Calithera Biosciences, Inc. Initiates Three Phase 1 Trials With First-In-Class Glutaminase Inhibitor CB-839 In Patients With Advanced Solid And Hematological Cancers
2/24/2014 11:11:27 AM
South San Francisco,, California, February 24, 2014 — Calithera Biosciences, Inc., a clinical-stage
biopharmaceutical company discovering and developing novel small molecule therapeutics in cancer,
today announced the commencement of patient dosing in its first Phase 1 study of CB-839 in patients
with advanced solid tumors. CB-839 is a potent, selective, orally bioavailable inhibitor of glutaminase that
interferes with tumor metabolism and blocks cancer cell growth and survival.
"We are pleased to be advancing the first glutaminase inhibitor into clinical trials. Glutaminase is a novel
target in cancer metabolism, and these studies will allow us to assess the safety, pharmacokinetics and
pharmacodynamics of this exciting new agent," said Susan M. Molineaux, Ph.D., founder, Chief Executive
Officer and President of Calithera Biosciences. "CB-839 has demonstrated significant anti-tumor activity
in both solid and hematological tumor models and we look forward to reporting initial clinical results with
Two additional Phase 1 studies, one in patients with advanced multiple myeloma and non-Hodgkin’s
lymphoma and another in patients with acute leukemias, are being conducted in parallel. All three
Phase 1 clinical trials are single-arm, open-label dose escalation studies that allow for expansion in
specific tumor types once the maximum tolerated dose is reached. The primary objectives of each of
these studies are to determine the safety and tolerability of CB-839 and to establish a dose for Phase 2
studies. Secondary endpoints of the Phase 1 clinical studies include pharmacokinetics,
pharmacodynamics and evidence of anti-tumor response.
The trials are being conducted at clinical sites in the United States.
Glutaminase Inhibition: A Novel Mechanistic Approach to Targeting Cancer
While most normal cells rely primarily on glucose as a fuel, many tumor cells rely on the amino acid
glutamine to meet the demands of rapid growth under conditions that limit nutrient and oxygen availability.
Glutaminase, the first enzyme in the glutamine metabolism pathway, controls the conversion of glutamine
to glutamate. In glutamine-requiring cancer cells, inhibition of glutaminase with CB-839 results in
depletion of intracellular pools of TCA cycle intermediates, glutathione, and amino acids. This leads to
inhibition of cell growth and often leads to induction of apoptosis. In preclinical studies, CB-839 is
effective against a significant fraction of tumor cells from a variety of solid and hematologic tumor cell
types, including triple-negative breast cancer, non-small cell lung cancer, renal cell carcinoma,
mesothelioma, multiple myeloma, diffuse large B-cell lymphoma and acute leukemias. CB-839
suppresses tumor growth in preclinical animal models, but is well tolerated on a continuous daily dosing
regimen, highlighting the tumor-specific impact of glutaminase inhibition. Calithera presented some of
these preclinical results in December 2013 at the 55th American Society of Hematology (ASH) Annual
Meeting and at the 2013 San Antonio Breast Cancer Symposium.
About Calithera Biosciences
Calithera Biosciences, Inc. is a clinical-stage company focused on the discovery, development and
commercialization of first-in-class small molecule oncology therapeutics. The company is building a
pipeline of targeted anti-cancer compounds that inhibit pathways critical to tumor growth and survival.
Calithera’s lead product, CB-839, is currently being tested in patients with advanced solid and
hematological cancers. Calithera Biosciences is headquartered in South San Francisco. For more
information about Calithera Biosciences, please visit www.calithera.com.
Susan M. Molineaux, Ph.D.
President and CEO
Karen L. Bergman or
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