BioLineRx receives two U.S. patent allowances for BL-1021 to treat neuropathic pain

BioLineRx, a biopharmaceutical development company, announced today that two Notices of Allowance have been issued by the United States Patent and Trademark Office (USPTO) for BL-1021 (see structure), an orally available small molecule for treating neuropathic pain. The first has been issued for a patent application claiming BL-1021's composition, that when issued, will be valid until at least September 2022. Additional patents claiming BL-1021's composition are granted or pending in Europe, Japan, Canada, Korea, Mexico, Israel, India, China and Australia. The other Notice of Allowance is for a patent application claiming the use of BL-1021 for the treatment of pain, that when issued, will be valid until at least January 2028.

BioLineRx receives two U.S. patent allowances for BL-1021 to treat neuropathic pain: BioLineRx, a biopharmaceutical development company, announced today that two Notices of Allowance have been issued by the United States Patent and Trademark Office (USPTO) for BL-1021, an orally available small molecule for treating neuropathic pain.

Novel way to treat drug-resistant brain tumor cells

In continuation of my update on Lapatinib

Research by Dr. Paul Clark, a scientist in Kuo's lab and the study's lead author, shows why. When cetuximab treatment switches off EGFR activity and should inhibit cancer-cell growth, cancer stem cells compensate by turning on two other EGFR family receptors (ERBB2 and ERBB3) and continue to grow. One of these receptors, ERBB2, is implicated in certain types of chemotherapy-resistant breast cancer. Fortunately, another novel drug already approved by the FDA, lapatinib (see the structure), inhibits ERBB2 activity and signaling by multiple EGFR members.

This study shows that cancer stem-cell growth was markedly inhibited by lapatinib treatment, which results in combined knockout of multiple EGFR family members.

"This is good news, because these drugs target an important mechanism for the (GBM) cancer cells to grow so quickly and evade current therapies, and these molecularly targeted drugs are also well-tolerated by patients and have minimal side effects," Dr. Clark said.

Ref : http://www.med.wisc.edu/news-events/wisconsin-research-team-reveals-novel-way-to-treat-drug-resistant-brain-tumor-cells/37811

Novel way to treat drug-resistant brain tumor cells: New research explains why the incurable brain cancer, glioblastoma multiforme (GBM), is highly resistant to current chemotherapies.

Increased fiber intake associated with lower risk of dying over twelve year period - Life Extension Update

Fiber could promote health via several mechanisms, including helping to control weight, improving glycemic control, and aiding in the maintenance of a favorable intestinal environment. Fiber may help protect against circulatory diseases by lowering low density lipoprotein (LDL) cholesterol, which, when elevated, is a major risk factor for cardiovascular disease. Fiber intake has also been associated with a reduction in inflammatory markers including C-reactive protein, interleukin-6 and tumor necrosis factor-alpha. The authors note that greater total fiber intake could be a marker of an overall dietary pattern that benefits health.

"We observed inverse associations between total dietary fiber intake and mortality, and specifically mortality from circulatory, digestive, and non-cardiovascular disease, noncancer inflammatory diseases," the authors conclude. "These results show that high fiber intake, mainly from cereals and vegetables, may reduce the risk of death from these diseases." 

Increased fiber intake associated with lower risk of dying over twelve year period - Life Extension Update

Drug Combo Tackling Solid Tumors

Cancer Research UK's Drug Development Office has opened the first trial of a new drug combination in patients with advanced solid tumors and in a subset of patients who have non-small cell lung cancer. This trial will combine two compounds that aim to starve the tumors while simultaneously blocking cancer cell growth.

The study will take place across three UK hospitals. The Churchill Hospital, Oxford is the lead center. The trial of up to 48 patients will run in two stages. In the first stage patients with any solid tumor will each receive a drug called vandetanib (below left) and an investigational drug called selumetinib (right structure below)AZD6244, ARRY142886). In the second stage patients with non-small cell lung cancer (NSCLC) will receive the combination.

This is the first time the compounds have been trialled together. It is hoped that combining these treatments will increase the number of cancer ‘weakspots’ targeted at the same time.

Chief investigator, Dr. Denis Talbot, consultant medical oncologist at Oxford University Hospitals NHS Trust and Cancer Research UK clinician at The University of Oxford, said: “Therapies for lung cancer often become ineffective because the disease becomes resistant to treatment, so we’re delighted to launch this trial to test a new approach that we hope will help people with this common disease.

“There is progress being made in the treatment of lung cancer but survival rates still remain low. This is because the majority of patients – up to two thirds – are diagnosed once the cancer has already spread to other organs when it’s more difficult to treat successfully.

 “We hope that this new approach may eventually contribute to increased survival for lung cancer patients.”

Ref : http://cancerhelp.cancerresearchuk.org/trials/a-trial-of-vandetanib-and-selumetinib-for-solid-tumours-including-nsclc-vansel-1

Takeda announces updated results from orteronel phase 2 study on nmCRPC

Takeda announces updated results from orteronel phase 2 study on nmCRPC: Millennium: The Takeda Oncology Company with its parent company Takeda Pharmaceutical Company Limited today announced updated results from a phase 2 study of orteronel, a selective oral 17,20 lyase inhibitor, dosed without prednisone in patients with non-metastatic castration resistant prostate cancer (nmCRPC) and rising prostate-specific antigen.

