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

Thursday 18 May 2017 09:02
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(R) (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(R)) 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(R) (cetuximab)

Erbitux(R) 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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Source: Merck