Archive for the ‘Immunosuppressant’ Category

FDA Approves Twice a Day Dose of Dimethyl Fumarate for MS

Monday, April 15th, 2013

FDA Approved March 2013 Dimethyl Fumarate CAS 624-49-7The recent approval of dimethyl fumarate CAS# 624-49-7, on March 27th, 2013, was an encouraging sign for the 2.5 million patients worldwide who are suffering with Multiple Sclerosis. The FDA approved Tecfidera, the brand name for dimethyl fumarate, which is developed by Biogen. As easy to dispense oral capsules, this new treatment for MS is expected to become a pharmaceutical star. Projections from analysts are more than promising, with some analysts indicating that dimethyl fumarate will be the number one medication to treat Multiple Sclerosis and gross three billion dollars in sales yearly.

The need for a novel and efficacious treatment for MS is long awaited. Dimethyl fumarate has proven to be particularly effectual for patients with relapsing forms of MS. As a chronic autoimmune disease, Multiple Sclerosis is an inflammatory condition that affects the central nervous system of the patient. The communication between the brain and body becomes awry, and symptoms such as muscle weakness and decreased balance and coordination become chronic. Multiple Sclerosis holds the title of being the most common cause of neurological disability in young adults, with women making up more of this patient population as compared to men. Patients typically undergo periods of time deemed to be relapses and recovery. The relapse period for patients involves severely decreased functioning both neurologically and physically, and as time progresses the recovery periods get shorter. Studies of Tecfidera, or dimethyl fumarate, showed a significant amount of patients experienced decreases in relapses of their MS symptoms, as compared to those patients who were dosed with the placebo. The patients who received dimethyl fumarate benefited greatly by this drug, with their average relapse rate cut by 49% after a two year period of study. The studies thus far have been for patients with elapsing-remitting MS, which is the most common form of MS that is diagnosed. This specific form is often characterized by flare-ups followed by periods of remission.  Roughly 85% of people with Multiple Sclerosis are diagnosed with this form of MS.

Patients who were administered dimethyl fumarate appreciated the simple twice a day dose schedule. Prior treatments for Multiple Sclerosis have been offered as infused or injectables only, such as Avonex, Copaxone (see article highlighting the favorable outcomes for patients taking Copaxone) and Tysabri. The adverse effects are limited, with the main concern being that dimethyl fumarate can decrease the white blood cell counts of patients, which raises their risk of infection. Patients who receive treatment with this powerhouse medication should be monitored closely by their physician as to their lymphocyte count. Side effects that are more common include diarrhea, flushing and nausea. Side effects from dimethyl fumarate have shown to decrease over time.

Annette Funicello Multiple SclerosisThe loss of beloved Mousketeer Annette Funicello to complications from Multiple Sclerosis has been in the headlines as of late. Her struggle with this virulent disease took its toll on her, and while none of her fans know her exact symptoms, her family has stated that MS affected her in a profound way.

There is currently no cure for Multiple Sclerosis on the horizon, so treatments like dimethyl fumarate are essential for this struggling patient population.

LGM Pharma provides dimethyl fumarate 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.

New FDA approval for Anakinra API for the Treatment of NOMID

Monday, February 25th, 2013

On January 8, 2012, the FDA has approved Anakinra CAS# 143090-92-0, known as the brand name Kineret, to treat both adults and children with neonatal-onset multisystem inflammatory disease, or NOMID. Five years of data demonstrated that Anakinra is effectual at controlling the daily symptoms of NOMID, which include joint pain, headache, rash and fevers. In addition to offering relief from the debilitating symptoms of NOMID studies also showed that administration of this medication helped to stabilize integral central nervous system functions for patients, particularly hearing and vision. Certain cases of NOMID cause severe symptoms, like headaches, seizures and vomiting which result from chronic meningitis. Intellectual disabilities may also occur in some people with this NOMID.

interleukin antagonistIn a class of medications called interleukin antagonists Anakinra is  efficacious at blocking the activity of interleukin, which is a protein in the body that elicits joint damage. Dosage of Anakinra is available as a subcutaneous injection, to be administered once daily at the same time. Prefilled glass syringes are offered for patients, with 7 syringes, or one for each day of the week. Most patients see significant improvement in their symptoms within four weeks’ time. Adverse effects of Ankinra are uncommon, and may include headache, nausea and stomach pain. The news from the FDA approving Ankinra for the treatment of neonatal-onset multisystem inflammatory disease has created hope from the patients suffering from this genetic disorder. The mutations in the NLRP3 gene are the cause of this disorder for patients, and symptoms like a recurring rash and joint and tissue inflammation are present from birth in the majority of patients. LGM Pharma offers API Ankinra for research and development purposes. Clients can be assured of quality 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.

