Archive for the ‘Research Molecule’ Category
Tuesday, February 21st, 2012
Intended 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.
Phase 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.
Tags: Arena Pharmaceuticals, BLOSSOM, Eisai Inc, lorcaserin, Lorcaserin 846589-98-8, Lorqess, weight loss
Posted in Anti-Obesity Product, Research Molecule, Therapeutic Classification | No Comments »
Monday, February 20th, 2012
Risperidone, CAS number 106266-06-2, is sold under the brand name Risperdal in the United States. First developed by Janssen-Cilag, risperidone is an atypical antipsychotic that was initially released in 1994. Risperdal (risperidone) is used for patients suffering from adolescent and adult schizophrenia, schizoaffective disorder, and manic states of bipolar disorder. The FDA approved risperidone in 2003 for short term treatment of the mixed and manic states associated with bipolar disorder. Risperidone joins lithium and divalproex sodium as one of three options for treatment for children ages 10-17 with bipolar disorder. As the first the FDA approved the drug for the treatment of schizophrenia in teenaged children ages 13-17, risperidone offers a low incidence of extrapyramidal side effects when given at low doses. In 2006 the FDA approved the use of risperidone for children with autism who suffer from violent outbursts and severe aggression. Janssen’s patent on four milligram tablets of Risperdal expired at the end of December 2003, thus opening the market up to alternative generic versions of the drug. LGM Pharma supplies risperidone for R&D purposes, and offers assistance to clients through all stages of research.
Careful dosing of risperidone in patients taking the antidepressants fluoxetine and paroxetine is prudent for providers, as these drugs increase the plasma concentration of risperidone. Caution also needs to be taken when treating elderly patients. Risperidone is not approved for elderly patients suffering from dementia related psychosis. Potential adverse effects from risperidone include muscle pain and tremor, insomnia, high and low blood pressure, weight gain, photosensitivity, rash and alopecia.
A recent study published in the Archives of General Psychiatry on January 2, 2012 indicated risperidone to be more efficacious when compared to lithium or divalproex sodium for the initial treatment of childhood mania. This study, deemed “The Treatment of Early Age Mania”, or TEAM, involved 279 children, ages 6-15. These children were all clinically diagnosed with bipolar 1 disorder, as described in the DSM-IV. Children in this study received a schedule of titrated medications, with risperidone being 4-6 milligram doses. While this study shows risperidone to be the preferred treatment for initial stages of childhood mania, researchers noted potential serious metabolic side effects were possible with the use of risperidone in children. Available as an oral or an injectable, risperidone continues to be an effective drug of choice for both adolescent and adult patients diagnosed with schizophrenia or certain types of bipolar disorder.
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.
Tags: 106266-06-2, Bipolar Disorder, extrapyramidal side effects, Risperidone, Schizophrenia, TEAM, The Treatment of Early Age Mania
Posted in Compounding Product, General API, Research Molecule | No Comments »
Friday, February 17th, 2012
Treating cutaneous T-cell lymphoma (CTCL) with a powerful drug that is safe and effective is essential. Bexarotene is a formidable treatment for those patients with CTCL, especially the patients who have found other treatments unsuccessful. Classified as a Retinoid, Bexarotene works to stop the growth of cancer cells. Bexarotene, CAS number 153559-49-0, is also known as the brand name Targretin, from Easai Inc.
Bexarotene has very recently been shown to be a potential opponent in the fight against Alzheimer’s disease. As of February 13th, 2012 Stacy Pagos Haller, President and CEO of the American Health Assistance Foundation (AHAF), announced documented success in studies using bexarotene. These recent studies show a distinct benefit to bexarotene in clearing out the excess plaque found in the Alzheimer’s-disease brains of the mice studied. Not only does bexarotene do this by enhancing the body’s natural defense mechanisms, it also helps to clear amyloid beta proteins, which is a naturally occurring protein in the brain, but is unable to be cleared from the Alzheimer’s diseased brain. This study, done by researchers at Case Western University yields a promising opportunity for future research on mice, as well as human participants. Another boon from this study is that bexarotene is already approved by the FDA and has been for over a decade for cancer treatment. Researchers hope to gain funding from both Congress and The White House for continued trials, as President Obama announced earlier this week that the government will provide an additional $130 million in Alzheimer’s research funding over the next two years. LGM Pharma supplies bexarotene for R&D purposes, and offers assistance to clients through all stages of research.
