Archive for the ‘Therapeutic Classification’ Category

Ropinirole Therapy Helps Patients with RLS

Monday, July 27th, 2015
dopamine agonist

Illustration by Carol Donner

Known as Restless Legs Syndrome, or RLS, this disruptive condition occurs in roughly 7% of the population worldwide. While patients older than age 65 are most commonly diagnosed, there are children who experience RLS as well. With approximately 10% of children experiencing a sleep disorder globally, the diagnosis of RLS in the adolescent population is gaining in numbers. Restless Legs Syndrome rears its ugly head mainly at night, affecting patients when they should be sleeping. Unfortunately this debilitating disorder causes sensations during the night that elicit an uncomfortable and irresistible urge for patients to move their legs. Inactive times, such as during a movie or a long car ride can also bring upon these relentless sensations, which can often be relieved only by walking or running around to stretch and exercise the legs. RLS not only disturbs sleep, it also becomes an embarrassing burden for patients to bear.

Ropinirole, also known as Requip, which is marketed by GlaxoSmithKline, is an effectual and safe treatment for patients experiencing RLS. Ropinirole offers the same effects as the chemical dopamine, which is also associated with patients who have low levels of dopamine due to Parkinson’s disease. However, while Ropinirole is used to treat patients with Parkinson’s disease, there is no evidence that shows patients with RLS are prone to developing Parkinson’s disease at a later date. In fact, genetic researchers at Emory University discovered in 2007 a gene variant which doubled a patient’s risk of developing RLS. Additionally, patients with family members who suffer from Restless Legs Syndrome may be more likely to develop RLS, as it has been documented in many studies to run in families.

RopiniroleRopinirole is a non-ergoline dopamine agonist approved by the FDA to treat both moderate-to-severe Restless Legs Syndrome and Parkinson’s disease. The transdermal drug delivery of Ropinirole, as well as its safety and tolerability profile makes this agent an efficacious choice for patients with RLS. Adverse effects from Ropinirole are uncommon, with patient complaints being minor. Commonly reported side effects include nausea, diarrhea, gas, dizziness and headache.

LGM Pharma can assist clients as a supplier/distributor of the API Ropinirole CAS# 91374-21-9 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.

CF Therapy Combination Lumacaftor and Ivacaftor Approved

Friday, July 24th, 2015

Cystic Fibrosis Therapy Combination Lumacaftor and Ivacaftor ApprovedOn July 2, 2015 the FDA announced its approval for the potent duo of Lumacaftor and Ivacaftor to treat patients suffering from Cystic Fibrosis (CF). Coined Orkambi, which is marketed by Vertex Pharmaceuticals, this effectual treatment is specifically approved for patients ages 12 and older who have the homozygous F508 mutation of the CF transmembrane conductance regulator, or CFTR gene. Orkambi has also already attained breakthrough therapy and Orphan Drug status in the United States and it is currently awaiting an EMA review. While both Lumacaftor and Ivacaftor have not proven to be efficacious for patients with CF as monotherapy, a Phase 2 study of the combination proved these two drugs greatly improve clinical outcomes in patients who are homozygous for the Phe508del CFTR mutation.

Two successful Phase 3 studies led the FDA to their positive opinion of Lumacaftor and Ivacaftor. Coined TRAFFIC and TRANSPORT these trials were comprehensive and multinational. As double-blind, placebo-controlled, randomized and parallel-group studies, both Lumacaftor and Ivacaftor proved to be effectual, tolerable and safe. The studies were designed to evaluate primarily the efficacy of Lumacaftor and Ivacaftor in combination for patients with the homozygous Phe508del CFTR mutation form of CF. Safety was a secondary objective of the study. The patients in these studies were assigned to one of three random groups and given one of the following doses:

  • 600 milligrams of Lumacaftor once a day in combination with 250 milligrams of Ivacaftor every 12 hours for 24 weeks.
  • 400 milligrams of Lumacaftor every 12 hours in combination with 250 milligrams of Ivacaftor every 12 hours for 24 weeks.
  • A Lumacaftor-matched placebo every 12 hours in combination with an Ivacaftor-matched placebo every 12 hours for 24 weeks.

