Merck KGaA and sanofi-aventis Sign Agreement to Jointly Investigate Novel Combinations Against Cancer

DARMSTADT, Germany--(BUSINESS WIRE)--Merck Serono, a division of Merck KGaA, Darmstadt, Germany, announced today that Merck, has signed a worldwide research and development agreement with sanofi-aventis U.S. Inc., under which Merck Serono and sanofi-aventis U.S. Inc. will collaboratively investigate novel experimental combinations of agents that could block specific pathways in cancer cells. This collaboration could deliver novel targeted oncology treatments with high therapeutic potential.

“Combining these two promising molecules makes eminent sense and we are excited to partner with Merck Serono.”

The novel combinations involve Merck Serono’s MEK inhibitor MSC1936369B (also known as AS703026), sanofi-aventis PI3K/mTOR inhibitor SAR245409 (also known as XL765) and class I PI3K inhibitor SAR245408 (also known as XL147), respectively.

Under the terms of this agreement, each party will be initially responsible for conducting a Phase I dose escalation study of these product candidates. Sanofi-aventis will be granted a research and development license to MSC1936369B to assess safety and initial clinical activity in combination with its PI3K inhibitor SAR245408. In conjunction, Merck Serono will be granted a research and development license to SAR245409 in order to assess safety and initial clinical activity in combination with its MEK inhibitor MSC1936369B.

“In the spirit of personalizing and stratifying cancer care, it is a logical step to combine new exciting molecules across pipelines and companies early on, to explore combined activity against cancer pathways,” said Dr. Wolfgang Wein, Executive Vice President for Oncology at Merck Serono. “We expect a strong synergy between both oncology units in driving the projects forward.”

“This collaboration reinforces our commitment to maximize our portfolio and to provide better treatments for patients with cancer” said Debasish Roychowdhury, M.D., Senior Vice President, Head of Global Oncology, sanofi-aventis. “Combining these two promising molecules makes eminent sense and we are excited to partner with Merck Serono.”

About MSC1936369B
MSC1936369B is an experimental selective inhibitor of protein kinases MEK1 and MEK2 (MAP/ERK kinase 1 and 2) effectively blocking downstream protein signaling. It is in early clinical development as monotherapy and in combination with standard of care. At the 2010 annual meeting of the American Society of Clinical Oncology (ASCO) first results have been presented from the on-going Phase I safety, pharmacokinetic and pharmacodynamic study of MSC1936369B in advanced solid tumors, where first signs for anti-tumor activity were observed.¹

About SAR245408 and SAR245409
Sanofi aventis SAR245408 is an inhibitor of class I PI3K (Phosphoinositol 3 Kinase). SAR245409 is a dual inhibitor of PI3K and mTOR (mammalian Target of Rapamycin). Both compounds have been shown to effectively block downstream signaling and are in early clinical development as monotherapy and in combination with standard of care. Results of six ongoing Phase I clinical trials were presented at the 2010 annual ASCO meeting.^2-7

References

1. Delord J, et al. ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s (suppl; abstr 2504)

2. Edelman G, et al ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s. (suppl; abstr 3004)

3. Moldovan C, et al. ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s. (suppl; abstr 3070)

4. Traynor AM, et al. ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s. (suppl; abstr 3078)

5. Braña I, et al. ASCO Annual Meeting 2010 J Clin Oncol. 2010;28:15s (suppl; abstr 3030)

6. Nghiemphu PL, et al. ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s (suppl; abstr 3085)

7. Cohen RB, et al. ASCO Annual Meeting 2010, J Clin Oncol. 2010;28:15s (suppl; abstr 3015)

ERK = Extracellular signal-regulated kinase
MAPK = Mitogen-activated protein kinase
MEK-inhibitor: MAP/ERK kinase-inhibitor
mTOR = mammalian target of rapamycin
PI3K = Phosphoinositide 3-kinase
PTEN = Phosphatase and tensin homolog

About Merck Serono

Merck Serono is the biopharmaceutical division of Merck KGaA, Darmstadt, Germany, a global pharmaceutical and chemical company. Headquartered in Geneva, Switzerland, Merck Serono discovers, develops, manufactures and markets prescription medicines of both chemical and biological origin in specialist indications. In the United States and Canada, EMD Serono operates through separately incorporated affiliates.

Merck Serono has leading brands serving patients with cancer (Erbitux^®, cetuximab), multiple sclerosis (Rebif^®, interferon beta-1a), infertility (Gonal-f^®, follitropin alfa), endocrine and metabolic disorders (Saizen^® and Serostim^®, somatropin), (Kuvan^®, sapropterin dihydrochloride) as well as cardiometabolic diseases (Glucophage^®, metformin), (Concor^®, bisoprolol), (Euthyrox^®, levothyroxine). Not all products are available in all markets.

With an annual R&D expenditure of over € 1bn, Merck Serono is committed to growing its business in specialist-focused therapeutic areas including neurodegenerative diseases, oncology, fertility and endocrinology, as well as new areas potentially arising out of research and development in rheumatology.

For more information, please visit www.merckserono.com or www.merck.de

About Merck

Merck is a global pharmaceutical and chemical company with total revenues of € 7.7 billion in 2009, a history that began in 1668, and a future shaped by approximately 40,000 (including Merck Millipore) employees in 64 countries. Its success is characterized by innovations from entrepreneurial employees. Merck's operating activities come under the umbrella of Merck KGaA, in which the Merck family holds an approximately 70% interest and free shareholders own the remaining approximately 30%. In 1917 the U.S.

subsidiary Merck & Co. was expropriated and has been an independent company ever since.

For more information, please visit www.merckserono.com or www.merck.de