Monday, August 31, 2015

Chemical compound shows promise in treating rheumatoid arthritis



ChemSpider 2D Image | (11Z)-11H-Indeno[1,2-b]quinoxalin-11-one oxime | C15H9N3O





Montana State University researchers and their collaborators have published their findings about a chemical compound that shows potential for treating rheumatoid arthritis.

The paper ran in the June issue of the Journal of Pharmacology and Experimental Therapeutics (JPET), and one of its illustrations is featured on the cover. JPET
is a leading scientific journal that covers all aspects of pharmacology, a field that investigates the effects of drugs on biological systems and vice versa.

"This journal is one of the top journals that reports new types of therapeutics that are being developed," said Mark Quinn, senior author on the paper and a professor in MSU's Department of Microbiology and Immunology. The department is part of the College of Agriculture and the
College of Letters and Science.

Rheumatoid arthritis is a chronic autoimmune disorder that affects an estimated 1.3 million people in the world, Quinn said. Characterized by stiff, swollen joints, it's a progressive disease that occurs when the body's immune system attacks its own cells. Inflammation in the lining of the joints leads to loss of bone and cartilage. People who have rheumatoid arthritis lose mobility and joint function without adequate treatment.

New kinds of drugs have been developed for treating the disease, Quinn said. Called biological drugs, or "biologics," they are made from genetically engineered proteins or antibodies that act on substances in the immune system. When used to treat rheumatoid arthritis, they interrupt signals that fuel the inflammatory process. Two such drugs are ENBREL and HUMIRA.

Biologics can be expensive, however, and some people don't respond to
them, Quinn said. Some people respond at first, but not forever.

"There is a real need to develop new kinds of drugs that are different," Quinn said. "They could be combined with other available drugs or replace drugs that aren't working for patients."

Researchers in his laboratory and elsewhere identified a new chemical compound, called IQ-1S, in a previous study, Quinn said. Then they conducted a new study to understand how the   small-molecule  compound
works against rheumatoid arthritis. They explained their findings in the JPET paper.  

Ref : http://jpet.aspetjournals.org/content/353/3/505.abstract?sid=8b8e3977-7bbd-40f4-ab43-f37402878df0



Chemical compound shows promise in treating rheumatoid arthritis

Friday, August 28, 2015

Salix Pharmaceuticals receives FDA approval for Xifaxan 550 mg to treat IBS-D in adults



Rifaximin.svg
In continuation of my update on xifaxan

Valeant Pharmaceuticals International, Inc. (NYSE: VRX) (TSX: VRX) announced that its wholly owned subsidiary, Salix Pharmaceuticals, Inc., has received approval from the U.S. Food and Drug Administration (FDA) for Xifaxan® 550 mg for the treatment of IBS-D in adults. The FDA approval of Xifaxan 550 mg is based on data from three phase 3 studies, TARGET 1, TARGET 2 and TARGET 3. Xifaxan 550 mg was studied in over 3,000 patients and demonstrated the efficacy and safety of repeat treatment following completion of a two-week course of treatment. A full course of Xifaxan 550 mg for IBS-D is available in a convenient 2 week pack of 42 pills.

"As a gastroenterologist who helps patients navigate the symptoms of IBS-D, I see the need for treatments that directly address those most bothersome, such as diarrhea and abdominal pain" said Dr. Mark Pimentel, director of the Gastrointestinal Motility Program and Laboratory at Cedars-Sinai in Los Angeles. "Today's approval gives a new option to these patients and providers."


Thursday, August 27, 2015

Actavis announces FDA approval of VIBERZI (eluxadoline) for IBS-D treatment

In continuation of my update on VIBERZI (eluxadoline)



Actavis plc,  announced today that VIBERZI™ (eluxadoline) was approved by the Food and Drug Administration (FDA) as a twice-daily, oral treatment for adults suffering from irritable bowel syndrome with diarrhea (IBS-D). VIBERZI (eluxadoline) has mixed opioid receptor activity, it is a mu receptor agonist, a delta receptor antagonist, and a kappa receptor agonist.

