Breakthrough in Treatment to Prevent Blindness | www.ucsf.edu

In continuation of my update on Azithromycin....
Breakthrough in Treatment to Prevent Blindness | www.ucsf.edu

A Novel Neurotrophic Drug for Cognitive Enhancement and Alzheimer's Disease

A new drug candidate may be the first capable of halting the devastating mental decline of Alzheimer's disease.  The drug, known as J147 (above  structure), improved memory and prevented brain damage caused by the disease claims the researchers from Salk's Cellular Neurobiology Laboratory, lead by David Schubert. The new compound,  could be tested for treatment of the disease in humans in the near future.Researchers add that, J147 enhances memory in both normal and Alzheimer's mice and also protects the brain from the loss of synaptic connections.

Salk researchers went on to show that it prevented cognitive decline in animals with Alzheimer's and that mice and rats treated with the drug produced more of a protein called brain-derived neurotrophic factor (BDNF), a molecule that protects neurons from toxic insults, helps new neurons grow and connect with other brain cells, and is involved in memory formation.

Because of the broad ability of J147 to protect nerve cells, the researchers believe that it may also be effective for treating other neurological disorders, such as Parkinson's disease, Huntington's disease and amyotrophic lateral sclerosis (ALS), as well as stroke.

Although it is yet unknown whether the compound will prove safe and effective in humans, the Salk researchers' say their results suggest the drug may hold potential for treatment of people with Alzheimer's...

Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0027865

Bristol-Myers Squibb and Tibotec partner to evaluate daclatasvir-TMC435 combination for HCV

Bristol-Myers Squibb and Tibotec partner to evaluate daclatasvir-TMC435 combination for HCV: Bristol-Myers Squibb Company announced today that it has entered into a clinical collaboration agreement with Tibotec Pharmaceuticals to evaluate the utility of daclatasvir (BMS-790052), Bristol-Myers Squibb's investigational NS5A replication complex inhibitor, in combination with Tibotec Pharmaceuticals' investigational NS3 protease inhibitor, TMC435, for the treatment of chronic hepatitis C virus (HCV).

Alkermes commences ALKS 9070 phase 3 clinical trial for schizophrenia...

Alkermes plc (NASDAQ: ALKS)  announced the initiation of a phase 3 clinical trial of ALKS 9070 (Aripiprazole) for the treatment of schizophrenia. ALKS 9070, a proprietary Alkermes molecule, is designed to provide patients with once-monthly dosing of a medication that, once in the body, converts into aripiprazole...

Ref : http://phx.corporate-ir.net/phoenix.zhtml?c=92211&p=irol-corporateNewsArticle&ID=1640788&highlight=

Lostartan can reduce cigarette smoke-induced lung injury

Researchers from Johns Hopkins University, BaltimoreLostartan, lead by have found that, Dr.Enid R. Neptune Losartan a drug used widely in the clinic (e.g., to treat high blood pressure), reduced lung disease in mice caused by exposure to cigarette smoke. Losartan blocks the protein angiotensin receptor type 1, and its effects on cigarette smoke-induced lung injury were a result of the fact that blocking angiotensin receptor type 1 leads to a decrease in levels of the soluble molecule TGF-beta. The authors therefore suggest that other TGF-beta-targeted therapeutics might also be viable candidates for the treatment of  chronic obstructive pulmonary disease, COPD....

Ref : http://www.jci.org/articles/view/46215?search[article_text]=&search[authors_text]=Enid+Neptune

MK 1775 shows promise against sarcomas..........

   2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6- (4-(4-methyl- piperazin-1-yl)phenylamino)-1H-pyra -zolo [3,4-d]pyrimidin-3(2H)-one.  

MK 1775 (see structure), a small, selective inhibitor molecule, has been found to be active against many sarcomas when tested by researchers at Moffitt Cancer Center in Tampa, Fla. Researchers found that MK1775 treatment induces apoptopic cell death in four sarcoma cell lines at clinically relevant doses.

To further prove that inhibition of Wee1 by MK1775 leads to mitotic cell death in sarcomas cells, the researchers performed additional studies, including studies on sarcomas related to mutations, such as with the p53 gene. They also showed that MK1775 was an active inhibitor of Wee1 regardless of the p53 mutation status of the tumors in the cell lines tested.

"The cytotoxic effect of Wee1 inhibition on sarcoma cells appears to be independent of p53 mutation status following our testing sarcoma cell lines with different p53 mutations," he said. "All of them were highly sensitive to MK1775, suggesting that Wee1 inhibition may represent a novel approach in the treatment of sarcomas."

Researchers concluded that their laboratory tests on sarcoma cell lines suggest that MK1775 is effective as a monotherapy even in the cell lines that include p53 wild, p53 null and p53 mutant statuses.

More... 

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint

In continuation of my update on gemcitabine

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint: Oncolytics Biotech Inc. announced the interim data from a Phase 2 clinical trial using intravenous administration of REOLYSIN® in combination with gemcitabine (Gemzar) in patients with advanced pancreatic cancer (REO 017) indicated that the clinical study had successfully reached its primary endpoint, and that the drug combination is active.

New Antibodies Treat Autoimmune Disease like Crohn's in Mice....

 Synthetic drugs treat (below structure)  Crohn's disease in mice.................

[zinc-binding motif (where X is any amino acid) in MMPs, a symmetrical tripodal tris-imidazol–zinc complex (Zn-tripod; ZnC₃₆H₅₉N₁₁O₈)]


New Antibodies Treat Autoimmune Disease in Mice
Ref : http://www.nature.com/nm/journal/vaop/ncurrent/full/nm.2582.html

Salk scientists develop new drug that improves memory and prevents brain damage in mice

A new drug candidate may be the first capable of halting the devastating mental decline of Alzheimer's disease, based on the findings by a research group of Salk's Cellular Neurobiology Laboratory.