Bexarotene as a treatment for CTCL is taken by the patient once daily, as a capsule, and with food. Side effects most often noted are headache and elevated blood lipid levels. Less often seen side effects include nausea, weakness, chills, abdominal pain and dermatitis.
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.
Tags: Alzheimer's, Bexarotene, Bexarotene 153559-49-0, Case Western University, CTCL, cutaneous T-cell lymphoma, Easai Inc., President Obama, Targretin
Posted in Chemotherapeutic / Anti-Neoplastic, Research Molecule, Therapeutic Classification | No Comments »
Monday, February 13th, 2012
Pixantrone maleate, CAS Number 146675-97-8, is an anthracenedione anthracycline derivative, developed by Cell Therapeutics Incorporated. Pixantrone maleate is used for treatment of patients with non-Hodgkin’s lymphoma. LGM Pharma is a provider of pixantrone maleate for research and development purposes.
As a promising treatment for aggressive non-Hodgkin’s lymphoma, pixantrone maleate is well tolerated when substituted for anthracyclines in combination regimens, and shows comparable rates of complete remission. Pixantrone is similar in structure to the anthracenedione mitoxantrone, however it lacks the 5,8-dihydroxy substitution groups, which is found in mitoxanthrone. Mitoxanthrone was shown in studies to induce the rates of patient cardiotoxicity in patients. A trial, deemed PIX301 phase III, used pixantrone maleate as a single-agent for patients with relapsed or refractory aggressive non-Hodgkin’s lymphoma. For this trial randomized patients received either pixantrone or another single agent of the investigators’ choice. Positive results were found, showing the rate of confirmed and unconfirmed remissions in patients treated with pixantrone was significantly higher than in those patients who received other agents. The overall response rate and progression-free survival in patients in the trial were also demonstrated in the PIX301 phase lll trial. Another study, phase III PIX302, treated patients with indolent non-Hodgkin’s lymphomas, and combined pixantrone and rituximab in treatment. Trials found this combination to be superior to rituximab used alone in patients with relapsed or refractory disease. Evidence in all trials also shows that pixantrone maleate is well tolerated when substituted for anthracyclines in combination regimens for aggressive non-Hodgkin’s lymphoma .
Photo courtesy of http://www.cancer.gov
The United States Food and Drug Administration is in the process of considering pixantrone for use in adult patients with relapsed or refractory aggressive non-Hodgkin’s lymphoma, as well as and indolent non-Hodgkin’s lymphoma, on a fast-track basis. LGM Pharma can work with its clients through all research stages, clinical trials, development phases, regulatory documentation submission and up till commercialization of the pixantrone maleate product. Click here to inquire about Pixantrone Maleate CAS# 146675-97-8.
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.
Tags: 146675-97-8, Anthracyclines, non-Hodgkin's Lymphoma, Pixantrone maleate, Pixantrone maleate 146675-97-8, rituximab 174722-31-7
Posted in Chemotherapeutic / Anti-Neoplastic, Research Molecule, Therapeutic Classification | No Comments »
Friday, February 10th, 2012
Carfilzomib, CAS number 868540-17-4, is a late-stage, selective next-generation proteasome inhibitor for patients with multiple myeloma. Developed by Onyx, carfilzomib has the ability to irreversibly bind to and inhibit the chymotrypsin-like activity of the 20S proteasome, which is an enzyme that degrades unwanted cellular proteins. The subsequent inhibition of the proteasome-mediated proteolysis creates a build-up of polyubiquinated proteins. This build up may cause apoptosis, cell cycle arrest and even inhibit tumor growth. LGM Pharma is a provider of the API carfilzomib for research and development.
