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N.B. Quadriga's Transformative Treatment for Brain Cancers Dosed in First Human Subject

-- First-in-class dual function small molecule drug utilities LAT1 amino acid transporter pathway to cross blood-brain barrier and deliver warhead directly into cancer cells, a potential breakthrough in central nervous system cancer treatment --
2020-07-23 19:00 3862

SHANGHAI and NANTONG, China, July 23, 2020 /PRNewswire/ -- N.B. Quadriga (NBQ), a clinical stage biopharmaceutical company developing transformative medicines for brain cancers, today announced that the first patient has been dosed in a Phase 1 study of NBQ72S, also known as QBS10072S, in patients with advanced malignancies. NBQ72S is a novel, first-in-class, bifunctional small molecule that targets human LAT1 (L-type amino acid transporter 1), a member of the solute carrier (SLC) superfamily of transporters, which is highly expressed on the blood-brain barrier (BBB) and in many aggressive forms of cancers, such as glioblastoma multiforme (GBM), breast cancer, lung cancer, and melanoma. NBQ72S is designed to exploit LAT1 for efficient, active transport across the BBB into the brain and specifically targets and enters high LAT1 expressing tumor cells, but not normal tissues which typically do not express LAT1. Inside the cancer cells, NBQ72S exerts its cell-killing activity by disrupting DNA replication of those rapidly dividing cells leading to cell death.

"There is a very high unmet medical need for central nervous system (CNS) cancers including brain metastases (BM) and primary glioblastoma in China and across the world. We are excited about the potential of our investigational new drug, NBQ72S, to transform treatment for patients with brain tumors. Built upon promising preclinical data, this first-in-human (FIH) dosing is an important milestone for the company and our co-development partner Quadriga BioSciences," said Frank Yan, Ph.D., Chief Executive Officer of NBQ and Partner at 3E Bioventures Capital. "Many cancers express LAT1 especially at later stages. We see a much broader application of our drug in cancer treatment, both for systematic cancers and those involving the brain, as well as potential combination with existing therapies of complimentary mechanisms of action for additional indications."

"Advancing NBQ72S into clinical development is an important step in providing therapeutic options for patients for whom very few treatment options are currently available, other than radiation and surgery," said W. K. Alfred Yung, M.D., Professor of Neuro-Oncology at MD Anderson and executive committee member of the Moon Shots Program. "One of the biggest hurdles to developing effective treatments for brain cancer is that most drugs cannot cross the blood-brain barrier, and it is encouraging to see the preclinical data that NBQ72S was able to be transported across the BBB, accumulate preferentially in the brain tumor, resulting in reduced tumor growth and improved survival in animal models of leptomeningeal disease from triple-negative breast cancer (TNBC) and GBM. I look forward to the development of this drug in patients with brain metastases and glioblastoma multiforme across the world."

"We are very pleased to partner with NBQ for this first-in-class LAT1 targeted cancer clinical program. Initiation of this study is a major milestone for both companies," said Gordon Ringold, Ph.D., Chief Executive Officer of Quadriga BioSciences. "We believe this program has the potential to significantly help patients with brain metastases and those with late stage astrocytoma, also known as glioblastoma multiforme."

About the Study

This study is a Phase 1, open label, multi center, single and multiple dose, dose escalation and expansion study to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of QBS10072S (also known as NBQ72S) in previously treated patients with advanced or metastatic cancers with high LAT1 signatures, and in patients with relapsed or refractory grade 4 astrocytoma. The primary objectives of the study are to determine the maximum tolerated dose (MTD), pharmacokinetics, and preliminary anti-tumor activity of QBS10072S. Disease specific expansion cohorts with brain metastases and astrocytoma will be enrolled at the maximally tolerated or biologically relevant dose. Please refer to ClinicalTrials.gov for additional clinical trial details.

About N.B. Quadriga (NBQ)

NBQ is an innovative, clinical stage biopharmaceutical company based in China, developing transformative first-in-class drugs to treat cancers with central nervous system (CNS) involvement and other tumors with high unmet medical need. NBQ develops clinical assets by targeting one unique member of the solute carrier (SLC) transporter superfamily, namely L-type amino acid transporter 1 (LAT1), which not only is significantly expressed on the blood-brain barrier (BBB) but also broadly overexpressed in cancer patients especially with brain metastases (BM) and glioblastoma multiforme (GBM). Our mission is to discover and bring preclinical stage assets to clinical development and translate basic science into medicine for patients with cancer in China and around the world.

About Brain Metastases (BM)

Brain metastases are cancer growths that spread to the brain from a cancer that originates from another part of the body. They are the most commonly diagnosed central nervous system (CNS) cancer and often associated with significant morbidity and mortality, representing a high unmet medical need. These types of brain tumors are estimated to occur 10 times more frequently than primary brain cancer. Systemic tumors of the lung, breast, and melanoma are the leading causes of brain metastases. While estimates vary substantially across different primary tumor types, brain metastases account for approximately 10% of all cancers diagnosed.

About Primary Brain Cancer and Glioblastoma Multiforme (GBM)

Globally, an estimated 405,000 patients are diagnosed with, and over 247,000 patients die from, primary brain cancer each year, i.e., cancer originating from the brain or the central nervous system (CNS). China and the U.S. are the two countries with the highest numbers of new diagnoses of primary brain cancer. Glioblastoma multiforme is the most common and most aggressive form of primary malignant tumor of the central nervous system (47.7%). Current treatments for patients with newly diagnosed GBM include surgery followed by radiation and chemotherapy. The five-year survival rate of patients with GBM is less than five percent. The last medication that extends survival of patients with GBM was approved by U.S. Food and Drug Administration (FDA) in 2005. Recurrence of GBM is, unfortunately, almost inevitable, and there are no established viable treatment options for patients with relapsed/refractory (r/r) GBM.

Media Contact:
Ryan Ulrich
Phone: +86 13391135457
Email: media@nbquadriga.com 

 
Source: N.B. Quadriga
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