Archive for the ‘Research Molecule’ Category

Loteprednol Etabonate Safe for Children and Adults with Inflammatory Eye Conditions

Thursday, April 19th, 2012

loteprednol etabonateLoteprednol Etabonate, also known as Lotemax, is an anti-inflammatory corticosteroid eye solution. As a prescription eye drop, loteprednol etabonate, CAS number 82034-46-6, is used to treat a variety of inflammatory eye conditions. These conditions typically affect the anterior chamber of the eye and include allergic conjunctivitis, superficial punctate keratitis, acne rosacea, Iritis, herpes zoster keratitis, cyclitis and certain types of infectious conjunctivitis. A typical dose for many of the aforementioned conditions is one to two drops in the affected eye(s), administered up to four times daily. Common side effects include vision disturbances, such as blurriness, dry eye, itching, swelling of the conjunctiva, excess tear production and light sensitivity. Systemic adverse effects such as headache and rhinitis have also been noted. The first patent for Lotemax expired as recently as March 2012. LGM Pharma provides API loteprednol etabonate for R&D purposes, and provides complete support to clients throughout the research and development process.

As an ester corticosteoid, loteprednol etabonate has shown a well documented safety profile through over a decade of studies. In addition to it’s efficacy in decreasing the production of inflammatory precurser proteins, loteprednol etabonate offers increased lipiphilicity, which allows a greater cell penetration. While loteprednol etabonate is structurally similar to other corticosteroid solutions, it is unique in that the number 20 position ketone group is absent in the structure, making it a highly lipid soluble treatment. In a trial studying the safety and effectiveness of loteprednol etabonate 0.5% versus prednisolone acetate 1.0% ophthalmic suspension, loteprednol was found to have a favorable profile in regard to intraocular pressure increases. This conclusion was published in the American Journal of Opthalmology, which revealed that the treatment of these patients with acute anterior uveitis saw less of an increase in intraocular pressure after receiving loteprednol etabonate. In opposition, patients who received prednisone acetate displayed a greater incidence of intraocular pressure increases.

Currently being explored for it’s use in treating seasonal allergies with allergic conjunctivitis, loteprednol etabonate is being marketed as such an eye drop by Bausch and Lomb, known as Alrex. The April 1, 2012 issue of Paediatric Drugs, published online, revealed results from a trial which measured both the tolerability and safety of loteprednol etabonate 0.5% and tobramycin 0.3%. These ophthalmic suspensions were tested in pediatric subjects, ages 0-6, in randomized and parallel group studies. Adverse events in the group of children who received loteprednol etabonate were deemed low, and the use of loteprednol was determined to be safe for children in short term dosing for conditions such as blepharoconjunctivitis.

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.

Valsartan Found Safe for Use in Adults and Children with Hypertension

Tuesday, April 17th, 2012

ValsartanValsartan, CAS number 137862-53-4, is used as a treatment for high blood pressure, as well as congestive heart failure. As part of a class of medications called angiotensin II receptor antagonists, valsartan impedes the action of natural substances in the body that cause a tightening of blood vessels, thus allowing a smoother blood flow to the heart. Also known as Diovan, manufactured by Novartis in the United States, valsartan can be essential in the health of cardiac patients, especially after a patient experiences a heart attack. LGM Pharma is an exclusive provider of the Teva API Valsartan for compounding, research and development, as well as client support throughout the R&D process.

Available as a tablet in 40, 80, 160 and 320 milligram doses, valsartan can also be found in some markets as a hard gelatin capsule, containing either 40, 80 or 160 milligrams per dose. Typical doses range from 40 to 320 milligrams daily. Typical side effects include dizziness, headache, cough, nausea, exhaustion, joint pain, blurry vision, rash and diarrhea.

The patent protection for Diovan expires in 2012, making way for generic possibilities for this leading blood pressure drug. With the increase in childhood obesity, as well as hypertension in children rising, valsartan was recently tested in children ages 6-16. The results, published in The Journal of Clinical Hypertension on March 18, 2011 indicated a favorable response from the trial. There were 261 randomized children participating, and they received  a low (10/20 mg), medium(40/80 mg), or high dose (80/160 mg) of valsartan for two weeks total. Patients were randomized to a 2-week placebo-controlled withdrawal phase at the conclusion of two weeks. Both systolic blood pressure (SSBP) and sitting diastolic blood pressure (SDBP) were found to be lowered in the valsartan versus the placebo controlled group. In addition, the safety and efficacy of valsartan was impressive, with headache being the most adverse effect noted among adolescent patients. Researchers deemed valsartan to be safe and well tolerated, which is encouraging for further studies in treating hypertension in children.

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.

Meropenem is a Powerful Antibiotic with a Wide Range of Use in the Treatment of Bacterial Infections

Tuesday, April 17th, 2012

meropenemMeropenem, CAS number 96036-03-2, is a broad spectrum antibiotic, effective for both gram negative and gram positive bacteria, including pseudonomas. An injectable antibiotic, meropenem was approved for use by the FDA in July of 1996. Developed by Sumitomo Pharmaceuticals, meropenem is marketed by AstraZeneca in the United States with the brand names Merrem and Meronem. Patients allergic to either penicillin or cephalosporin antibiotics should not take meropenem. Meropenem is administered as an injection in a large muscle or added to an intravenous fluid.