"The FDA's approval of VIBERZI is the first step to providing physicians with a new, evidence-based, treatment option for their adult patients with IBS-D," said David Nicholson, Executive Vice President, Actavis Global Brands R&D. "At Actavis, we are dedicated to providing new treatment options, and the development of new agents that help address the most bothersome symptoms of IBS-D. We are very pleased to be working with the FDA to advance this IBS-D treatment and we eagerly await DEA scheduling determination later this year."




Eluxadoline.png

Ref : http://pubchem.ncbi.nlm.nih.gov/compound/11250029#section=Canonical-SMILES


Actavis announces FDA approval of VIBERZI (eluxadoline) for IBS-D treatment

Tuesday, August 25, 2015

First-line axitinib ‘feasible’ in advanced, metastatic RCC


Axitinib2DACS.svg




We know that, Axitinib (AG013736; trade name Inlyta) is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models and has shown partial responses in clinical trials with renal cell carcinoma (RCC) and several other tumour types.  It was approved by the U.S. Food and Drug Administration after showing a modest increase in progression-free survival, though there have been reports of fatal adverse effects...
--------------------------------------------------------------------------------------

Now..

A Japanese single-institution study suggests that axitinib may be a feasible first-line option for patients with locally advanced or metastatic renal cell carcinoma (RCC). Axitinib treatment resulted in “improved oncological outcomes” and had an “acceptable safety profile”, say the researchers in BMC Urology.

The team reviewed medical records for 18 patients with locally advanced or metastatic RCC who received first-line axitinib for a median duration of 10.8 months, five and nine patients had a partial response and stable disease, respectively, while four progressed.



Monday, August 24, 2015

Drug combination lengthens lives of metastatic colorectal cancer patients


                         fluoropyrimidine                    TAS-102

Capecitabine.svg Capecitabine


A drug developed 50 years ago and abandoned because it was considered to be too toxic has gained a second life in an international clinical trial. Research led by scientists at Dana-Farber Cancer Institute showed the drug and a potentiating agent lengthened the lives of patients with metastatic colorectal cancer, all of whom had exhausted available standard treatments.

In a paper published online today by the New England Journal of Medicine, investigators at Dana-Farber and research centers around the world found that the drug combination - given as a single pill known as TAS-102 - not only extended patients' overall survival, but also delayed the advance of the disease and did so with very few side effects.

According to the study authors, the results are especially impressive because half of the patients had just finished treatment with the standard class of chemotherapy agents - fluoropyrimidines (e.g. 5-fluorouracil [5-FU] or capecitabine [Xeloda]) but had failed to benefit from them. The fact that TAS-102 temporarily halted the disease in many of these patients suggests that it operates through a different biochemical pathway than 5-FU, and therefore may serve as an alternative to standard therapy.

"Colorectal cancer is the second most common cause of cancer deaths [after lung cancer] in the United States and is an enormous health problem around the world," said the study's lead author, Robert J. Mayer, MD, faculty vice president for academic affairs, medical oncologist and colorectal cancer researcher at Dana-Farber. "To have a well-tolerated, effective new drug in a cancer that is so prevalent is good news for patients."

The trial, a phase 3 study involving major cancer research institutions in Europe, the United States, Australia and Japan, enrolled 800 patients with metastatic colorectal cancer that was progressing despite previous treatment. Participants were randomly assigned to receive TAS-102 or a placebo pill...

More : http://www.nejm.org/doi/full/10.1056/NEJMoa1414325

Friday, August 21, 2015

Mifepristone-eribulin combination clinically active in triple-negative breast cancer patients

Corcept Therapeutics Incorporated, a pharmaceutical company engaged in the discovery, development and commercialization of drugs that treat severe metabolic, oncologic and psychiatric disorders by modulating the effects of cortisol, today announced results of a multi-center Phase 1/2 dose-escalation study of mifepristone and chemotherapy drug eribulin (Halaven®) 

Mifepristone.svg Mifepristone (or RU-486)

Eribulin.svgeribulin (Halaven®)

that show it is well tolerated and clinically active in patients with triple-negative breast cancer. These results were published in the 2015 American Society of Clinical Oncology (ASCO) Annual Meeting Program (abstract e12070), which was released today.