There were a total of 1,122 patients who underwent randomization, specifically 559 in the TRAFFIC study and 563 in the TRANSPORT study. At least one dose of the study drug or the placebo drug was dispensed to 1,108 patients. Both studies of the Lumacaftor/Ivacaftor combination elicited viable clinical changes as early as 15 days into the studies, and showed a sustained efficacy through the 24 week mark. In both studies the percentage of patients who had a relative improvement in the percentage of predicted FEV1 of 5% or higher was demonstrative in the patients who received Lumacaftor and Ivacaftor, as compared to the patients who received the placebo. Additionally, clinically significant reductions of protocol-defined pulmonary exacerbations were found in the patients who were dosed in both Lumacaftor–Ivacaftor trial groups. The reporting of adverse events was similar in both the Lumacaftor/Ivacaftor and placebo groups, with common complaints being a higher than normal creatine kinase level, rash and bronchospasms.

Cystic Fibrosis ManifestationsAs a genetic disease associated with high rates of early-onset mortality Cystic Fibrosis affects roughly 30,000 patients in the United States. Of these patients almost 30 percent are homozygous for the F508 mutation. The recent approval of Lumacaftor and Ivacaftor as Orkambi is an encouraging development which is greatly needed for this patient population.

LGM Pharma can assist clients as a supplier/distributor of the Lumacaftor CAS# 936727-05-8 API and the Ivacaftor CAS# 873054-44-5 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.

Linaclotide A Success for CIC and IBS-C Therapy

Tuesday, July 21st, 2015

linaclotide-intestines

Fourth quarter results from Ironwood Pharmaceuticals, marketers of Linzess, or Linaclotide, were glowing. Net sales in the United States of Linzess were estimated at $93.8 million for the fourth quarter of 2014, which was a sizable 18 percent quarter over quarter increase. This exciting news was shared in mid-February 2015, with financial gains for Linaclotide proving to be more profitable than planned. Over 440,000 prescriptions were filled in the fourth quarter of 2014 for Linzess (Linaclotide) which was an increase of 12 percent quarter over quarter. A staggering 2 million prescriptions for Linzess have been filled since its debut in December of 2012. These figures remain upbeat for this formidable therapy, designed for treating patients with both chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C).

As the only and the first guanylate cyclase-C agonist approved by the FDA, Linaclotide has proven to be a viable treatment for acting locally in the intestine to speed gastrointestinal transit and for reducing gastrointestinal pain and discomfort.

Offered in oral capsules, the approved dosage of Linaclotide is as follows:

  • IBS-C– 290 mcg one time daily, preferably on an empty stomach. Ideal administration should be at least 30 minutes before the first meal of the day.
  • CIC– 145 mcg daily, preferably 30 minutes before the first meal of the day.

Linaclotide is contraindicated for use in children ages six and younger. The safety and efficacy has been established for patients ages 18 and older for when using Linaclotide. Serious adverse effects from Linaclotide are uncommon, with most common side effects reported being diarrhea, flatulence and abdominal discomfort.

Chronic idiopathic constipation effects almost 30 million Americans, with between 12 and 19 percent of Americans having fewer than three bowel movements a week, which are difficult to pass. Linaclotide achieved study goals in patients with CIC, and also helped reduce bloating, abdominal pain and the severity of constipation in patients. Approximately 62 percent of patients who received Linaclotide in studies expressed that they were “very likely” to continue using this therapy after the study concluded.

Linaclotide is also effectual for treating patients with irritable bowel syndrome with constipation. By increasing the secretion of chloride and water in the intestines Linaclotide not only softens stools but it also stimulates bowel movements.

LGM Pharma can assist clients as a supplier/distributor of the API Linaclotide, CAS # 851199-59-2, 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.

Sacubitril and Valsartan Combo Entresto is FDA Approved

Thursday, July 9th, 2015

Entresto LCZ696 (Valsartan/sacubitril)  FDA approved July 7, 2015Entresto, the novel combination therapy which combines Sacubitril and Valsartan, was FDA approved on July 7, 2015. Previously known as the investigational compound LCZ696, Entresto received an FDA nod to reduce the risk of both hospitalization and cardiovascular mortality in patients with chronic heart failure, especially those with a reduced ejection fraction and an NYHA Class II-IV diagnosis.

Perhaps the biggest news-maker from this FDA nod is the novel molecule Sacubitril, getting it’s first FDA approval. Sacubitril is an effectual first-in-class neprilysin inhibitor. Combined with the angiotensin receptor antagonist Valsartan, Entresto shined in comprehensive studies.

