Archive for the ‘Therapeutic Classification’ Category

Liraglutide FDA Approval Brings First Ever Injectable Weight Loss Drug

Monday, January 26th, 2015

Liraglutide FDA Approved As 1st Ever Injectable Weight Loss DrugThe close of 2014 brought exciting news for Novo Nordisk’s innovative weight loss drug Saxenda. The Liraglutide FDA approval is the first of its kind as it’s the only available injectable treatment for obesity. The FDA overwhelmingly gave a nod to this easy to use form of Liraglutide as a safe and effectual option for patients suffering from obesity and in need of medical weight loss. Already approved in 2010 by the FDA for Type 2 Diabetes as the trade name Victoza, Liraglutide has proven to be an efficacious product aimed at combating the most common cause of diabetes worldwide. The newly approved Saxenda will contain a greater amount of Liraglutide than its initial product, Victoza, and it is designed to be an effective GLP-1 agonist that will promote weight loss and weight control.

The increase of obesity globally has become a serious and costly epidemic. Chronic management of obesity is called for, with treatments like Liraglutide considered to be a positive step in the right direction. As of 2015 one-third of adults in the United States are estimated to be classified as obese. The Liraglutide FDA approval of Saxenda (rDNA origin injection) is specifically endorsed as an adjunct treatment for chronic weight management alongside both increased physical activity and a healthy diet. Liraglutide works for weight control by sending a message of satiety to the center of the brain, which in turn slows down the stomach. Liraglutide has been documented in clinical trials to work exceptionally well at controlling hunger especially during the initial weeks of treatment, which naturally parlays to early weight loss and feelings of success amongst patients.

A landmark clinical trial which involved patients who were classified as obese but who were not diabetic showed an average yearly weight loss of 4.5 percent, as compared to a placebo. Approximately 49 percent of the patients who received Liraglutide as Saxenda lost at least 5 percent of their body weight. The dosage of Liraglutide is 3.0 milligrams per day, which is considerably higher than the dosing for patients with Type 2 Diabetes, which is between 1.2 milligrams and 1.8 milligrams daily. Adverse effects proved to be rare amongst trial participants. Common side effects reported were nausea and upset stomach, however no patient ended their participation due to these effects.

Another pivotal study, coined SCALE™, or Satiety and Clinical Adiposity−Liraglutide Evidence in Non-diabetic and Diabetic adults, proved to be noteworthy in the phase 3 clinical trial segment. Over 5,000 patients were enrolled in this trial, who were considered to be either obese or overweight. All patients exhibited various comorbidities associated with their condition. The use of Liraglutide for participants in this trial, combined with a reduced calorie diet and active exercise resulted in decidedly greater weight loss as compared to diet and exercise alone. Additionally, patients involved in the aforementioned study were able to gain control over weight related comorbid conditions, such as hypertension, high glycemic levels and dyslipidemia. Patients are advised to avoid the use of Liraglutide as Saxenda for weight control if they are currently using insulin, have or have had pancreatitis or are taking other products to promote weight loss.

LGM Pharma can assist clients as a supplier/distributor of the API Liraglutide, CAS # 204656-20-2, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

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.

Mocetinostat Trials Commence for Lymphoma and Bladder Cancer Treatments

Monday, January 19th, 2015

Two encouraging trials commenced at the start of 2015 for anti-cancer therapy Mocetinostat. Both studies, sponsored by Mirati Therapeutics, focus on this powerful and selective inhibitor of HDAC 1, 2, 3 and 11, which all are major players in the regulation of cancer gene expression. As an orally-bioavailable therapy, Mocetinostat has been at the forefront of over a dozen clinical trials worldwide, involving more than 400 patients with both solid tumors and hematologic malignancies.

non-hodgkins-lymphoma

Image courtesy of cancer.org

Mocetinostat therapy is currently involved in an investigator sponsored Phase 2 study for patients with non-Hodgkin’s lymphoma. This study began on January 6, 2015 and is focused on specific deletions and mutations of the EP300 and CREBBP genes in lymphomas. These mutations and deletions are implicated in both refractory and relapsed follicular lymphoma and diffuse large B-cell lymphoma. Utilizing targeted treatment alongside genetic sequencing has led to an exciting endeavor for researchers seeking to find potential predictive responses in patients with the aforementioned genetic mutations who are administered Mocetinostat. Approximately 25 percent of patients who are diagnosed with diffuse large B-cell lymphoma and follicular lymphoma have the EP300 and CREBBP mutations. This open-label Phase 2 study thus far has 54 patients with refractory non-Hodgkin’s lymphoma enrolled, as well as 27 patients with follicular lymphoma and 27 patients diffuse large B-cell lymphoma. The clinical trial participants will receive a dosage of 90 milligrams of Mocetinostat three times a week on a 28 day schedule. The FDA has granted an Orphan Drug Designation to Mocetinostat as a treatment for patients with diffuse large B-cell lymphoma.