“Triple-negative breast cancers are among the most aggressive and difficult to treat of all the breast cancer types. We are encouraged by the results we have seen using mifepristone to enhance the efficacy of chemotherapy in this patient population,” said Rita Nanda, MD, principal investigator and Associate Director, Breast Medical Oncology, University of Chicago Medicine. “Cancer patients abundantly produce the stress hormone cortisol, which can help tumor cells escape chemotherapy effectiveness when cortisol binds to the cells’ glucocorticoid receptors (GR). Because mifepristone also binds with tumor GR, we are postulating that mifepristone will lessen the cortisol activity in tumor cells and make chemotherapy more effective. Patients with triple-negative breast cancer need better treatments and we are hopeful that mifepristone when combined with chemotherapy, will benefit them.”

Researchers enrolled 13 metastatic breast cancer patients for the first phase of the study to determine the maximum tolerated dose of the mifepristone-eribulin combination. The results showed that the combination regimen was well-tolerated with evidence of clinical activity for patients with triple-negative breast cancer (TNBC). The recommended Phase 1/2 dose of 300 mg of mifepristone daily with 1.1./mg/m2 of eribulin showed no evidence of a drug-drug interaction and will be used in the next phase of the study. An additional 20 patients with GR-positive metastatic TNBC will be enrolled into the study’s efficacy phase.

Thursday, August 20, 2015

Drug combination lengthens lives of metastatic colorectal cancer patients


                         fluoropyrimidine                    TAS-102

Capecitabine.svg Capecitabine


A drug developed 50 years ago and abandoned because it was considered to be too toxic has gained a second life in an international clinical trial. Research led by scientists at Dana-Farber Cancer Institute showed the drug and a potentiating agent lengthened the lives of patients with metastatic colorectal cancer, all of whom had exhausted available standard treatments.

In a paper published online today by the New England Journal of Medicine, investigators at Dana-Farber and research centers around the world found that the drug combination - given as a single pill known as TAS-102 - not only extended patients' overall survival, but also delayed the advance of the disease and did so with very few side effects.

According to the study authors, the results are especially impressive because half of the patients had just finished treatment with the standard class of chemotherapy agents - fluoropyrimidines (e.g. 5-fluorouracil [5-FU] or capecitabine [Xeloda]) but had failed to benefit from them. The fact that TAS-102 temporarily halted the disease in many of these patients suggests that it operates through a different biochemical pathway than 5-FU, and therefore may serve as an alternative to standard therapy.

"Colorectal cancer is the second most common cause of cancer deaths [after lung cancer] in the United States and is an enormous health problem around the world," said the study's lead author, Robert J. Mayer, MD, faculty vice president for academic affairs, medical oncologist and colorectal cancer researcher at Dana-Farber. "To have a well-tolerated, effective new drug in a cancer that is so prevalent is good news for patients."

The trial, a phase 3 study involving major cancer research institutions in Europe, the United States, Australia and Japan, enrolled 800 patients with metastatic colorectal cancer that was progressing despite previous treatment. Participants were randomly assigned to receive TAS-102 or a placebo pill...

More : http://www.nejm.org/doi/full/10.1056/NEJMoa1414325

Wednesday, August 19, 2015

Combination of contraceptive and cholesterol-lowering drugs kills cancer cells in a new way

The combination of a cholesterol-lowering drug, Bezafibrate (first left structure), and a contraceptive steroid, Medroxyprogesterone Acetate (second right), could be an effective, non-toxic treatment for a range of cancers, researchers at the University of Birmingham have found.

Bezafibrate.svg   Medroxyprogesterone 17-acetate.png
The findings published in the journal Cancer Research show that the drugs kill cancer cells in a completely new way.

