Menarini Group and Insilico Medicine sign exclusive global license agreement for …

Florence, Italy and New York (ots/PRNewswire)

• KAT6 is a new target in hormone-sensitive breast cancer tumors and other cancers. Overexpression of KAT6A/B is associated with poor clinical outcomes in patients with ER+/HER2- breast cancer, one of the most common subtypes.
• The molecule showed high preclinical activity. Insilico presented data on this new molecule at the San Antonio Breast Cancer Symposium in early December.
• The agreement includes upfront and milestone payments with a total potential of over $500 million as well as royalties.

The Menarini Group (“Menarini”) is a leading international manufacturer of pharmaceuticals and diagnostic products, and Stemline Therapeutics, Inc. (“Stemline”) is a wholly owned subsidiary of the Menarini Group committed to helping cancer patients with transformative oncology therapies. Together with Insilico Medicine (“Insilico”), a clinical-stage drug discovery biotechnology company powered by generative artificial intelligence (AI), the companies today announced that Stemline has entered into an exclusive license agreement for the worldwide rights to use Insilico’s AI platform to develop and commercialize a novel small molecule KAT6A inhibitor that could be a treatment option for hormone-sensitive cancers and other oncology indicators.

Breast cancer is one of the most commonly diagnosed tumor types and is one of the leading causes of cancer-related deaths among women worldwide.[1] Around 70% of breast cancer tumors are estrogen receptor-positive (ER+). Endocrine therapy is and remains the treatment of choice for ER+ breast cancer. However, tumors can develop resistance to endocrine therapy, which can lead to worsening of the disease. This is a major clinical challenge and shows how important it is to develop new forms of therapy that can overcome treatment resistance.

KAT6A plays an important role in many types of cancer. Overexpression of KAT6A is associated with poor clinical outcomes in patients with ER+/HER2- breast cancer – one of the most common subtypes. In preclinical studies, the molecule demonstrated potent inhibition of KAT6A in several CDX and PDX models with good efficacy and safety. Insilico presented data on this molecule at the San Antonio Breast Cancer Symposium in early December.

“We are excited to collaborate with Insilico, which gives us the opportunity as a leading company to use generative AI to explore a promising new treatment approach and develop potentially transformative new cancer therapies,” said Elcin Barker Ergun, CEO of the Menarini Group. “With Elacestrant, we have launched the first innovation in endocrine therapy for ER+ and HER2 breast cancer patients in the US and Europe in almost 20 years. Our goal is to further improve patient outcomes. KAT6A as a target may prove to be extremely effective, and not only in breast cancer.”

The new molecule was developed by the R&D team at Insilico using a pharma-specific generative AI platform to inhibit KAT6A and block the endocrine receptor (ER) at the transcriptional level. This opens the opportunity to overcome resistance to endocrine therapies that can develop due to mutations or ligand-independent constitutive activation of ER. Currently, endocrine therapy in combination with CDK4/6 inhibitors is considered the standard of care for ER+/HER2- breast cancer patients with advanced metastases. New combinations with CDK4/6 inhibitors and/or new orally administered SERDs are needed to further expand the results.

“Our latest therapy, developed using generative AI, is very promising. It could represent a new treatment option for breast cancer patients,” explains Dr. Alex Zhavoronkov, founder and co-CEO of Insilico Medicine. “With its innovative vision and focus on transformative oncology therapies, Stemline is the ideal partner to further develop this molecule and bring it through clinical trials.”

Under the agreement, Stemline will pay Insilico $12 million upfront. The total value of the agreement, including all development, regulatory and commercial milestones, is over $500 million, followed by double-digit royalties.

Information about the Menarini Group

The Menarini Group is a leading international pharmaceutical and diagnostics company with sales of over $4.4 billion and over 17,000 employees. Menarini focuses on therapeutic areas with high unmet needs for products in cardiology, oncology, pulmonology, gastroenterology, infectious diseases, diabetology, inflammation and analgesia. With 18 manufacturing sites and 9 research and development centers, Menarini’s products are available in 140 countries worldwide. For more information, visit menarini.com.

About Stemline Therapeutics Inc.

Stemline Therapeutics, Inc. (“Stemline”), a wholly owned subsidiary of the Menarini Group, is a commercial-stage biopharmaceutical company focused on the development and commercialization of novel oncology therapeutics. Stemline markets ORSERDU® (elacestrant) in the US and EU, an oral endocrine therapy for the treatment of postmenopausal women or adult men with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression after at least one endocrine therapy. Stemline also markets ELZONRIS® (tagraxofusp-erzs), a novel CD123-targeted treatment for patients with blastic plasmacytoid dendritic cell neoplasm (BPDCN), an aggressive hematologic cancer in the United States and Europe, which is currently the only approved treatment for BPDCN in the US and EU. Stemline also markets NEXPOVIO® (selinexor), an XPO1 inhibitor for multiple myeloma, in Europe. Stemline also has an extensive clinical pipeline of small molecules and biologics in various stages of development for a range of solid and hematologic cancers.

About Insilico Medicine Insilico Medicine, a generative artificial intelligence (AI)-powered international clinical-stage drug discovery biotechnology company, combines biology, chemistry and clinical trial analysis using cutting-edge AI systems. The company has built AI platforms that use deep generative models, reinforcement learning, transformers and other advanced machine learning techniques to discover new targets and engineer molecular structures with desired properties. Insilico Medicine develops breakthrough solutions for the discovery and development of innovative drugs to treat cancer, fibrosis, immunity, central nervous system diseases, infectious diseases and age-related diseases. www.Insilico.com

[1] Sung H, Ferlay J, Siegel RL, Laversanne M, Soerjomataram I, Jemal A, Bray F. Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin. 4 February 2021. doi: 10.3322/caac.21660. Epub ahead of print. PMID: 33538338.

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Press contact:

Valeria Speroni Cardi,
[email protected],
+ 39 05556801 | Brita Belli,
Head of PR,
Insilico Medicine,
[email protected] | Menarini Stemline,
Cheya Pope,
[email protected]