Insilico Medicine has joined forces with Menarini through its subsidiary Stemline Therapeutics to develop a small molecule KAT6A inhibitor to treat hormone-sensitive cancers, focusing on ER+/HER2- breast cancer.
The collaboration involves an exclusive licensing agreement, providing Stemline with global rights to develop and commercialise a novel KAT6A inhibitor, which is designed using Insilico’s artificial intelligence (AI) platform.
The molecule has shown positive results in preclinical studies, demonstrating a potent inhibition in multiple CDX and PDX models, as well as a good safety and efficacy profile. Insilico presented data on this development at the San Antonio Breast Cancer Symposium last month.
Insilico will receive $12m in an upfront payment from Menarini, as well as milestone payments with a combined value of more than $500m and sales royalties.
In September 2019, Insilico announced its AI-powered drug discovery system GENTRL, which was created in alliance with WuXi AppTec, a global open-access R&D and manufacturing platform, as well as professor Alán Aspuru-Guzik, who works in quantum computing and AI in chemistry.
In the announcement accompanying the agreement, Menarini CEO Elcin Barker Ergun said: “Having brought the first innovation in endocrine therapy after almost 20 years to the US and Europe with elacestrant for ER+/HER2- breast cancer patients, our aim is to further augment patient outcomes, and targeting KAT6A can potentially serve that in breast cancer and beyond.”
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KAT6A proteins play a crucial role in regulating gene expression and are implicated in various cancers, including poor clinical outcomes of ER+/HER- breast cancers.
Other companies are also looking at the same protein inhibition. Pfizer’s PF-07248144 is under development for the treatment of locally advanced or metastatic ER+/HER2- breast cancer, metastatic castration-resistant prostate cancer and metastatic non-small cell lung cancer (NSCLC).
According to GlobalData’s Pharmaceutical Intelligence Center, PF-07248144 is currently being investigated in a Phase I clinical trial, with a Phase II trial planned.
GlobalData is the parent company of Pharmaceutical Technology.