Early stage clinical trials of the drugs in elderly patients with acute myeloid leukaemia (AML) have shown promising results, with survival three months longer on average than standard palliative care. The combination, known as BaP, has also been used alongside chemotherapy to successfully treat children with Burkitt's lymphoma (BL), the most common childhood cancer in Eastern Africa.

Until now it was uncertain whether the activity of the drugs against these two very different blood cancers was mediated by a common mechanism or by different effects in each cancer type.

The scientists, who were funded by Leukaemia & Lymphoma Research, used state of the art technology to interrogate the drug's effects on the metabolism and chemical make-up of AML and BL cells and found that in both cell types the drugs block an enzyme crucial to the production of fatty acids, which cancer cells need to grow and multiply. They also demonstrated that the ability of BaP treatment to deactivate this enzyme, called stearoyl CoA desaturase, was what prompted cancer cells to die.

Read More at Cancer Research

Tuesday, August 18, 2015

Combination therapy provides promising results in patients with advanced non-small cell lung cancer

An early phase study testing an anti-PDL1 agent in combination with standard chemotherapy in the treatment of advanced non-small cell lung cancer has provided promising early results, prompting multiple phase III studies in lung cancer. The findings are being presented at the annual meeting of the American Society of Clinical Oncology (ASCO).

In this phase 1b study, patients with untreated non-small cell lung cancer received one of three standard platinum-based chemotherapy regimens (paclitaxel/carboplatin, pemetrexed/carboplatin or nab-paclitaxel/carboplatin) with MPDL3280A, an antibody targeting PD-L1. Early results from the 

Taxol.svgPaclitaxel Carboplatin-skeletal.svgCarboplatin Pemetrexed.svgPemetrexed

first 37 patients showed impressive response rates between 60-75 percent, comparing favorably to historical outcomes with chemotherapy alone, where historical response rates from randomized trials are around 30 - 35 percent. In addition, two complete responses already have been documented, with no evidence of lung cancer on CT scans.

"A complete response is not typically seen in patients with stage IV lung cancer," says the abstract's lead author, Stephen V. Liu, MD, assistant professor of medicine at Georgetown Lombardi Comprehensive Cancer Center. "And the response rates seen with MPDL3280A and chemotherapy were higher than one would expect with chemotherapy alone."

Monday, August 17, 2015

STA, Helsinn announce approval of AKYNZEO for prevention of chemotherapy-induced CINV

In continuation of my update on AKYNZEO®

Australian biopharmaceutical company Specialised Therapeutics Australia (STA) and Helsinn, a Swiss group focused on building quality cancer care, announce that the Therapeutic Goods Administration (TGA) has approved AKYNZEO® for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately and highly emetogenic cancer chemotherapy.
AKYNZEO® is the first approved fixed dose combination oral agent that targets two critical signalling pathways associated with CINV by combining netupitant, an NK1receptor antagonist, and palonosetron, a 5-HTreceptor antagonist, in a single capsule for the prevention of CINV. 

Netupitant.svg
Palonosetron structure.svg

"Cancer patients are burdened with having to take multiple drugs, often several times per day and certainly multiple times per cycle of chemotherapy, to reduce unwanted side effects. With every increased drug/schedule there is an increased risk of mistakes and/or non-compliance," said Professor Dorothy Keefe, Clinical Ambassador, Transforming Health and Professor of Cancer Medicine, University of Adelaide. "The availability of this combination of drugs, in a single capsule, allows 'once per cycle' dosing (which is even better than once per day dosing) for the benefit of the patient."

The approval of AKYNZEO® was based on the submission of Phase 2 and Phase 3 trials with AKYNZEO® in patients undergoing treatment with moderately and highly emetogenic chemotherapy regimens for a variety of tumour types. The most common adverse reactions reported by ≥ 1% of patients treated with AKYNZEO® for one or more cycles were headache, constipation and fatigue.

