Data Published in Cancer Research, a journal of the American Association for Cancer Research
Publication highlights potent activity of NXP900, a differentiated inhibitor of the SRC/YES1 Kinases
Fort Lee, NJ, Feb. 22, 2022 (GLOBE NEWSWIRE) -- Nuvectis Pharma, Inc. (NASDAQ: NVCT) (“Nuvectis” or the “Company”), a biopharmaceutical company focused on the development of precision medicines for serious conditions of unmet medical need in oncology, today announced a publication in Cancer Research by scientists from the University of Edinburgh titled Loss of Integrin-Linked Kinase Sensitizes Breast Cancer to SRC Inhibitors, highlighting NXP900's robust activity in preclinical models of Triple Negative Breast Cancer (“TNBC”) with Integrin-Linked Kinase (“ILK”) loss. NXP900 is Nuvectis’ novel and highly-selective SRC/YES1 inhibitor that effectively shuts down SRC-mediated signaling by inhibiting both the catalytic and scaffolding functions of SRC/YES1 kinases, without triggering immunosuppressive effects.
A copy of the publication is available on Nuvectis' website at www.nuvectis.com/NXP900.
The study was led by Dr. Valerie G. Brunton, Ph.D., Professor and Chair of Cancer Therapeutics at the Institute of Genetics and Cancer at the Cancer Research UK Edinburgh Centre in Edinburgh, Scotland. Dr. Brunton and the team at the University of Edinburgh demonstrated that loss of ILK sensitizes TNBC to treatment with SRC inhibitors, and that treatment with NXP900 (referred to as “eCF506” in the publication) was superior to treatment with bosutinib, an approved multi-kinase inhibitor that is known to inhibit the catalytic function of SRC kinase. Importantly, it was shown that NXP900 completely blocked the growth of ILK-knock-out tumors (subcutaneously injected in an immunodeficient mouse model) demonstrating superiority vs bosutinib. The studies also showed that NXP900 was significantly more potent in the same TNBC model (without ILK knock-out) versus bosutinib. This further supports the notion that complete shutdown of SRC-mediated signaling is key to unlocking the full potential of SRC inhibition as an anti-cancer treatment strategy
“Our findings are that loss of ILK sensitizes breast cancer to SRC/YES1 inhibitors and that this exposes a therapeutic vulnerability in breast cancer, representing a potential avenue for clinical development." said Dr. Brunton, who added, “we are enthusiastic about NXP900’s promising activity in in vitro and in vivo models and hope this can pave the way for improved breast cancer treatment.”
“We are encouraged by the data reported in the publication reported today. This is the second paper published to date highlighting NXP900's robust preclinical activity in TNBC, which remains a significant unmet medical need. Moreover, the ILK loss within TNBC represents a potential biomarker-based clinical approach." Mr. Bentsur added, "The in vivo results further reinforce our belief that NXP900 is positioned to potentially become the first SRC/YES1 inhibitor to treat solid tumors. We are currently evaluating the compound in various additional in vivo models and plan to use the results to guide our clinical program."
About NXP900
NXP900 was discovered at the University of Edinburgh and is a unique, differentiated, and potent SRC/YES1 kinase inhibitor. NXP900 is highly selective and inhibits both the catalytic and the scaffolding activities of the kinases by locking them in their closed conformation. This is in contrast with other multi-kinase inhibitors with activity against only the catalytic activity of SRC/YES1 that target the kinase in the open conformation, thereby leaving it available to bind to signaling partners, resulting in only partial pathway inhibition. In addition, treatment with NXP900 does not result in immunosuppression, which is a challenge with other multi-kinase inhibitors, due to their lack of selectivity.
In addition to the in vivo studies conducted to date in TNBC, Nuvectis is currently conducting in vivo studies with NXP900 in various tumor types to potentially identify additional cancers of focus for future clinical trials. Nuvectis intends to complete the IND-enabling studies for NXP900 in 2022.
About Triple Negative Breast Cancer
The American Cancer Society estimates that there will be about 290,000 cases of breast cancer in 2022.1 Triple-negative breast cancer is a sub-type of breast cancer that does not have any of the receptors that are commonly found in breast cancer, estrogen, progesterone and human epidermal growth factor (HER2). TNBC accounts for about 10-15% of breast cancers, or an estimated 35,000 patients annually in the U.S. TNBC differs from other types of invasive breast cancer in that it grows and spreads faster, and has limited treatment options and a worse prognosis.
Although the precise overlap between the ILK loss and TNBC is still being evaluated, the Company estimates that the total addressable patient population of ILK loss within TNBC may be as high as 6,500 patients annually. In addition, ILK loss is also believed to be prevalent in approximately 6% of all other breast cancer subtypes, which may represent an additional potential opportunity for treatment with NXP900 in breast cancer.
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About Nuvectis Pharma, Inc.
Nuvectis Pharma, Inc. is a biopharmaceutical company focused on the development of innovative precision medicines for serious conditions of unmet medical need in oncology. The Company is currently developing two drug candidates: NXP800, a clinical-stage HSF1 pathway inhibitor currently in a Phase 1 study in patients with advanced solid tumors, and NXP900, a novel SRC/YES1 kinase inhibitor currently in preclinical development with IND-enabling studies ongoing.
Forward Looking Statements
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