The data demonstrate that TG02 and carfilzomib, which target the key survival protein Mcl-1 via independent mechanisms, can produce a synergistic effect in human myeloma cell lines and overcome the protective effects of the ‘bone marrow niche'.
San Diego (PRWEB) December 06, 2013
Tragara Pharmaceuticals, Inc. today announced that two posters on TG02, the Company's unique oral multi-kinase inhibitor, will be presented at the American Society of Hematology (ASH) 2013 Annual Meeting (December 7-10, 2013) in New Orleans.
Researchers from the Winship Cancer Institute of Emory University in Atlanta will present a poster entitled, “Dual Inhibition Of Mcl-1 By The Combination Of Carfilzomib and TG02 In Multiple Myeloma”. The data demonstrate that TG02 and carfilzomib, which target the key survival protein Mcl-1 via independent mechanisms, can produce a synergistic effect in human myeloma cell lines and primary isolates and overcome the protective effects of the ‘bone marrow niche’. The poster (#3171) will be shown on Sunday, December 8, 2013, from 6:30PM -8:30PM in Hall G of the Ernest N. Morial Convention Center.
Separately, researchers from the Weill Medical College of Cornell University will present a poster entitled “Leukemia Stem/Progenitor Cells From AML Patients Treated With The Multi-Kinase Inhibitor TG02 Demonstrate Increased Proliferation and Are Sensitized To Chemotherapeutic Agents”. The data show that TG02 induces a mobilization effect in bone marrow-resident leukemia stem cells that results in increased proliferation and, thus, sensitization to chemotherapeutic drugs such as Ara-C. Leukemia stem cells are typically difficult to target with traditional chemotherapy, as these cells are frequently found in bone marrow niches where they exist in a dormant state. TG02 produced an effect that reawoke these stem cells, causing them to proliferate and become more vulnerable targets for chemotherapy. The poster (#3892) will be shown on Monday, December 9, 2013, from 6:00PM - 8:00PM in Hall E of the Ernest N. Morial Convention Center.
TG02 is currently in phase I clinical testing in patients with acute leukemia and in patients with multiple myeloma in the United States. A phase I clinical study in patients with CLL is planned for 2012.
TG02 is a unique, oral multi-kinase inhibitor which combines the benefits of inhibiting important cyclin dependent kinases equipotently with JAK2, FLT3, and ERK5 inhibition. TG02 exerts its antitumor activity primarily via its potent CDK9 inhibition, which leads to the depletion of key survival proteins, such as Mcl-1, resulting in p53-independent apoptosis of a wide range of tumor cells. TG02 development will initially focus on the treatment of hematologic malignancies, including multiple myeloma (MM) and chronic lymphocytic leukemia (CLL), based on the consistent anti-tumor activity that has been observed across a broad spectrum of hematologic cancer models, including those resistant to currently available therapies. In these models, TG02 demonstrated both single agent activity and synergy when administered with current standard of care therapies. Subsequent development will focus on an important group of solid tumors with unmet medical need, such as small cell lung cancer, triple negative breast cancer, and melanoma, which will also benefit from this mechanism of action, complemented with the benefits of inhibiting both JAK2 and ERK5. These pathways affect disease progression and survival in hematologic malignancies and solid tumors.
TG02 is currently being evaluated in two separate phase I clinical trials in patients with MM and CLL in the United States.
In early 2010, TG02 was selected by the Multiple Myeloma Research Foundation as a winner of its Biotech Investment Award, which represents a multi-year research grant commitment to fund the early-stage drug development of novel compounds that show potential in treating MM.
Tragara Pharmaceuticals, Inc. is a privately held pharmaceutical company based in San Diego, Calif. The company is focused on the clinical and commercial development of proprietary medicines for the treatment of cancer. TG02 is a unique, oral multi-kinase inhibitor which combines the benefits of inhibiting important cyclin dependent kinases equipotently with JAK2, FLT3, and ERK5 inhibition. TG02 exerts its antitumor activity via its potent CDK9 inhibition, which leads to the depletion of key survival proteins, such as Mcl-1, resulting in p53-independent apoptosis of a wide range of tumor cells. Tragara is managed by a team of entrepreneurs with both Big Pharma and Biotech experience in the development and commercialization of oncology therapeutics. Its investors include: Domain Associates, Mitsubishi International Corporation, Morgenthaler Ventures, ProQuest Investments and RusnanoMedInvest.
Tragara strives to provide much-needed therapies that will contribute to patient health through better survival and an increase in the quality of life. For more information, visit http://www.tragarapharma.com.