STA Chief Executive Officer Mr Carlo Montagner said AKYNZEO® was a valuable addition to STA's Oncology Supportive Care portfolio, providing patients with access to an effective and convenient antiemetic therapy. "We look forward to making this drug available to cancer patients around the country, for improved management of some of the most common side effects of chemotherapy, which can severely diminish a patient's quality of life. STA will now seek to have AKYNZEO® listed on the Pharmaceutical Benefits Scheme for reimbursement."

Friday, August 14, 2015

Cholesterol-lowering statin drugs could delay prostate cancer growth in patients receiving ADT

In a study published online today by JAMA Oncology, the researchers report that men who had been taking statins since the start of androgen deprivation therapy (ADT) went a median of 27.5 months before their disease began to worsen, compared to 17.4 months for men who didn't take statins. The trial involved 926 patients, 70 percent of whom had their disease progress during a six-year period.

"This median 10-month benefit in delaying disease progression suggests that statins could be a valuable addition to our current therapies for prostate cancer," says the study's first author, Lauren Harshman, MD, medical oncologist at the Lank Center for Genitourinary Oncology at Dana-Farber. "These results are supported by multiple prior epidemiologic studies demonstrating that statin use may be associated with improved outcomes in prostate cancer, but require validation."

The trial grew out of laboratory studies that suggested statins could delay prostate cancer growth in patients receiving ADT. (ADT reduces the amount of androgen in the body, preventing prostate cancer cells from using it to fuel their growth. For many years, it has been the frontline treatment for patients with hormone-sensitive prostate cancer that has spread beyond the prostate gland.)
The laboratory phase of the research focused on a protein called SLCO2B1, which helps a variety of drugs and hormones enter cells. One of these immigrants to the cell is dehydro-epiandrosterone  sulfate (DHEAS), a precursor of testosterone, the hormone that spurs prostate cancer cell growth. Statin drugs, too, rely on SLCO2B1 to gain entry to cells.

More : http://oncology.jamanetwork.com/article.aspx?articleid=2288665

Thursday, August 13, 2015

Dexamethasone May Help Prevent Severe Kidney Injury Following Heart Surgery

In continuation of my update on dexamethasone....Skeletal formula of dexamethasone

The anti-inflammatory drug dexamethasone helps prevent serious kidney complications that can arise following heart surgery, according to the results of a randomized clinical trial. The findings, which appear in an upcoming issue of the Journal of the American Society of Nephrology (JASN), could lead to a change in care for patients during cardiac operations.

Acute kidney injury (AKI) is one of the most devastating complications following cardiac surgery. Approximately 1% of patients undergoing cardiac surgery require dialysis to treat severe AKI that arises after surgery, and the incidence is higher among patients with pre-operative chronic kidney disease. These patients experience strikingly high death rates while in the hospital that exceed 40%. "One percent sounds like a small percentage, however given the fact that each year, over half a million people undergo heart surgery in the United States alone, this means that an estimated 5000 patients develop renal failure and of those about 2500 die as a result of this complication," said Kirolos Jacob, MD (University Medical Center, Utrecht, The Netherlands). He noted that these figures are rising due to the aging population.

Because heart surgery initiates an inflammatory reaction in the body that can have negative effects on the kidneys, Dr. Jacob and his colleagues wondered whether giving patients dexamethasone, an anti-inflammatory drug, could decrease the risk of severe AKI following cardiac surgery. The team analyzed the results of a large randomized controlled trial called the Dutch Dexamethasone for Cardiac Surgery (DECS) trial, which included 4465 patients undergoing cardiac surgery who were randomized to receive placebo or dexamethasone during surgery. The original trial tested whether dexamethasone could reduce the risk of a variety of major postoperative complications. In this analysis, the investigators specifically examined kidney failure and focused on the most severe form: AKI requiring dialysis.

Dexamethasone appeared to protect against the development of severe AKI. Patients who received the drug had about a 2.5-times lower risk of developing AKI requiring dialysis compared with those receiving a placebo.

"The beneficial effects of dexamethasone were particularly present in those who already had pre-existing kidney disease before heart surgery," said Dr. Jacob. "This reinforces the fact that this drug could be of major importance for the increasing elderly population with pre-existing kidney disease undergoing a heart operation."

