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

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Synta's ganetespib shows potent in vitro and in vivo activity against multiple breast cancer types

Synta researchers  have reported that, Ganetespib (structure)  shows potent in vitro and in vivo activity against multiple types of breast cancer including HER2-positive, ER/PR positive, triple-negative, and inflammatory breast cancer. 

"These results demonstrating that ganetespib potently inhibits key signaling pathways involved in the growth and proliferation of multiple forms of breast cancer are encouraging, and supportive of the results presented earlier at this meeting showing single-agent, anti-tumor activity in patients with breast cancer who have progressed on or failed to respond to multiple prior therapies," said Vojo Vukovic, M.D., Ph.D., Chief Medical Officer, Synta. 

Researchers conclude that, the combined preclinical and clinical results create a strong rationale for advancing ganetespib development in both HER2-positive and triple-negative breast cancer.

More : http://phoenix.corporate-ir.net/phoenix.zhtml?c=147988&p=irol-newsArticle&ID=1638540&highlight=

Combination of bortezomib and panobinostat shows promise against advanced multiple myeloma

In co\continuation of  my update on Bortezomib...

A phase 2 clinical trial has shown that pairing bortezomib with an experimental drug, panobinostat: Panobinostat is a histone deacetylase (HDAC) inhibitor, a type of drug that blocks key processes involved in gene expression and protein degradation. Panobinostat clogs up a protein disposal mechanism in myeloma cells so that harmful byproducts accumulate and eventually cause programmed cell death.(see below structure), may be a promising new treatment for such patients, Dana-Farber Cancer Institute researchers say.

 The PANORAMA 2 trial included 53 patients with relapsed multiple myeloma who had undergone multiple rounds of prior treatment and, in more than half, also stem cell transplant. The researchers reported on 44 patients receiving the panobinostat-bortezomib-dexamethasone combination.

Results showed that in the first phase of the treatment, 9 of the patients had at least a partial response of their disease, and 2 of the 9 saw their myeloma almost disappear, a so-called near complete response. Another 7 patients experienced minimal response, which is also associated with clinical benefit. 

More : http://ash.confex.com/ash/2011/webprogram/Paper41145.html

Ruxolinitib reduces spleen size by 35% in patients with myelofibrosis

In continuation of my ruxolinitib

In a major advance in treatment, a multicenter study found that ruxolinitib did a better job than off-label chemotherapy drugs reducing the terrible symptoms associated with myelofibrosis, including pain, enlarged spleen, anemia, fever, chills, fatigue, and weight loss. 

Only about 10 percent of myelofibrosis patients are eligible for a bone marrow transplant and chemotherapy often falls short, Dr. Mesa says. A handful of off-label chemotherapy drugs have been modestly helpful, he says.

A randomized, double-blind clinical trial, known as the COMFORT-1 study, showed that ruxolinitib reduced spleen size by more than 35 percent in almost all of the 154 patients studied. An enlarged spleen, caused by sequestered over-proliferating blood cells, causes discomfort and can also lead to the need for blood transfusions and further medical complications for patients.

"The studies confirmed the drug is very effective. As a representative of a particular class of molecular inhibitors called JAK2 inhibitors, which are now being widely studied, ruxolinitib suggests this category will continue to be promising for myelofibrosis," Dr. Mesa says.

Ref : More...

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

UMass Amherst Researchers Test a Drug-Exercise Program Designed to Prevent Type 2 Diabetes

In continuation of my update on Metformin...

Kinesiology researcher Barry Braun of the University of Massachusetts Amherst and colleagues recently reported unexpected results of a study suggesting that exercise and one of the most commonly prescribed drugs for diabetes, metformin, each improves insulin resistance when used alone, but when used together, metformin blunted the full effect of a 12-week exercise program in pre-diabetic men and women.

Ref : http://www.umass.edu/newsoffice/newsreleases/articles/142505.php

Editorial: An apple a day keeps colitis away

In continuation on my update on the benefits of apple

Editorial: An apple a day keeps colitis away:

More : http://msuextension.org/publications/AgandNaturalResources/MT200812AG.pdf

'via Blog this'

European Commission approves Vyndaqel® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP)

We know that, Tafamidis (see structure) or Vyndaqel was discovered in the Jeffery W. Kelly Laboratory at The Scripps Research Institute using a structure-based drug design strategy and was developed at FoldRx pharmaceuticals, a biotechnology company led by Richard Labaudiniere that was acquired by Pfizer in 2010.

Tafamidis or Vyndaqel functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. In patients with FAP, this protein dissociates in a process that is rate limiting for aggregation including amyloid fibril formation, causing neurodegeneration and failure of the autonomic nervous system and/or the peripheral nervous system and/or the heart.

Now, European Commission has approved Vyndaqel^® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy.

More...

HSC NEWS - Bat plant could give some cancers a devil of a time

In a new study published this month in the Journal of the American Chemical Society, researchers with The University of Texas Health Science Center at San Antonio have pinpointed the cancer-fighting potential in the bat plant, or Tacca chantrieri......

HSC NEWS - Bat plant could give some cancers a devil of a time

FDA Approves Intermezzo.....

The U.S. Food and Drug Administration today approved Intermezzo (zolpidem tartrate sublingual tablets) for use as needed to treat insomnia characterized by middle-of-the-night waking followed by difficulty returning to sleep.

This is the first time the FDA has approved a drug for this condition. Intermezzo should only be used when a person has at least four hours of bedtime remaining. It should not be taken if alcohol has been consumed or with any other sleep aid....

More....

Coffee may protect against womb cancer: Study

 In continuation of my update on the benefits of coffee

A new study shows that regular intake of coffee may significantly lower risk for endometrial or womb cancer.

For the study the researchers looked at coffee consumption and endometrial cancer risk in more than 67,000 women aged between 34 and 59 enrolled in the long-running Nurses' Health Study. The researchers found that women who took more than four cups of coffee a day over a 26-year period were 25 percent less likely to get the cancer. Women who drank two to three cups a day were 7 percent less likely to get it. Drinking less than four cups a day was not associated with reduced risk. Furthermore drinking tea did not reduce the risk. Additionally drinking more than two cups of decaffeinated coffee a day was tied to a 22 percent reduced risk for endometrial cancer.

The benefit wasn't a complete surprise, since coffee has been shown to lower estrogen and insulin levels, and higher levels of these hormones have been associated with an increased risk of endometrial cancer. But the new findings do help to clarify how obesity, estrogen and coffee might interact in triggering tumors.

“It would be premature to make a recommendation that women drink coffee to lower their endometrial cancer risk,” study author Dr. Edward Giovannucci, professor of nutrition and epidemiology at Harvard School of Public Health...

Ref : http://cebp.aacrjournals.org/content/early/2011/10/03/1055-9965.EPI-11-0766.abstract?sid=d8d229ed-e4b4-4b7a-bc6a-f3f86cba4c0e