Bladder Cancer

Image courtesy of patienteducationcenter.org

Another Mocetinostat study has begun for patients with bladder cancer who have histone acetyltransferase gene CREBBP and EP300 mutations. This Phase 2 clinical trial will evaluate the safety and efficacy of Mocetinostat in this patient population. Roughly one-quarter of patients diagnosed with bladder cancer have the EP300 and CREBBP mutations. The use of Mocetinostat as a pointed HDAC inhibitors leads researchers to believe a targeted dysregulation in histone and DNA acetylation will occur in the patients with these types of bladder cancer. Participants in this trial will receive an oral capsule of Mocetinostat three times a week on a 28 day cycle. Many years have elapsed without new therapies to treat bladder cancer, which becomes metastatic in more than 50 percent of patients. The use of a potent treatment like Mocetinostat is an exciting development in the fight against refractory cancer of the bladder. The most frequently reported grade 3 and 4 adverse effects from treatment with Mocetinostat have been fatigue and neutropenia.

Mocetinostat CAS 726169-73-9LGM Pharma can assist clients as a supplier/distributor of the API Mocetinostat, CAS # 726169-73-9, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

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.

Is Mirabegron the Next Treatment to Combat Obesity?

Tuesday, January 13th, 2015
activated human brown fat

PET images of a 21-year-old man who was given placebo (top) or 200 mg of the β3-AR agonist mirabegron (bottom). Twelve male subjects were given placebo or 200 mg mirabegron.

The January 6, 2015 issue of Cell Metabolism offered exciting news regarding the fight against obesity. Mirabegron, an FDA approved drug for treating overactive bladder, appears to be a viable option for combatting obesity as well. The secret is in Mirabegron’s ability to metabolize brown fat, which generates heat by burning energy, which fights obesity. The new research focused on how Mirabegron effected both the white fat and brown fat in rodents and humans. While the white fat in the body stores energy, the brown fat utilizes the energy, leading to weight loss and weight maintenance.

The aforementioned study was small and involved a dozen young, healthy men who had not previously taken Mirabegron. The male participants were administered 200 milligrams of Mirabegron daily, roughly 50 milligrams higher than the optimal dose for patients taking this drug for overactive bladder. Results were encouraging, with all of the men showing an average increase in their resting metabolic rate by about 203 calories per day. The ability of Mirabegron, as an effectual β3-adrenergic receptor, to stimulate human brown adipose tissue led to the participants’ ability to burn more calories. The assumption is that by Mirabegron leading to a higher rate of glucose consumption, weight loss and maintenance may not be the only advantages of Mirabegron. Research and development teams are now exploring whether Mirabegron may also hold the key to the management of type 2 diabetes. The brown fat, or brown adipose tissue, generates β3-adrenergic receptor levels higher than just about every other organ in the human body. The unique ability of this already approved drug makes Mirabegron an API to watch.

Mirabegron CAS No: 223673-61-8Currently approved as the brand name drug Myrbetriq, marketed by Astellas Pharmaceuticals, Mirabegron is approved for the treatment of overactive bladder. In the class of drugs coined beta-3 adrenergic agonists, Mirabegron works by curtailing frequent, uncontrolled and urgent urination by relaxing the bladder muscles. A long-acting tablet is available for patients, which is taken once daily, with or without food. Adverse effects are uncommon, with most side effects reported being minor. A small number of patients currently taking Mirabegron for overactive bladder experience headache, dizziness, dry mouth and stomach pain.

LGM Pharma can assist clients as a supplier/distributor of the Mirabegron, CAS # 223673-61-8 API for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

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.

NRTI Lamivudine Looks Promising for AMD Treatment

Monday, January 5th, 2015

As an efficacious treatment for the HIV virus, the NRTI Lamivudine is now showing promise as a drug to combat age-related macular degeneration, known also as AMD. Nucleoside reverse transcriptase inhibitors, or NRTIs are the most commonly used class of anti-HIV medications and they are touted to successfully act on the enzyme reverse transcriptase, prohibiting the replication of the HIV virus which causes AIDS. A milestone study, recently released from the Kentucky University’s Department of Ophthalmology and Visual Sciences investigated nucleoside reverse transcriptase inhibitors (NRTIs), a class of drugs that has been used to treat HIV/AIDS for the past 30 years, and revealed innovative research regarding the NRTI Lamivudine for the treatment of AMD. Patients suffering from age-related macular degeneration experience a collection of the toxic molecule RNA in the retina, causing this debilitating condition. The toxic RNA molecule is remarkably similar to the HIV virus, as both need the reverse transcriptase enzyme to conclude their life cycle. These landmark findings have extended the possibilities for the use of not only Lamivudine for the treatment of AMD, but also many other NRTIs like Zidovudine, CAS # 30516-87-1 and Stavudine, CAS # 3056-17-5.