Read more at : http://dx.doi.org/10.1681/ASN.2014080840

Wednesday, August 12, 2015

Potential new painkiller provides longer lasting effects ..........



Medications have long been used to treat pain caused by injury or chronic conditions. Unfortunately, most are short-term fixes or cause side effects that limit their use. Researchers at the University of Missouri have discovered a new compound that offers longer lasting painkilling effects, and shows promise as an alternative to current anesthetics.

"Because of its versatility and effectiveness at quickly numbing pain in targeted areas, lidocaine has been the gold standard in local anesthetics for more than 50 years," said George Kracke, Ph.D., associate professor of anesthesiology and perioperative medicine at the MU School of Medicine and lead author of the study. "While lidocaine is effective as a short-term painkiller, its effects wear off quickly. We developed a new compound that can quickly provide longer lasting relief. This type of painkiller could be beneficial in treating sports injuries or in joint replacement procedures."

Painkillers work by interfering with the nervous system's transmission of nerve signals that the body perceives as pain. Lidocaine is used as an injectable pain reliever in minor surgical or dental procedures, or as a topical ointment or spray to relieve itching, burning and pain from shingles, sunburns, jellyfish stings and insect bites. The new compound developed at MU, boronicaine, could potentially serve many of those same functions as an injectable or topical painkiller.
National Academy of Sciences member M. Frederick Hawthorne, Ph.D., director of MU's International Institute of Nano and Molecular Medicine and a pioneer in the field of boron chemistry, synthesized boronicaine as a derivative of lidocaine. By changing aspects of the chemical structure of lidocaine, the researchers found that the new compound provided pain relief that lasted five times longer than lidocaine. In pre-clinical, early stage studies, boronicaine provided about 25 minutes of relief, compared to about five minutes of pain relief with lidocaine.

"Although some conditions may warrant the use of a short-lasting painkiller, in many cases a longer lasting anesthetic is a better option," Kracke said. "Having a longer lasting anesthetic reduces the dosage or number of doses needed, limiting the potential for adverse side effects." While other types of painkillers can provide longer pain relief than lidocaine, they can cause heart toxicity, gastrointestinal issues and other side effects. Preliminary findings show no toxicity in single-dose studies of boronicaine, though more studies are needed.
"Boronicaine could have distinct advantages over existing painkilling medications," said Hawthorne, who also serves as the Curators' Distinguished Professor of Chemistry and Radiology at MU. "We're conducting more research into the side effects of the compound, but in time it could very well become a useful material to use as an anesthetic."

Ref : http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201402369/pdf

Tuesday, August 11, 2015

Viagra to prevent transmission of the malaria parasite?



By increasing the stiffness of erythrocytes infected by the causal agent of malaria, Viagra favors their elimination from the blood circulation and may therefore reduce transmission of the parasite from humans to mosquitoes. This astonishing discovery, made by scientists from the CNRS, INSERM, Universit√© Paris Descartes -- at the Institut Cochin -- and the Institut Pasteur, working in collaboration with a team from the London School of Hygiene and Tropical Medicine, could lead to a treatment to reduce the spread of malaria within a population. Their work is published in PLOS Pathogens on 7 May 2015.


More : http://journals.plos.org/plospathogens/article?id=10.1371/journal.ppat.1004815



Viagra to prevent transmission of the malaria parasite? 

Monday, August 10, 2015

Plant-derived compound targets cancer stem cells

In continuation of my updates on cauliflower, cabbage, broccoli

A compound and an enzyme that occur naturally in cruciferous vegetables--cauliflower, cabbage, broccoli and Brussels sprouts--may help prevent recurrence and spread of some cancers, according to researchers. When they treated human cervical cancer stem cells with phenethyl isothiocyanate (PEITC) in a Petri dish, about 75 percent died within 24 hours using a 20-micromolar concentration of the compound.  
Phenethyl isothiocyanate.svg