With a fast track status given to Onyx for a rolling submission of carfilzomib by the FDA in January 2011, two Stage 3 clinical trials are underway. The first of the Stage 3 trials, known as ASPIRE, is an international and randomized trial. This trial combines carfilzomib with lenalidomide and low-dose dexamethasone, versus lenalidomide and low-dose dexamethasone alone, as a potential treatment for relapsed patients with multiple myeloma. The second of the Stage 3 trials is deemed FOCUS. This study of carfilzomib as a single agent in the relapsed and refractory setting is designed to support a regulatory filing in Europe. Additional ongoing clinical studies in patients with multiple myeloma are also underway, including a carfilzomib Phase 1b/2 study for patients with advanced solid tumors.
Previous trials include a single-arm, Phase 2 trial in patients with relapsed and refractory multiple myeloma. Carfilzomib, as a single-agent showed a positive response in this trial of 257 patients, with a 36% response rate. In another Phase 2 trial of patients with refractory multiple myeloma carfilzomib was combined with lenalidomide and dexamethasone. The durable response rate of 78% led researchers to initiate the current Stage 3 study, ASPIRE.
Clinical trials have shown carfilzomib to be effective when administered for periods of 14-23 months, with no overlapping or new incidence of toxicity. While 22% of patients in Phase 2 trials tolerated treatment well for over a year, adverse effects have been noted. Patients receiving grade 3 or higher treatment showed treatment emergent effects including thrombocytopenia, anemia, lymphoenia, neutropenia, pneumonia, fatigue and hyponatremia. However, current studies show carfilzomib to have a positive safety profile, including low rates of neuropathy.
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.
Tags: ASPIRE, Carfilzomib, Carfilzomib 868540-17-4, multiple myeloma
Posted in Chemotherapeutic / Anti-Neoplastic, Research Molecule, Therapeutic Classification | No Comments »
Monday, February 6th, 2012
Anacetrapib, CAS number 875446-37-0, is a CETP inhibitor being developed by Merck to treat hypercholesterolemia, or elevated cholesterol. Clinical trials reported by Merck have been encouraging. In late 2010 researchers from Merck reported a staggering 138% increase in good cholesterol, as well as a 40% drop in bad cholesterol among patients taking Anacetrapib. This trial involved 1,623 patients, and Anacetrapib is now poised to be one of the next generation cholesterol drugs in the market. LGM Pharma is a provider of the API Anacetrapib for research and development purposes.
The results of the 2010 study show a potential alternative treatment for patients suffering from not only coronary artery disease, but also those patients with diabetes. The proven ability of Anacetrapib to increase high-density lipoprotein (HDL) cholesterol among these high-risk patients is crucial, as these patients are at a high residual risk for a cardiovascular event to occur.
Studies of Anacetrapib done in 2007 included trials using doses of 10 milligrams, 40 milligrams, 150 milligrams and 300 milligrams. A recent study, conducted by Ronald Krauss (Children’s Hospital Oakland Research Institute, California, USA) and colleagues included once a day treatments, of either 20 milligrams or 150 milligrams for thirty patients. This study showed both doses to be effective, with the 150 milligram dose offering slightly more efficacy. The current clinical trial, coined REVEAL is underway, which encompasses 30,000 patients.
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.
