Navigation Links
TG02 Potently Inhibits the Proliferation and Survival of Multiple Myeloma Cell Lines through Depletion of the Key Survival Protein MCL-1

San Diego (PRWEB) April 05, 2013

Tragara Pharmaceuticals, Inc. today announced that profiling biological data on TG02, the Company's unique oral kinase inhibitor, has been published in Clinical Cancer Research. Researchers from the Instituto de Biologia Molecular y Celular del Cancer, University of Salamanca, utilized in vivo models and patient-derived ex vivo samples to evaluate the antitumor activity and mechanism of action of TG02 in multiple myeloma. The data show that TG02 potently and consistently inhibited proliferation and survival of multiple myeloma cell lines, even under protective bone marrow niche conditions, and selectively induced apoptosis of primary patient-derived malignant plasma cells. The study also reported that that TG02 induced robust activation of the intrinsic pathways of apoptosis via its ability to deplete the key survival protein Mcl-1.

In this study, TG02 displayed significant single agent activity in two multiple myeloma xenograft models. Additionally, TG02 enhanced the in vivo activity of bortezomib and lenalidomide, two currently approved treatments for myeloma. As most of the treatment regimens for myeloma patients are based upon drug combinations, TG02’s demonstrated ability to augment the antitumor activity of other agents is a clinically important observation. The researchers also reported that the studied TG02 combinations were well tolerated by the animals.

TG02 is currently in phase I clinical testing in patients with multiple myeloma in the United States. An additional phase I clinical study in patients with chronic lymphocytic leukemia is also underway and a phase I study in acute leukemia has been completed.

1. Álvarez-Fernández, Stela, et al. "Potent antimyeloma activity of a novel ERK5/CDK inhibitor." Clinical Cancer Research (2013).

About TG02
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. TG02 development will initially focus on the treatment of hematologic malignancies, including multiple myeloma (MM) and chronic lymphocytic leukemia (CLL), because of the consistent antitumor activity that was 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. Subsequent phase Ib clinical studies of TG02 in combination with other agents are planned for later in 2013.

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.

About Tragara
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, Morganthaler Ventures, and ProQuest Investments.

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

Read the full story at

Source: PRWeb
Copyright©2012 Vocus, Inc.
All rights reserved

Related medicine news :

1. Bloodstream scavenger inhibits clotting without increased bleeding
2. Molecule found that inhibits recovery from stroke
3. New monoclonal antibody inhibits tumor growth in advanced solid tumors in phase I clinical trial
4. Kentucky team inhibits Alzheimers biomarkers in animal model by targeting astrocytes
5. CWRU School of Medicine researchers discover gene that permanently stops cancer cell proliferation
6. Vaccine yielded encouraging long-term survival rates in certain patients with NSCLC
7. Cancer Care Costs Higher in U.S. Than Europe, But Survival Longer
8. Adding drug to standard chemotherapy provides no survival benefit for older lung cancer patients
9. Hispanics Seem to Have Better Odds of Lung Cancer Survival
10. Equal access to care helps close survival gap for young African-American cancer patients
11. Heart Attack Survival Varies Widely Among Hospitals, Study Finds
Post Your Comments:
(Date:11/24/2015)... ... November 24, 2015 , ... American Specialty ... Program have announced their endorsement of the Medical Fitness Network (MFN), a ... proud to have the MFN as one of our endorsed organizations,” said ASH ...
(Date:11/24/2015)... N.Y. (PRWEB) , ... November 24, 2015 , ... Autism ... Tuesday, the global movement driven by social media and the generosity of people around ... then encourage their social media networks to give – and share the personal stories ...
(Date:11/24/2015)... ... November 24, 2015 , ... World Patent ... Blending, a household invention that revolutionizes the vending machine industry by providing healthy ... is worth $2 billion," says Scott Cooper, CEO and Creative Director of World ...
(Date:11/24/2015)... , ... November 24, 2015 , ... Robert Yeager ... Trend Report . Throughout the past year there have been multiple breakthroughs and challenges ... During this transition, PharmMD has enabled their customers and partners to stay ahead of ...
(Date:11/24/2015)... ... November 24, 2015 , ... Dehydration, defined as a loss of body water ... the hot sun, and heat stroke and death will quickly follow. A normal human ... Kleyne. Every cell, system and structure requires water to function properly. Kleyne, who believes ...
Breaking Medicine News(10 mins):
(Date:11/24/2015)... Nov. 24, 2015   HeartWare International, Inc . ... miniaturized circulatory support technologies that are revolutionizing the treatment ... Chief Executive Officer Doug Godshall is scheduled ... Annual Healthcare Conference on December 1, 2015 at 3:00 ... in New York . ...
(Date:11/24/2015)... BERN, Switzerland , November 24, 2015 /PRNewswire/ ... Biomedical Engineering Research of the University of ... Diabetes and Clinical Nutrition of the Bern University Hospital ... exclusive collaboration to develop a novel generation artificial pancreas. ... delivery of insulin for diabetic patients with the unequalled ...
(Date:11/24/2015)... 2015 F1000Workspace - a research ... it was launched just six months ago. --> ... platform for scientists - since it was launched just six ... loaded on to F1000Workspace - a research collaboration, ... was launched just six months ago. --> ...
Breaking Medicine Technology: