or programmed death ligand-1. Avelumab is designed to potentially engage both the adaptive and innate immune systems. By binding to PD-L1, avelumab is thought to prevent tumor cells from using PD-L1 for protection against white blood cells, such as T-cells, exposing them to anti-tumor responses. Avelumab has been shown to induce antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro. In November 2014, Merck and Pfizer announced a strategic alliance to co-develop and co-commercialize avelumab.

***Indications

The U.S. Food and Drug Administration (FDA) granted accelerated approval for avelumab (BAVENCIO®) for the treatment of (i) metastatic Merkel cell carcinoma (mMCC) in adults and pediatric patients 12 years and older and (ii) patients with locally advanced or metastatic urothelial carcinoma (UC) who have disease progression during or following platinum-containing chemotherapy, or who have disease progression within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials. Avelumab is not approved for any indication in any market outside the U.S.

Important Safety Information

The warnings and precautions for BAVENCIO include immune-mediated adverse reactions (such as pneumonitis, hepatitis, colitis, endocrinopathies, nephritis and renal dysfunction and other adverse reactions), infusion-related reactions and embryo-fetal toxicity.

Common adverse reactions (reported in at least 20% of patients) in patients treated with avelumab include fatigue, musculoskeletal pain, diarrhea, nausea, infusion-related reaction, peripheral edema, decreased appetite/hypophagia, urinary tract infection and rash.

About Erbitux® (cetuximab)

Erbitux® is a highly active IgG1 monoclonal antibody targeting the epidermal growth factor receptor (EGFR). As a monoclonal antibody, the mode of action of Erbitux is distinct from standard non-selective chemotherapy treatments in that it specifically targets and binds to the EGFR. This binding inhibits the activation of the receptor and the subsequent signal-transduction pathway, which results in reducing both the invasion of normal tissues by tumor cells and the spread of tumors to new sites. It is also believed to inhibit the ability of tumor cells to repair the damage caused by chemotherapy and radiotherapy and to inhibit the formation of new blood vessels inside tumors, which appears to lead to an overall suppression of tumor growth. Erbitux also targets cytotoxic immune effector cells towards EGFR expressing tumor cells (antibody dependent cell-mediated cytotoxicity, ADCC).

The most commonly reported side effect with Erbitux is an acne-like skin rash. In approximately 5% of patients, hypersensitivity reactions may occur during treatment with Erbitux; about half of these reactions are severe.

Erbitux has already obtained market authorization in over 90 countries world-wide for the treatment of RAS wild-type metastatic colorectal cancer and for the treatment of squamous cell carcinoma of the head and neck (SCCHN). Merck licensed the right to market Erbitux, a registered trademark of ImClone LLC, outside the U.S. and Canada from ImClone LLC, a wholly-owned subsidiary of Eli Lilly and Company, in 1998.

About M3814

M3814 is an investigational small-molecule inhibitor of DNA-dependent protein kinase (DNA-PK). DNA-PK is a key enzyme for non-homologous end-joining (NEHJ), the most important DNA double strand break repair pathway (DSB), and could potentially enhance the efficacy of many commonly used DNA-damaging agents such as radiotherapy and chemotherapy. M3814 complements Merck's extensive DNA damage response (DDR) portfolio and is currently in Phase I studies.

About M7824

M7824, anti-PD-L1/TGF-ß trap, is an investigational potentially first-in-class bi-functional immunotherapy designed to simultaneously block two immuno-inhibitory pathways (PD-L1 and transforming growth factor beta) that are commonly used by cancer cells to evade the immune system. The aim of this investigational drug is to control tumor growth by restoring and enhancing anti-tumor immune responses. M7824 is currently in Phase I studies for solid tumors.

About Tepotinib

Tepotinib (also known as MSC2156119J) 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 currently under evaluation in Phase I/II trials.

About Merck

Merck is a leading science and technology company in healthcare, life science and performance materials. Around 50,000 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 2016, Merck generated sales of EUR 15.0 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 KGaA, Darmstadt, Germany holds the global rights to the "Merck" name and brand except in the United States and Canada, where the company operates as EMD Serono, MilliporeSigma and EMD Performance Materials.

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Contact:

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