The FDA decided to quickly approve Entresto, which is marketed by Novartis, after receiving results from a vast study coined PARADIGM-HF. This study has proven to be the largest clinical trial ever conducted in patients with heart failure to date. The FDA’s decision is based on results from the 8,442-patient who were enrolled in this trial, which proved Entresto was both clinically and statistically superior to Enalapril, a standard ACE inhibitor used for heart failure therapy. Entresto drove the risk of cardiac mortality and hospitalization from heart failure down by 20 percent in the trial, meeting the primary study endpoint. Adverse effects from Entresto were not deemed severe, and included dizziness, cough, and lowered blood pressure, as well as higher than normal potassium levels, which could affect patients with preexisting kidney disease.

A staggering six million people in the United States are suffering from heart failure, with nearly half of these patients also exhibiting the reduced ejection fraction form of this disease. Patients diagnosed with chronic heart failure endure repeated hospital visits, fluid retention, breathlessness, extreme fatigue and face a high risk of mortality. The ageing population both in the U.S. and worldwide will undoubtedly lead to more cases of heart failure being diagnosed, and experts predict a hefty eight million Americans will be diagnosed with heart failure by 2030.

Entresto has been approved in three dosage strengths: 24/26 milligrams, 49/51 milligrams, and 97/103 milligrams of Sacubitril/Valsartan, respectively. The NEJM has referred to these dosages as 50 milligrams, 100 milligrams, and 200 milligrams for clinical trial literature purposes regarding the PARADIGM-HF results. The optimal dose for patients with heart failure who have a reduced ejection fraction and are classified as having a NYHA Class II-IV diagnosis is 97/103 milligrams of Entresto twice a day by mouth.

LGM Pharma can assist clients as a supplier/distributor of the API Entresto LCZ696 (Valsartan/sacubitril) CAS# 936623-90-4 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.

Diatrizoic Acid is an Effectual Contrast Media Standard

Tuesday, July 7th, 2015

Diatrizoic Acid CAS# 117-96-4Known in the United States as the brand name Gastrografin, which is marketed by Bracco Diagnostics, Diatrizoic Acid is an efficacious contrast media product. As a member of ionic iodinated contrast media drug class, Diatrizoic Acid is primarily used for investigation of the gastrointestinal tract. Diatrizoic Acid can be administered via an oral therapy or as an enema. Follow up gastrointestinal examinations are often made using barium and Diatrizoic Acid to achieve accurate diagnosis for several specific issues including:

  • Suspicion of acute hemorrhage.
  • Peptic ulcer perforation risk.
  • Post-surgery following stomach or intestine resection.
  • For the visualization of a tumor prior to an endoscopy.
  • To ascertain the development of a gastrointestinal fistula.
  • In conjunction with computerized tomography in the abdominal area.

It is uncommon that adverse effects are found in patients who receive Diatrizoic Acid, however a few exceptions have occurred in patients who complained of diarrhea, nausea and vomiting post administration. The oral formula of Diatrizoic Acid as Gastrografin is a lemon flavored solution which most patients find palatable. Typical dosages of Diatrizoic Acid range from 30 to 90 milliliters, depending on the weight and size of the patient. Children are also able to receive Diatrizoic Acid, with children around age 5 typically receiving the lowest 30 milliliter dosage. Pediatric doses are often diluted in water, milk or a carbonated beverage. The adult dose range of iodine content is 11 to 33 grams of iodine, based on a 30 to 90 milliliter dose. When used as an enema for an adult Diatrizoic Acid is usually dosed at 240 milliliters (88 grams of iodine) with 1,000 milliliters of water. An enema for children over age 5 is dosed at 90 milligrams (33 grams of iodine) and 500 milliliters of water. Children under age 5 are dosed individually according to size and need.

As a commonly mentioned contrast media, Diatrizoic Acid is an effectual agent used to help diagnose a plethora of gastrointestinal issues. The use of Diatrizoic Acid for preventing unnecessary surgery is evident, as the accurate evaluation of patient gastrointestinal issues is crucial for proper diagnosis and follow-up care.

LGM Pharma can assist clients as a supplier/distributor of the API Diatrizoic Acid, CAS# 117-96-4 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.