Meropenem is potent, and particularly effective in the treatment of infections of the abdomen, such as appendicitis and peritonitis, skin infections and bacterial meningitis. Typical side effects include nausea, vomiting, diarrhea or constipation, and injection site discomfort. Patients who are pregnant or nursing, or who take certain medications, specifically probenecid (Benemid), valproic acid (Depakene or Depakote), and certain vitamins must tell their doctor. If a patient experiences seizures, dizziness or extreme fatigue it is recommended they contact their provider immediately.

A recent case study report from The International Journal of Tuberculosis and Lung Disease reveals a potential treatment for drug resistant tuberculosis through the use of the combination of meropenem with clavulanate. These promising results, published February 8, 2012 ,indicate optimistic possibilities using meropenem as a treatment for a wider variety of bacterial infections then previously thought. LGM Pharma is a provider of the API meropenem for research and development, including client 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.

Tegaserod Maleate Effective and Available for Treatment of Chronic Constipation

Monday, April 16th, 2012

tegaserod maleateTegaserod Maleate, CAS number 189188-57-6, is an efficacious treatment for patients suffering from both chronic idiopathic constipation and Irritable Bowel Syndrome with constipation. Known by it’s trade name Zelnorm, which was marketed by Novartis, this drug was removed from the U.S. market in 2007, amid concerns of adverse cardiovascular side effects. Despite the recall and discontinuation of Zelzorm in the U.S. and Canada, over twenty five countries continue to market generic tegaserod maleate, sometimes under the name Zelmac.

As a 5-HT4-receptor agonist, tegaserod maleate is effective as it imitates the action of the neurotransmitter serotonin, of which a large percentage of serotonin in the body is found in the gastrointestinal tract. By aiding the muscles of the digestive tract, tegaserod maleate also helps to move food through more quickly, relieving constipation. This decrease in nerve sensitivity leads to decreased feelings of pain and bloating as well. Reported side effects of tegaserod maleate include headache, diarrhea, flatulence, fatigue, hemorrhoids, and abdominal pain.

Offered in 2 and 6 milligram tablets, tegaserod maleate has proven to be a formidable, short term treatment for women who have irritable bowel syndrome (IBS) with constipation as their main bowel problem. This same efficacy has not been proven in men studied with similar conditions. Tegaserod Maleate is also proven to be a viable treatment in patients younger than 65 years of age with chronic idiopathic constipation, lasting at least six months or longer. In 2011 the Neurogastroenterology & Motility (NMO) Journal online offered positive information that was reported in an article titled “Influence of tegaserod on proximal gastric tone and on the perception of gastric distention in functional dyspepsia.” This article, which detailed the randomized and controlled trial, involving 30 male patients with abnormalities in gastric sensorimotor function, thus leading to functional dyspepsia. The trial results indicated that a significantly enhanced meal-induced accommodation was found with patients who received tegaserod maleate. While further research is underway regarding the use of tegaserod maleate for patients with chronic constipation, strides continue to be made using this one of a kind drug. LGM Pharma provides tegaserod maleate for research and development purposes, and offers support to clients throughout the entire 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.

Lapatinib Ditosylate and the Power of Cancer Fighting Kinase Inhibitors

Thursday, April 5th, 2012

kinase-inhibitorsAs a kinase inhibitor, Lapatinib Ditosylate is efficacious when used to treat metastatic breast cancer. The ability of lapatinib ditosylate to inhibit deviating active kinases within cancer cells, and prevent cell division, makes it an effective choice for patients with advanced breast cancer. Also known as Tykerb, which is marketed by GlaxoSmithKline, lapatinib ditosylate is often given to patients in conjunction with capecitabine, for the treatment of advanced  breast cancer. Lapatinib Ditosylate, CAS number 388082-78-8, is effectual when combined with capecitabine when treating patients whose tumors overexpress HER2, and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. In combination with letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer, lapatinib ditosylate is extremely capable and effective. Lapatinib Ditosylate joins the kinase inhibitor group of drugs alongside several other powerhouse cancer opponents, such as Gefitinib, Erlotinib, Dasatinib, Nilotinib and Temsirolimus, which LGM Pharma is proud to provide to clients for research and development purposes.

lapatinib ditosylateDosing of lapatinib ditosylate for patients with metastatic breast cancer is a 1,250 milligram tablet, administered once daily for days 1-21, in combination with 2,000 milligrams twice daily of capecitabine. Patients being treated for HER2 positive metastatic breast cancer typically receive a 1500 milligram tablet once daily, alongside 2.5 milligrams of letrozole daily. Lapatinib Ditosylate was approved on January 29, 2010 by the FDA, after a clinical trial deemed EGF30008 showed a meaningful increase in progression free disease and additional survival rates for patients. Adverse effects were reported, albeit in less than 10 percent of patients. Diarrhea, fatigue, nausea and rash were the most commonly reported side effects.

On April 1, 2012 the Pharmaceutical Management Agency Clinicians’ Newsletter published exciting news regarding their decision to fund the use of lapatinib ditosylate. PHARMAC’s Exceptional Circumstances, also known as Named Patient Pharmaceutical Assessment, or NPPA, announced that lapatinib (Tykerb) will be funded as an alternative to trastuzumab (Herceptin) for first line treatment of patients metastatic breast cancer. Both drug treatments, lapatinib and trastuzumab, will also be funded for these patients with HER 2 positive metastatic breast cancer who experience early intolerance to their first choice in the study. The unique method of administration for lapatinib as an oral tablet patients can take at home is an easier and viable option compared to trastuzumab, which must be administered by IV infusion in a hospital. This announcement of funding for lapatinib ditosylate is only the beginning of what is sure to ignite future research with the array of kinase inhibitors.

 

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.