Age- related macular degeneration is a serious disease that leads to progressive vision loss and is currently untreatable in 90 percent of patients. The two forms of AMD are classified as dry and wet. The most common form is dry AMD, as it accounts for most cases. Wet AMD is less common, occurring in less than 10 percent of cases, however it can become virulent quickly. Statistics show that over 11 million adults in the United States have partial or total blindness due to AMD, and this figure is expected to double by the year 2050. Worldwide cases of AMD are estimated to surpass 200 million people worldwide by 2020. The FDA has not approved any therapies to combat dry AMD to date.

Research gleaned has indicated that NRTIs, specifically Lamivudine, staves off cell death in mice. A pleasant surprise for researchers was the ability of NRTIs to block the group of proteins coined inflammasones. These overactive inflammasones contribute to AMD and are believed to purport several other diseases such as atherosclerosis, diabetes and Alzheimer’s disease. Concern regarding adverse effects among scientists using Lamivudine and other NRTIs to treat AMD is apparent, however it is a minor concern. The re-purposing of NRTIs for the treatment of dry AMD relies on the past research and development of these crucial drugs, with the majority of adverse effects originally associated with these drugs being allayed by perfecting their use. While negative side effects were of concern when NRTIs were initially administered there has been a plethora of safety information gathered by R&D over the past several decades. Reduced dosing regimens, alongside newer compounds with effectual safety profiles makes the use of NRTIs for conditions other than HIV prudent. Lamivudine, in specific, has been deemed to be a remarkably safe and effective drug, with virtually no negative side effects. Perhaps this information is why researchers are looking at Lamivudine as a possible treatment for Ebola as well. The “off-label” use and acceptability of NRTIs is becoming widely praised across the globe, leading to hope and excitement for the future of pharmaceutical research. LGM Pharma can assist clients as a supplier/distributor of the API Lamivudine, CAS # 134678-17-4, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

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.

No Increased Risk of AML in Lenalidomide Drug Recipients

Tuesday, December 23rd, 2014

LenalidomideReassuring findings were presented at the American Society of Hematology Annual Meeting at the beginning of December 2014 regarding the use of the immunomodulatory drug Lenalidomide. Concerns for patients with myelodysplastic syndrome (MDS) being administered this potent anti-cancer drug were quelled, when a comprehensive study revealed that this lifesaving treatment did not lead to a transformation to AML in Lenalidomide patients. Results from this study were deemed to be landmark, as it was the largest retrospective cohort study to date examining the concern of AML (acute myeloid leukemia) transformation in MDS patients. Findings were disseminated by Dana E. Rollison, PhD of the H. Lee Moffitt Cancer Center, and included data from approximately 1,248 patients who received Lenalidomide at the Moffitt Cancer Center between 2004 and 2012.

Myeloblast with Auer rod smearThe aforementioned study met the great need for additional information regarding the risk of AML transformation in MDS patients, particularly the people with both the del 5q and non-del 5q forms of this cancer. As a retrospective analysis, the information gleaned offered the opportunity for researchers to gather real world data in a controlled manner. The follow up period of roughly 30 months proved that the administration of Lenalidomide was associated with a sizably reduced risk of AML transformation in patients, 2.44 per 100 person-years and 5.5 per 100 person–years in the patient group that received Lenalidomide and the group that did not, respectively. Additionally, a protective effect from Lenalidomide was found in patients with a lower risk on The International Prognostic Scoring System (IPSS), which is the most commonly used tool in myelodysplastic syndrome to predict long-term outcomes. These findings are not only reassuring to patients with MDS, but also encouraging for practitioners treating this virulent cancer.

Lenalidomide affects the immune system by helping to slow tumor growth, as well as effectively treating cancer which results from progressive blood disease, or multiple myeloma. Patients with myelodysplastic syndrome, which is caused by an abnormal chromosome (deletion 5q MDS), receive effectual treatment from the use of Lenalidomide, as do patients with mantle cell lymphoma, a rare cancer affecting the lymph nodes. Common adverse effects include itching, diarrhea and exhaustion. Lenalidomide is currently available only via a certified pharmacy under a special program, which can be accessed from certain practitioners. LGM Pharma can assist clients as a supplier/distributor of the API Lenalidomide CAS# 191732-72-6, for research and development purposes. Clients can be assured of quality API products and continuous support throughout the R&D process.

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.