Archive for February, 2012

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Potential Help for Millions with Type 2 Diabetes from Dapagliflozin Treatment

Wednesday, February 29th, 2012

dapagliflozinDapagliflozin, CAS number 461432-26-8, is currently being reviewed by the FDA for treatment of type 2 diabetes in adults. Developed by Bristol-Myers Squibb and AstraZeneca, the method of action of dapagliflozin is to inhibit the subtype 2 of the sodium-glucose transport proteins, or SGLT2. This particular subtype is responsible for at least 90% of the glucose reabsorption in the kidney. By blocking this  transporter blood glucose is able to be easily eliminated through the urine. As of January 19, 2012  AstraZeneca announced that the U.S. Food and Drug Administration (FDA) had issued a complete response letter regarding the New Drug Application (NDA) for the investigational compound dapagliflozin. Both Bristol-Myers Squibb and AstraZeneca stated that they will work closely with the FDA to determine the appropriate next steps for the dapagliflozin application. LGM Pharma is a provider of the API dapagliflozin for research and development.

Foot on ScaleDapagliflozin is being investigated and evaluated for use as a monotherapy, in combination with other anti-diabetic agents, and as an adjunct treatment to diet and exercise in patients with type 2 diabetes. More than 5,000 patients in 19 clinical studies have participated in trials, and the need for newer treatments for the ever growing population of adults with type 2 diabetes is essential. Aston University researchers conducted a study with roughly 450 adults with type 2 diabetes. Each patient was given either one of three dosages of dapagliflozin or a placebo. These patients were all taking the highest maximum dose of metformin, yet still not seeing lowered blood sugar levels. Patients in this study received 24 weeks of treatment with dapagliflozin, and the results were encouraging, showing a significant reduction in blood sugar levels in all patients who were on a dose of dapagliflozin. These results can be further explored here: http://www.youtube.com/watch?v=KTRs0XIsXvQ&feat.

Concerns remain from the FDA, however, as to safety and efficacy of dapagliflozin. Discernment about which patients would benefit the most from the use of dapagliflozin, as well as concerns over cancer risks led to the current request for further data from Bristol-Myers Squibb and AstraZeneca. Clinical trials reported thus far indicate an increased risk for both breast and bladder cancer. About 0.4 percent of women taking dapagliflozin got breast cancer, compared with 0.1 percent of the women in the control group. As for the men in the study 0.3 percent of men who received dapagliflozin got bladder cancer, compared with about 0.05 percent of men who received the placebo. While these numbers are not staggering, some members of the advisory committee of the FDA expressed concern over any risks from dapagliflozin, even in small numbers. A decision and potential approval of this once a day pill is anticipated by October of 2012.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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Dronedarone for Patients with Non Permanent Atrial Fibrillation

Monday, February 27th, 2012

Atrial FibrillationPatients with the condition of non permanent cardiac arrhythmia are typical candidates for dronedarone. Approved by the FDA in July of 2009, dronedarone is manufactured by Sanofi-Aventis, is also known as SR33589, and was marketed as Multaq. Dronedarone, CAS number 141626-36-0, can be an essential treatment for both atrial fibrillation and atrial flutter. LGM Pharma is a provider of the API dronedarone CAS# 141626-36-0 for research and development.

Offered as 400 milligram tablets, dronedarone is appropriate for patients with non-permanent atrial fibrillation/flutter (AF/AFL). As of July 21, 2011 the FDA voiced concern over the use of dronedarone in patients with permanent AF. Preliminary studies using the brand Multaq for this patient population indicated a two fold increase in death, stroke and hospitalization for patients who received Multaq versus a placebo. This study, deemed PALLAS, is currently under review by the FDA. Providers must be cognizant and not prescribe dronedarone to any patients with permanent AF or AFL until further direction from the FDA is disseminated.

DronedaroneUsually given as a twice daily dosage, dronedarone should not be dispensed to patients who have ever been diagnosed with heart failure. Side effects include rash, heartburn, weakness and diarrhea. Patients must tell their doctors if they already take anticoagulants, beta-blockers, certain antidepressants and vitamins or supplements, as these may alter the efficacy of dronedarone. Information about the potential risk of severe liver injury was added by the FDA to the label for dronedarone in January 2011, amid concerns of possible hepatic injury and/or toxicity. This was deemed as an urgent communication from the FDA after two liver transplant cases came to light from patients who had been treated with Multaq. Recommendations from the FDA suggest that patients taking dronedarone for atrial fibrillation should be monitored at least every three months to document the absence of their arrhythmia.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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Atazanavir Sulfate Essential Treatment for HIV Infected Patients

Monday, February 27th, 2012

Atazanavir SulfateAtazanavir Sulfate, CAS number 229975-97-7, is essential in the management of HIV in affected patients. As an inhibitor of the HIV-1 protease, atazanavir sulfate is often used in combination with other antiretroviral medications to treat HIV-1 infected patients. LGM Pharma is a provider of the API atazanavir sulfate for research and development.