When given to mice with Alzheimer's, the drug, known as J147 (see structure), improved memory and prevented brain damage caused by the disease. The new compound, developed by scientists at the Salk Institute for Biological Studies, could be tested for treatment of the disease in humans in the near future.

"J147 enhances memory in both normal and Alzheimer's mice and also protects the brain from the loss of synaptic connections," says David Schubert, the head of Salk's Cellular Neurobiology Laboratory, whose team developed the new drug. "No drugs on the market for Alzheimer's have both of these properties."

Although it is yet unknown whether the compound will prove safe and effective in humans, the Salk researchers' say their results suggest the drug may hold potential for treatment of people with Alzheimer's.

More.....

Notch inhibitor appears to treat breast cancer....

In a novel therapeutic approach to treating breast cancer, Loyola University Medical Center researchers are reporting positive results from a clinical trial of a drug that targets tumor stem cells. A pilot study at Loyola found that an experimental drug known as a "notch inhibitor" appears to block this process by turning off key genes. Prior to surgery, the patients received one of two commonly used drugs, tamoxifen or letrozole. These drugs work by blocking estrogen stimulation of breast cancer cells. In addition to tamoxifen or letrozole, patients also received the experimental notch-inhibitor drug, MK-0752 (see structure).

 "The notch inhibitor appears to be doing what it is intended to do," said Dr. Clodia Osipo....

There were minimal side effects from either the notch inhibitor or the estrogen-blocking drugs. One patient experienced puffy eyes and coughing and four patients experienced facial acne. No patients experienced diarrhea or surgical complications.

Ref : Loyola Medicine News Release

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

In continuation of my update on Zoledronic acid....

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

Scientists identify why African naked mole-rat feels no pain when exposed to acid

In continuation of my update  naked mole-rat

Scientists identify why African naked mole-rat feels no pain when exposed to acid: British researchers of the Max Delbr-ck Center for Molecular Medicine (MDC) Berlin-Buch have found out why the African naked mole-rat (Heterocephalus glaber), one of the world's most unusual mammals, feels no pain when exposed to acid.

Ref : http://www.mdc-berlin.de/en/news/2011/20111220-mdc_researchers__ion_channel_makes_african1/index.html

Drug Duo of Ixabepilone and sunitinib Kills Chemotherapy-resistant Ovarian Cancer Cells......

In continuation of Sunitinib...

The use of two drugs never tried in combination before in ovarian cancer resulted in a 70 percent destruction of cancer cells already resistant to commonly used chemotherapy agents, say researchers at Mayo Clinic in Florida. Research  suggests that this combination (ixabepilone and sunitinib), might offer a much needed treatment option for women with advanced ovarian cancer. When caught at late stages, ovarian cancer is often fatal because it progressively stops responding to the chemotherapy drugs used to treat it. The finding also highlights the importance of the role of a molecule, RhoB, that the researchers say is activated by the drug duo. Neither drug is approved for use in ovarian cancer. Ixabepilone is a chemotherapy drug that, like other taxane drugs, targets the microtubules and stops dividing cells from forming a spindle. It has been approved for use in metastatic breast cancer. Sunitinib, approved for use in kidney cancer, belongs to a class of tyrosine kinase inhibitors that stops growth signals from reaching inside cancer cells.

                                           

     Sunitinib                                  Ixabepilone

Ref : http://www.mayoclinic.org/news2011-jax/6573.html

Geron Initiates Phase 2 Trial of GRN1005 in Brain Metastases from Breast Cancer

In continuation of my update on Paclitaxel and drug discovery....

Geron Corporation, announced the initiation of GRABM-B (GRN1005 Against Brain Metastases - Breast Cancer), a Phase 2 clinical trial to evaluate GRN1005 in patients with brain metastases arising from breast cancer. GRN1005 is the company's lead LRP-directed peptide-drug conjugate (LRP-directed PDC) that consists of the cytotoxic drug, paclitaxel, linked to a peptide (Angiopep-2) that targets the LRP receptor to cross the blood-brain barrier (BBB) and to target tumors in the brain.

The purpose of the Phase 2 study is to assess the efficacy, safety and tolerability of GRN1005 in patients with brain metastases from breast cancer. The trial is designed to include 100 patients with HER2 positive or HER2 negative metastatic breast cancer (MBC) disease, who will be assessed in two separate cohorts of 50 patients each.....

More...

Ref : http://www.geron.com/media/pressview.aspx?id=1287

Drug combination highly effective for newly diagnosed myeloma patients......

A three-drug combination treatment for the blood cancer multiple myeloma compares favorably to the best established therapy for newly diagnosed patients, according to a multi-center study led by Andrzej Jakubowiak, MD, PhD, professor of medicine and director of the multiple myeloma program at the University of Chicago Medical Center.

( Carfilzomib)

 (Lenalidomide)

( Thalidomide)

The combination includes an investigational medicine called carfilzomib combined with two standard medications: lenalidomide, an analogue of thalidomide, and low-dose dexamethasone, an anti-inflammatory with anti-cancer properties.

"This combination appears to deliver everything we expected and more," said Jakubowiak, who came to the University of Chicago this fall from the University of Michigan. "We have seen excellent efficacy — the best reported to date — without the neurotoxicity that has been problematic with other drug combinations."

Ref : http://www.uchospitals.edu/news/2011/20111206-myeloma.html