A compound and an enzyme that occur naturally in cruciferous vegetables -- cauliflower, cabbage, broccoli and Brussels sprouts -- may help prevent recurrence and spread of some cancers, according to associate professor Moul Dey of the South Dakota State University Department of Health and Nutritional Sciences. She has been doing research on phenethyl isothiocyanate (PEITC) through a five-year grant from the National Institutes of Health for more than $875,000 and support from the South Dakota Agricultural Experiment Station.
The precursor compound and enzyme in cruciferous vegetables combine during the chewing process to produce PEITC within the body, Dey explained. Though PEITC is a good candidate to develop as a dietary supplement, studies have also shown that sufficient cancer-preventing levels of PEITC can be achieved through diet alone.
Role of cancer stem cells
When cancer is treated with chemotherapy or radiation, the tumor disappears but the cancer stem cells live on. "These cells are frequently resistant to conventional therapies," Dey said.
Though cancer stem cells make up less than 5 percent of a tumor, they can regenerate the original tumor and migrate through the blood vessels spreading cancer to secondary locations.
"These tiny cells are very difficult to detect in a tumor," Dey pointed, adding that for a long time scientists did not even know they existed. "It's like finding a needle in a haystack."

Promising Results
When Dey and her team treated human cervical cancer stem cells with PEITC in a Petri dish, about 75 percent died within 24 hours using a 20-micromolar concentration of the compound.
In other experiments, Dey and her team have found that lower concentrations of PEITC are still very effective. Working with SDSU veterinary pathologist David Knudsen, Dey and her team found that 10-micromolar concentrations of PEITC can dramatically prevent the spread of cancer in mouse lung tissue.

"Preliminary evidence has shown a quite dramatic difference between the lung sections from the PEITC-treated and untreated mice," Dey said. However, she cautioned, although mice provide a model for human diseases, further testing is necessary to determine whether outcomes will be similar in humans.

Based on information from scientific literature, the concentrations of PEITC that Dey and her team typically use in their research -- 5 to 15 micromolars -- may be achieved through diets rich in certain types of cruciferous vegetables, particularly land and watercress.

Next, she and her team will examine how PEITC is able to overcome the resistance mechanisms that protect these stem cells from other drugs. "That's the second piece of this work," Dey added.

Friday, August 7, 2015

FDA Expands Uses of Vyvanse to Treat Binge-Eating Disorder



Lisdexamfetamine-Structural Formula V.1.svg


Lisdexamfetamine (contracted from L-lysine-dextroamphetamine) is a central nervous system (CNS) stimulant prodrug of thephenethylamine and amphetamine chemical classes. Its chemical structure consists of dextroamphetamine coupled with the essential amino acid L-lysine. Lisdexamfetamine itself is inactive and acts as a prodrug to dextroamphetamine upon cleavage of the lysine portion of the molecule.

---------------------
The U.S. Food and Drug Administration today expanded the approved uses of Vyvanse (lisdexamfetamine dimesylate) to treat binge-eating disorder in adults. The drug is the first FDA-approved medication to treat this condition.

In binge-eating disorder, patients have recurrent episodes of compulsive overeating during which they consume larger amounts of food than normal and experience the sense that they lack control. Patients with this condition eat when they are not hungry and often eat to the point of being uncomfortably full. Patients may feel ashamed and embarrassed by how much they are eating, which can result in social isolation. Binge-eating disorder may lead to weight gain and to health problems related to obesity.

FDA Expands Uses of Vyvanse to Treat Binge-Eating Disorder

Thursday, August 6, 2015

FDA Approves Prezcobix (darunavir and cobicistat) for HIV-1 Infection in Adults

Darunavir2DCSD.svg

In continuation of my update on darunavir  


Janssen Therapeutics, Division   of    Janssen    Products, LP     (Janssen), today announced the U.S. Food and Drug Administration (FDA)    has approved Prezcobix   (darunavir 800 mg/cobicistat 150 mg) tablets, an HIV-1  protease inhibitor combined with a CYP3A4 inhibitor, for the treatment of human immunodeficiency virus (HIV-1) in combination with other antiretroviral agents for treatment-naive and treatment-experienced adults with no darunavir resistance-associated substitutions.