FDA Approves Everolimus for Treating Advanced Breast Cancer

Friday, July 20th, 2012

Everolimus 159351-69-6Novartis gains FDA approval for Afinitor in advanced breast cancer marking a significant milestone for women battling this disease.

Everolimus CAS# 159351-69-6, is the active ingredient for Afinitor®. Click for more information on, and availability of Everolimus. Also, click for more articles on breast cancer and the HER2 receptor.

  • The approval was based on a randomized, double-blind, placebo-controlled, multi-center trial called BOLERO-2 (Breast cancer trials of OraL EveROlimus-2), which evaluated 724 postmenopausal women with advanced HR+ breast cancer with recurrence or progression following prior therapy with letrozole or anastrozole
  • Approval represents the first major advance for US patients with advanced HR+ breast cancer since aromatase inhibitors were introduced more than 15 years ago
  • In a Phase III trial, Afinitor plus exemestane more than doubled the time women lived before the cancer worsened compared to exemestane alone
  • Afinitor, the first mTOR inhibitor approved for advanced HR+ breast cancer, is given after the disease progresses following prior therapy with letrozole or anastrozole

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.

Prepare for the Future Exaction of Oncology Products

Thursday, July 5th, 2012

U.S. ShortagesThe Oncology segment of the pharmaceutical industry is not only a fast growing one, but it is also an area where shortages are anticipated. A decrease in availability of sterile injectable oncology drugs have been reported since 2007.  Furthermore, many of the sterile injectable oncology drugs that experienced shortages in 2010 and 2011 had a similar issue in both 2008 and 2009. This data, coupled with the predicted growth of oncology products through 2018, make the need for research and development of these drugs a crucial one. The publication Evaluate Pharma projected that oncology drugs would experience the most growth through the year 2018. This projection, offered in their May 2012, issue indicates a relevant need for oncology products to be produced at a rapid rate to meet the demands of the next decade. The need for both sterile injectable and oral oncology medications are sure to be in demand, and LGM Pharma is a proud provider of these API products.

lenalidomideLenalidomide, CAS# 191732-72-6, is also known as the brand name Revlimid, which is marketed by Celgene. As an oral capsule, lenalidomide is used to treat myelodysplastic syndrome, as well as in conjunction with dexamethasone to treat patients with multiple myeloma. Classified as immunomodulatory agents, lenalidomide is effectual at assisting the bone marrow to produce normal blood cells, and also killing abnormal cells in the bone marrow. Lenalidomide is usually taken once daily with water for 21 days consecutively, and then patients take a 7 day break. Side effects include loss of appetite, nausea, diarrhea, vomiting, exhaustion and weakness. Capsules are available in doses of 5,10,15 and 25 milligrams.

everolimusEverolimus, CAS# 159351-69-6, is also recognized as the brand name Afinitor, marketed by Novartis Pharmaceuticals. Approved on May 25, 2011, everolimus is FDA endorsed for progressive neuroendocrine tumors of pancreatic origin, specifically in patients with metastatic disease. Everolimus may also be used to treat patients with advanced renal cell carcinoma. Side effects include nausea, diarrhea, itching, nosebleeds, and pain in the extremities. Oral tablets are dosed in 2.5, 5, 7.5 and 10 milligrams each.

nilotinibNilotinib, CAS# 641571-10-0, is thought of as a “second-generation” tyrosine kinase inhibitor, created to follow it’s prolific successor, Imatinib Mesylate, CAS# 220127-57-1. Efficacious for the treatment of chronic myeloid leukemia, nilotinib is crucial as many patients develop a resistance to imatinib. In addition, nilotinib has been shown to have an amazing 20-fold increase in both the potency of kinase and proliferation assays when compared to imatinib. Known as the brand name Tasigna, which is marketed by Novartis, nilotinib ellicits side effects such as vomiting, dizziness, hair loss, diarrhea and rashes. Offered in both 150 and 200 milligram capsules, nilotinib is a novel choice for patients who no longer receive effective treatment from imatinib. Recognized as the brand name Gleevec, and also marketed by Novartis, imatinib is approved to treat a wide variety of cancers, including: acute lymphoblastic leukemia (refractory), chronic eosinophilic leukemia or hypereosinophilic syndrome, dermatofibrosarcoma protuberans, chronic myelogenous leukemia (Philadelphia chromosome positive), gastrointestinal stromal tumors, myelodysplastic and myeloproliferative disorders, and systemic mastocytosis. Imatinib is particularly effectual for treatment of patients with BCR-ABL, also known as the Philadelphia chromosome, KIT, and PDGFR gene rearrangements. Adverse effects are similar to those incurred by patients taking nilotinib, but may also include muscle cramps, weight gain due to fluid buildup, and edema. Imatinib is available in 100 or 400 milligram tablets, and the patent for Gleevec is set to expire in mid January of 2015.