Ref : http://investor.millennium.com/phoenix.zhtml?c=80159&p=irol-newsArticle&ID=1702187&highlight=

Antisense Pharma presents data from trabedersen Phase I/II cancer study at ASCO 2012

In continuation of my update on antisense drugs

Trabedersen, is an antisense compound that specifically inhibits expression of transforming growth factor beta 2 (TGF-β2) – a protein which is overexpressed in advanced tumors and which triggers key cancer pathomechanisms, i.e. suppression of antitumor immune response and metastasis. 

Antisense Pharma presents data from trabedersen Phase I/II cancer study at ASCO 2012: The biopharmaceutical company Antisense Pharma today presents trabedersen complete data from its clinical Phase I/II study in patients with advanced pancreatic cancer, malignant melanoma or colorectal cancer at the international cancer congress ASCO 2012 in Chicago, USA.

Ancient berry could protect against diabetic retinopathy

In continuation of my update on wolfberry

Ancient berry could protect against diabetic retinopathy: The ancient Tibetan goji berry could help fight blindness caused by long-term diabetes according to studies conducted by University of Sydney researchers.

Dapivirine Phase III trial now underway in Africa to treat HIV in women

Dapivirine Phase III trial now underway in Africa to treat HIV in women

Investigational diabetes drug appears to improve insulin sensitivity without side effects

Drugs for type 2 diabetes can contribute to weight gain, bone fractures and cardiovascular problems, but in mice, an investigational drug appears to improve insulin sensitivity without those troublesome side effects, researchers at Washington University School of Medicine in St. Louis have shown.

"Current diabetes medications activate a receptor that improves insulin sensitivity, but unfortunately also contributes to side effects that make some people discontinue the medication, contributing to other health problems," says principal investigator Brian N. Finck, PhD. "So even though these drugs are effective, we'd really like to find new insulin-sensitizing therapies that would avoid activating the same receptor."

Finck, a research assistant professor of medicine in the Division of Geriatrics and Nutritional Science, worked with colleagues at the University of Michigan and at the drug discovery company Metabolic Solutions Development Co., LLC. The scientists studied one of the company's investigational drugs, MSD-0602, focusing on its effects in obese mice.

The drug improved blood glucose levels and insulin tolerance in the mice, as did the two diabetes drugs that already are on the market: rosiglitazone (Avandia) and pioglitazone (Actos). All three medications appeared to be about equally effective, but MSD-0602 didn't bind to and activate a receptor in cells called PPARγ. Rather, the investigational drug clings to the mitochondria, part of the cell that produces energy.

"The drug altered the cell's ability to generate energy," Finck says. "And it also seems to have an anti-inflammatory role in the cell. We also found that the drug improved insulin sensitivity in many different kinds of cells including muscle, fat and liver cells."

 Next, he and his colleagues will attempt to identify proteins that bind to the mitochondrial membrane. Future therapies then could be developed specifically to bind to those proteins while avoiding activation of the PPARγ pathway.

Investigational diabetes drug appears to improve insulin sensitivity without side effects: Drugs for type 2 diabetes can contribute to weight gain, bone fractures and cardiovascular problems, but in mice, an investigational drug appears to improve insulin sensitivity without those troublesome side effects, researchers at Washington University School of Medicine in St. Louis have shown.

Ref : http://www.jbc.org/content/early/2012/05/23/jbc.M112.363960.full.pdf

Cyclacel Presents New Phase 2 Data of Sapacitabine for MDS

We know that, Sapacitabine is an oral nucleoside analog prodrug that acts through a dual mechanism. The compound interferes with DNA synthesis by causing single-strand DNA breaks and induces arrest of the cell division cycle at G2 phase. Both sapacitabine and its major metabolite, CNDAC, have demonstrated potent anti-tumor activity in both blood and solid tumors in preclinical studies. In a liver metastatic mouse model, sapacitabine was shown to be superior to gemcitabine (Gemzar; Lilly) or 5-FU, two widely used nucleoside analogs, in delaying the onset and growth of liver metastasis.

Cyclacel has initiated a number of clinical trials to evaluate sapacitabine in both solid and hematological tumors laying the foundation for future Phase 2 studies and combination studies with other anti-cancer agents. Three Phase 1 studies have been completed, which evaluated safety and pharmacokinetics of a variety of dosing schedules in approximately 120 patients with solid tumors. Sapacitabine is currently being evaluated in two Phase 2 trials in patients with advanced cutaneous T-cell lymphoma (CTCL) and in elderly patients with acute myeloid leukemias (AML).

Now Cyclacel Pharmaceuticals, Inc. announced new data from an ongoing, multicenter, Phase 2 randomized trial of oral sapacitabine capsules in older patients with myelodysplastic syndromes (MDS) after treatment failure of front-line hypomethylating agents, such as azacitidine or decitabine.