Tags: 875446-37-0, Anacetrapib, Anti-Hyperlipodemic, CETP inhibitor, coronary artery disease, Diabetes, elevated cholesterol, HDL cholesterol, hypercholesterolemia, REVEAL
Posted in Anti-Hyperlipodemic, Research Molecule, Therapeutic Classification | No Comments »
Friday, February 3rd, 2012
Apixaban, CAS number 503612-47-3, is showing itself to be a viable option for patients with atrial fibrillation who are in need of an anticoagulant. In two studies, ARISTOTLE and AVERROES, which included over 24,000 patients, Apixaban (Eliquis) showed statistically significant superiority to Warfarin. A 21% lower stroke risk for patients with atrial fibrillation was an encouraging finding from the ARISTOTLE/AVERROES studies. In addition, there was a 31% lowered risk of complications from bleeding in patients studied. These combined studies offered exceptional results as to the potential use of Apixaban in stroke prevention, which is a common concern for patients with atrial fibrillation.
A joint venture by Pfizer and Bristol-Myers Squibb, Apixaban is an anticoagulant that is a direct factor Xa inhibitor, or a Vitamin K antagonist. The typical dose for patients in the studies was five milligrams, given orally, twice daily. The potential concern over medication adherence due to multiple daily doses was not a significant issue in this study, as many patients with atrial fibrillation are used to taking medication several times daily already.
Apixaban is a drug that has been in testing for several years. Earlier studies conducted, such as a 2007 trial, are now in Phase III. These studies focused on combining related competing compounds, such as rivaroxaban, in the prevention of venous thromboembolism. In this study Apixaban showed equivalency when compared to Enoxaparin as an Antithrombotic drug for patients who had undergone a knee replacement surgery. LGM Pharma supplies Apixaban for R&D purposes, and offers assistance to clients through all stages of research.
As generic Warfarin is currently widely available, Apixaban will need to continue to prove both safety and efficacy in further studies to compete in the drug marketplace. A New Drug Application (NDA) for ELIQUIS® (apixaban) was submitted and a decision is expected from the FDA by March 28, 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.
Tags: 503612-47-3, anticoagulant, apixaban, ARISTOTLE, atrial fibrillation, AVERROES, ELIQUIS, Enoxaparin, NDA, rivaroxaban, Warfarin
Posted in Antithrombotic, Research Molecule, Therapeutic Classification | No Comments »
Monday, January 9th, 2012
Bardoxolone Methyl 218600-53-4, an Antioxidant Inflammation Modulator, is currently in clinical trials as a potential once a day treatment for those patients suffering from Chronic Kidney Disease (CKD). Developed by Reata Pharmaceuticals, Inc. in partnership with Abbott Laboratories and Kyowa Hakko Kirin, this drug will treat people suffering from CKD due to conditions such as Type 2 Diabetes Mellitus. Both oxidative stress and inflammation occur as a result of CKD, and Bardoxolone Methyl acts as an agent to activate the Nrf2 pathway, thus helping to preserve and aid kidney function in affected patients.
In phase 2 of the study a new formulation of Bardoxolone Methyl was tested, and showed an improved oral bioavailability when compared to the formulation used in previous studies. All dose levels of this new formulation were well tolerated, and the pharmacodynamic profile was deemed safe and consistent. The results from this improved formulation were presented at the World Congress of Nephrology meeting in 2011.
Phase 3 (BEACON) of the current multinational, double-blind and placebo-controlled study are underway, with results expected sometime in 2013. This last phase of the study is assessing and determining the efficacy of Bardoxolone Methyl as a treatment for patients with CKD, and the progression of the disease to End Stage Renal Disease (ESRD).
The majority of patients who experienced side effects noted muscle spasms. Other side effects noted to date include hypoglycemia, nausea and peripheral edema. However, hypoglycemia was reported in approximately equal proportions of patients, in both the Bardoxolone Methyl and placebo groups.
Researchers are optimistic that Bardoxolone Methyl Treatment will prove to be a viable and successful treatment for the vast number of patients suffering from CKD.
LGM Pharma takes pride in their role as the suppliers of Bardoxolone Methyl, as well as many other anti-diabetic drugs, for the future development of groundbreaking treatments for CKD patients.
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.