FDA Approves Prezcobix (darunavir and cobicistat) for HIV-1 Infection in Adults

Wednesday, August 5, 2015

FDA Approves Glyxambi (empagliflozin and linagliptin) for Type 2 Diabetes



Empagliflozin.svg



In continuation of my update on empagliflozin



The U.S. Food and Drug Administration (FDA) has approved Glyxambi (empagliflozin/linagliptin) tablets, from Boehringer Ingelheim Pharmaceuticals, Inc. (BIPI) and Eli Lilly and Company (NYSE: LLY), as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes (T2D) when both empagliflozin and linagliptin are appropriate treatments. Glyxambi is not recommended in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Glyxambi has not been studied in patients with a history of pancreatitis, and it is unknown if using Glyxambi increases the risk of developing pancreatitis in these patients.

Glyxambi is not recommended in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Glyxambi has not been studied in patients with a history of pancreatitis, and it is unknown if using Glyxambi increases the risk of developing pancreatitis in these patients.

Tuesday, August 4, 2015

FDA Approves Ibrance (palbociclib) for Postmenopausal Women with Advanced Breast Cancer



Palbociclib.svg


In continuation of my update on palbociclib

The U.S. Food and Drug Administration today granted accelerated approval to Ibrance (palbociclib) to treat advanced (metastatic) breast cancer.

Breast cancer in women is the second most common type of cancer in the United States. It forms in the breast tissue and in advanced cases, spreads to surrounding normal tissue. The National Cancer Institute estimates that 232,670 American women were diagnosed with breast cancer and 40,000 died from the disease in 2014.
Ibrance works by inhibiting molecules, known as cyclin-dependent kinases (CDKs) 4 and 6, involved in promoting the growth of cancer cells. Ibrance is intended for postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer who have not yet received an endocrine-based therapy. It is to be used in combination with letrozole, another FDA-approved product used to treat certain kinds of breast cancer in postmenopausal women.

FDA Approves Dutrebis (lamivudine and raltegravir) for HIV-1 Infection



Lamivudine structure.svg   Raltegravir structure.svg


The United States Food and Drug Administration (FDA) has approved Dutrebis, a fixed dose combination tablet containing 150 mg of lamivudine and 300 mg of raltegravir. Dutrebis tablet is approved for use in combination with other antiretroviral products for the treatment of HIV-1 infection in adults and pediatric patients greater than or equal to 6 years of age weighing at least 30 kg. The recommended dosage of Dutrebis is one tablet taken twice daily with or without food.

Dutrebis approval was based on an open-label, single dose, randomized, two-period, crossover study in healthy subjects (n=108). One Dutrebis fixed dose combination table was shown to provide comparable lamivudine and raltegravir exposures to one Epivir 150 mg tablet plus on Isentress 400 mg tablet. Due to the higher bioavailability of raltegravir contained in Dutrebis, the exposures provided by the 300 mg dose of raltegravir are comparable to 400 mg of ralegravir given as the raltegravir poloxamer formulation (Isentress), which accounts for the difference in raltegravir dose.


Monday, August 3, 2015

FDA Approves Lenvima (lenvatinib) for Differentiated Thyroid Cancer


LENVIMA (lenvatinib) Structural Formula Illustration



LENVIMA, a kinase inhibitor, is the mesylate salt of lenvatinib. Its chemical name is 4- [3chloro-4-(N’-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carbox- amide methanesulfonate. The molecular formula is C21H19ClN4O4•CH4O3S, and the molecular weight of the mesylate salt is 522.96. The chemical structure of lenvatinib mesylate is:

The U.S. Food and Drug Administration today granted approval to Lenvima(lenvatinib) to treat patients with progressive, differentiated thyroid cancer (DTC) whose disease progressed despite receiving radioactive iodine therapy (radioactive iodine refractory disease).

FDA Approves Lenvima (lenvatinib) for Differentiated Thyroid Cancer