With a trade name Reyataz (Bristol-Myers Squibb), atazanavir sulfate is availible in capsule form, in doses of 100, 150, 200 or 300 milligrams. Patients commonly receive one dose daily, alongside additonal medications, as well as food. A typical complementary treatment given alongside atazanavir sulfate is ritonavir. Atazanavir is also a stand alone option for those patients who cannot tolerate ritonavir. Also offered as a prophylaxis for possible HIV exposure to healthcare workers, atazanavir sulfate is crucial to the treatment of HIV-1 infections.

Contraindictions include hyperbilirubinemia, cardiac abnormailities, rash and dermatologic reactions, hyperglycemia, hemophilia and hepatic impairment. Common side effects include headache, dizziness, depression, insomnia, diarrhea, abdominal pain and jaundice. Even with the negative effects possible with treatment for patients using atazanavir sulfate, the positive effects of this drug greatly outweigh the negative effects. Atazanavir sulfate enables patients with HIV to extend their lives and manage their symptoms and disease.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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Linaclotide a New Hope for Patients with Chronic Constipation

Thursday, February 23rd, 2012

linaclotideLinaclotide, CAS Number 851199-59-2,  is an exciting new drug, aimed at helping patients with Irritable Bowel Syndorme and Constipation (IBS-C). As patients suffering from both IBS and constipation also experience abdominal pain, linaclotide is touted to relieve both constipation and abdominal pain. Linaclotide is a first in class, 14-amino acid peptide guanylate cyclase-C (GC-C) receptor agonist, as well as an intestinal secretagogue. LGM Pharma is a provider of Linaclotide for research and development purposes.

On October 24, 2011 the FDA accepted for review the New Drug Application (NDA) for linaclotide to treat irritable bowel syndrome with constipation (IBS-C), as well as chronic constipation (CC). The review is expected to take ten months, and the  target date for potential approval is aimed for June 2012.  Ironwood Pharmaceuticals, Inc. and Forest Laboratories, Inc. have reported positive results from their Stage 3 clinical trials. The most recent data from a Phase 3 program included four double-blind placebo-controlled trials and two open-label long term safety studies. With more then 2,800 patients receiving either a once daily dose of linaclotide or a placebo, significant improvements were noted in the patients who received linaclotide. These patients reported marked improvement with abdominal pain, abdominal discomfort, bloating, and bowel symptoms.

With diarrhea being the most common adverse event reported in linaclotide-treated patients, other unwanted effects reported include flatulence and headaches. Linaclotide is an oral capsule and has been administered once daily in trials. Usually taken before the first meal of the day, doses ranged in trials from 75 to 3000 mcg daily. The duration of therapy ranged from a single dose to 26 weeks.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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Is Lorcaserin the Next Weight Loss Drug?

Tuesday, February 21st, 2012

LorcaserinIntended for weight management, including weight loss and maintenance of weight loss, lorcaserin is poised to become the next weight loss drug. Lorcaserin is aimed at clinically obese patients, or patients with a Body Mass Index, or BMI, >30, or patients who are overweight (BMI >27) and have at least one weight related co-morbid condition. Arena Pharmaceuticals, Inc. and Eisai Inc. submitted a New Drug Application (NDA) for lorcaserin on January 10th, 2012, and the FDA has accepted this resubmission. Previously submitted to the FDA in October of 2010, lorcaserin was not approved. The concern was data reported which indicated mammary tumors in female rats. As the cancer promoting properties could not be ruled out, and due to marginal weight loss results reported, a federal advisory committee voted against the approval of lorcaserin at that time.

As a selective 5-HT2C receptor agonist, lorcaserin is believed to target this receptor in the brain and hypothalamus, which are areas thought to be involved in the control of appetite and metabolism. This activation of the 5-HT2C receptors in the hypothalamus are believed to activate proopiomelanocortin (POMC) production, thus promoting weight loss through satiety. While the particulars and the exact mechanism of appetite regulation is not completely understood, lorcaserin has shown 100:1 affinity for 5-HT2C receptors versus other receptors.

BMI ChartPhase 2 clinical trials from Arena have demonstrated that patients who received lorcaserin experienced a significantly greater weight loss than patients who received a placebo. Another earlier trial, deemed BLOSSOM, was reported on September 18, 2009. These positive findings showed that 47. 2% of lorcaserin patients lost at least 5% of their body weight, compared to 25. 0% of patients on the placebo. Taking 10 milligrams of lorcaserin either once or twice daily, patients also experienced an average weight loss of 5. 9%, or 12. 7 pounds. This was compared to 2. 8%, or 6. 3 pounds, for patients on the placebo.

Adverse side effects reported during trials of lorcaserin included headache, dizziness, and nausea. The FDA has assigned a new Prescription Drug User Fee Act (PDUFA) target date of June 27, 2012 for lorcaserin. LGM Pharma is a provider of Lorcaserin CAS# 846589-98-8 for research and development purposes. Lorcaserin has an expected trade name of Lorqess.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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