Tags: 218600-53-4, Antioxidant Inflammation Modulator, Bardoxolone Methyl, Chronic Kidney Disease, End Stage Renal Disease, Nrf2 pathway
Posted in Anti-Diabetic, Research Molecule, Therapeutic Classification | No Comments »
Monday, January 9th, 2012
As of December 7, 2011 the Oncologic Drugs Advisory Committee voted to approve Axitinib CAS# 319460-85-0 (Inlyta) as a second-line treatment for patients with Advanced Renal Cell Carcinoma. This unanimous vote was based upon the findings of the phase 3 trial done in 2010, which compared Axitinib and Sorafenib. Axitinib, when compared to Sorafenib in clinical trials, was shown to significantly extend survival and disease progression.
Developed by Pfizer, Axitinib is a small molecule tyrosine kinase inhibitor. Phase 2 trials showed promise for patients with Breast Cancer, as Axitinib showed to inhibit tumor growth. Another trial, combining Axinitib with Gemcitabine initially showed improvement in patients with advanced pancreatic cancer. However, as of 2009 Pfizer announced that the results of this chemotherapy combination did not actually improve survival rates, when compared to the use of Gemcitabine alone. The trial was halted at that point.
Common side effects of Axitinib included diarrhea, hypertension, nausea and fatigue, of which all were considered manageable. Axitinib is an inhibitor for Vascular Endothelial Growth Factor receptors 1, 2 and 3, and hypertension is often considered to be a common side effect for these anti VEGF drugs. Reported dosage for trials of Axinitib were five milligrams, given twice daily.
LGM Pharma, an active pharmaceutical ingredient supplier, has built a reputation as being the “go to source” for hard to find API’s such as Axitinib, which is available on their website for R&D and drug 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.
Tags: Advanced Renal Cell Carcinoma, Axitinib, Axitinib 319460-85-0, breast cancer, Inlyta, pancreatic cancer, small molecule tyrosine kinase inhibitor, sorafenib, VEGF drugs
Posted in Chemotherapeutic / Anti-Neoplastic, Research Molecule, Therapeutic Classification | No Comments »
Monday, January 9th, 2012
Pfizer is currently conducting clinical trials for the drug Tofacitinib CAS# 540737-29-9, as a non injectable treatment for Rheumatiod Arthritis, as well as Psoriasis. Tofacitinib is also being investigated as potential treatment for inflammatory bowel disease, a preventative for organ transplant rejection, and other immunological diseases. Both five and ten milligram doses are slated to be offered, introducing an alternative treatment to current RA drugs, such as Abbott’s injectable drug Humira.
Developed to target the JKA protein, which is the protein that leads to joint destruction in RA patients, Tofacitinib has shown itself to be a viable competitor in trials thus far. Phase 3 trials that began in 2007 are planned to continue through 2015, with a phase 3 trial also underway for the treatment of Psoriasis.
Patients participating in the clinical trials were either dosed at five or ten milligrams, taken twice daily. Initial, as well as long term results have shown the drug to be safe and free of adverse side effects. There were four documented deaths at the beginning of the clinical trials, but Pfizer determined only one death was actually due to Tofacitinib.
On December 20, 2011 Pfizer announced that the U.S. Food and Drug Administration (FDA) had accepted for review the New Drug Application (NDA) for Tofacitinib . Described as a new, investigational oral JAK inhibitor, Tofacitinib is for the treatment of adult patients with moderate to severely active Rheumatoid Arthritis.
This immunosuppressant drug is supplied by LGM Pharma for R&D purposes and is available for prompt shipment.
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.
Tags: 540737-29-9, Humira, inflammatory bowel disease, JAK inhibitor, JKA protein, NDA, Phase 3 trials, Psoriasis, Rheumatiod Arthritis, Tofacitinib, Tofacitinib 540737-29-9
Posted in Chemotherapeutic / Anti-Neoplastic, Immunosuppressant, Research Molecule, Therapeutic Classification | No Comments »
Phase 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.