pemetrexed disodiumPemetrexed Disodium, CAS# 150399-23-8, is known as the brand name Alimta, and is marketed by Eli Lilly. Patients suffering from advanced or metastatic nonsquamous non-small cell lung cancer (NSCLC) or malignant pleural mesothelioma (MPM) will find pemetrexed to be a life prolonging treatment. As a sterile injection given via a slow infusion into a vein, this injection typically takes 10 minutes to administer. Normally given every 21 days, side effects may include nausea, vomiting, diarrhea, low blood cell counts and mouth sores. Patients taking pemetrexed should be dosed with folic acid and vitamin B-12 to protect their stomach, blood cells, and bone marrow from the side effects of this potent drug.

bortezomibBortezomib, CAS# 179324-69-7, is another sterile injectable medication, used to treat both multiple myeloma and mantle cell lymphoma. This formidable treatment is administered as either an injection into the vein or under the skin (subcutaneously). Known by the brand name Velcade, which is marketed by Millennium Pharmaceuticals, bortezomib may cause side effects such as peripheral neuropathy, low blood pressure, pyrexia and neutropenia.

With over 20 million new cases of cancer predicted in 2025 worldwide, the World Health Organization is urging researchers to continue to develop new products to combat this future onslaught of patients. An impressive market of growth has been demonstrated in both the U.S. and worldwide. Anti-cancer drug sales exceeded 50 billion dollars worldwide in 2009 alone. According to the Oncology Market Leaders – Analyses and Outlook – 2010-2025 report, the aging of the population around the world, as well as lifestyle and medical therapies in developing nations has only strengthened the need for more oncologic research,  medications, treatments and development. LGM Pharma is a provider of all of your oncology products, and offers complete assistance to clients 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.

Sirolimus Continues to be Effective, Even When Thought to be Contraindicated

Monday, May 21st, 2012

Sirolimus 53123-88-9As an immunosuppressant drug used to prevent transplant rejection, Sirolimus, CAS number 53123-88-9, is a macrolide. Particularly useful for kidney transplant patients, sirolimus is also known as the brand name Rapamune, which is marketed by Pfizer. The first patent for Rapamune is set to expire in October 2012. An addtional patent will expire in July of 2013. Offered in either tablet or liquid form, sirolimus is typically taken once daily, either always with food or always without food. Derived from actinomycete Streptomyces hygroscopicus, sirolimus is usually used in combination with cyclosporine and corticosteroids to prevent the rejection of organ or tissue transplants. Extreme adverse events related to sirolimus are rare, but may include anemia, renal failure and pleural effusion. Side effects most reported by patients include nausea, vomiting, constipation, hypertension, insomnia, diarrhea, fever, urinary tract infections, tremors, headache and rash.

On January 6, 2012 Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy published a pilot study involving the use of sirolimus in conjunction with voriconazole.  As these drugs are typically contraindicated, researchers were interested in assessing the use and safety administering both sirolimus and  voriconazole concurrently, as many patients who receive both drugs are in need of optimal medication management. Study results were encouraging and indicated that both sirolimus and voriconazole can be safely coadministered, but consideration should be given as to which drug the patient receives first. Also to be considered by providers are the specific dosage of sirolimus, as well as information regarding CYP3A isoenzyme inhibitors. It was noted in this study that providers should be prudent and scrupulously monitor patients taking sirolimus before, during, and after the coadministration of voriconazole. Information gleaned from this study has lead toward the development of innovative protocols regarding medication management of this once thought contraindicated combination. LGM Pharma is a provider of API sirolimus, as well as voriconazole, for research and development purposes.

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.