Brexpiprazole: A molecule that should be on your radar

Brexpiprazole CAS# 913611-97-9Brexpiprazole is a drug used to either treat Schizophrenia or to prevent its relapse. It is also approved for use as an adjuvant in the treatment of Major Depressive Disorder (MDD), as an add-on when first line antidepressants fail to provide sufficient clinical results. Brexpiprazole has been launched under the brand name Rexulti.

Brexpiprazole was considered a major newcomer in 2015, with the potential to become the next blockbuster in mental health disorders. Drugs used in mental health have always maintained their position in top ten selling groups of drugs globally, and will continue to do so as per the IMS Institute for Healthcare Informatics report titled “Global Outlook for Medicines Through 2018”.

Brexpiprazole is classified as an atypical antipsychotic and adjunctive antidepressant, having a dopamine and serotonin receptor partial agonism. It is very similar in action to Aripiprazole (better known as Abilify), which has long maintained its position as one of the top 10 selling drugs in the US, and as one of the best-selling drugs for mental health globally. Brexpiprazole offers the benefit of improved pharmacokinetics and safety profile (lesser extrapyramidal side effects like restlessness and agitation). This is especially important, as both Schizophrenia and MDD are chronic diseases.
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Aripiprazole Lauroxil NDA Submitted to Treat Schizophrenia

The Brain in SchizophreniaThe USFDA has received the Aripiprazole Lauroxil NDA, submitted by Ireland-based Alkermes for treating patients with schizophrenia. Alkermes shares gained almost 2.3% on the news.

Aripiprazole lauroxil is a partial dopamine agonist of the second generation class of antipsychotics, with one-month and two-month formulations, developed for the treatment of the mental disorder schizophrenia, which is a chronic, severe and disabling brain disorder.

Alkermes has submitted the NDA based on results from the successful randomized, multicenter, double-blind, placebo-controlled, phase III trial which assessed the efficacy and safety of aripiprazole lauroxil, where the drug demonstrated significant improvements in schizophrenia symptoms when compared to a placebo.

“We have designed aripiprazole lauroxil to be a differentiated treatment option for schizophrenia, with a ready-to-use format with multiple dosing options.”

Alkermes CEO Richard Pops said: “We have designed aripiprazole lauroxil to be a differentiated treatment option for schizophrenia, with a ready-to-use format with multiple dosing options, to help meet the individual needs of patients and their healthcare providers.

“These attributes, together with the robust clinical data observed in the pivotal study, position aripiprazole lauroxil to be a meaningful new entrant in the growing long-acting injectable antipsychotic market, and we look forward to working with the FDA to bring this important new medication to patients and physicians as quickly as possible.”

The completion of the Phase III study, in which both doses of aripiprazole lauroxil tested, 441mg and 882mg administered once monthly, reached the primary endpoint with statistically significant and clinically meaningful reductions in Positive and Negative Syndrome Scale (PANSS) scores, met all secondary endpoints and demonstrated significant improvements in schizophrenia symptoms versus placebo.

Aripiprazole lauroxil was generally well tolerated in the study, and the observed safety profile of aripiprazole lauroxil was similar to that reported with oral aripiprazole. The most common adverse events in the study were insomnia, akathisia and headache.

LGM Pharma is supplier/distributor of the API Aripiprazole CAS 129722-12-9 for research and development purposes, as well as the Aripiprazole (TEVA API) for compounding purposes within the U.S.. 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.

FDA Approves Aripiprazole As A Once A Month Treatment for Schizophrenia

AripiprazoleAs a blockbuster medication used to treat schizophrenia, Aripiprazole CAS# 129722-12-9 has recently been approved by the FDA as a once a month treatment. Marketed by Otsuka and Bristol-Myers Squibb, this monthly dosage of aripiprazole will be sold under the name Abilify Maintena. Aripiprazole is a solid and reliable long-acting antipsychotic medication, and this FDA approval is momentous to the 1.1 percent of the U.S. population suffering from this devastating mental illness.

Patients with schizophrenia will benefit greatly from this easy to administer once a month dose of aripiprazole. However, other conditions are also successfully treated with aripiprazole. Known as the brand name Abilify, aripiprazole is an antipsychotic medication that is used to treat bipolar disorder, which is also known as manic depression, major depressive disorder in adults alongside antidepressant medications, and as a treatment option for autistic children who are ages 6 and older for symptoms of aggression, irritability, mood swings, and self-injury related to their autistic disorder.  Aripiprazole works by changing the actions of chemicals in the brain. Treatment with aripiprazole should not to be used for patients with psychotic conditions related to dementia, as it may cause these this patient population extreme harm, such as heart failure, pneumonia, or even sudden death.  Less serious adverse effects of aripiprazole may include anxiety constipation, dizziness, drowsiness, headache, upset stomach, weakness and weight gain.

The approval of the once a month treatment for schizophrenia by the FDA on February 28, 2013 is novel as this is the first dopamine D2 partial agonist approved as a once a month injection.  The advent of this unprecedented treatment addresses the ongoing need for relapse prevention in patients with this life altering mental illness. Aripiprazole, or Abilify Maintena, proved to be extremely effectual in a 52-week study. The aforementioned study was placebo-controlled, double-blind, and randomized-withdrawal. As a Phase 3 maintenance trial, Abilify Maintena {aripiprazole} evaluated the time to relapse as the primary endpoint.  269 adult patients who received the once a month dosage had significantly delayed time to relapse as compared to 134 adult patients who received a placebo. In addition, a key secondary endpoint was met, in terms of the percentage of patients who experienced a relapse or exacerbation of psychotic symptoms. Patients who were administered Abilify Maintena had a sharply lower relapse rate of 10 percent as compared to the placebo group who had a 40 percent relapse rate.  With an estimated 24 million people diagnosed with schizophrenia worldwide, fresh treatment options like aripiprazole as a monthly maintenance injection is welcomed by both patients and practitioners.

LGM Pharma offers API Aripiprazole, CAS number 129722-12-9, as well as the TEVA API Aripiprazole 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.


Lurasidone Combats Schizophrenia Symptoms

lurasidoneLurasidone CAS# 367514-87-2, is an atypical antipsychotic medication. Also known as the brand name Latuda, lurasidone is an effectual treatment for the symptoms of schizophrenia. As a second generation antipsychotic, or SGA, lurasidone is available in 20, 40, 80 and 120 milligram tablets. Latuda was approved by the FDA in October of 2010 for the specific treatment of schizophrenia in adults. While lurasidone is not a cure for schizophrenia, it is a viable solution for symptom relief for the patients suffering from this devastating mental illness.

Several weeks may go by before the patient begins to feel the effects of lurasidone, so it is important that patients be aware that instant symptom relief is atypical. The tablet is typically taken once daily by mouth, with a meal of at least 350 calories. Six week treatment intervals are recommended as these have been studied and documented as safe and tolerable dosage periods. You should plan to reevaluate patients after each six week period to determine the efficacy of this medication. Common adverse effects were minimal, and included somnolence, akathisia, nausea and Parkinsonism. Five short-term studies were completed prior to its FDA approval and the results demonstrated success in each one. These 6-week studies included placebo controlled as well as active-control arms of olanzapine or quetiapine extended-release. Phase III clinical trials encompassed 3,000 adult participants, and a successful outcome was determined based on the measurement of degrees of positive and negative symptoms and indicators of overall patient function at the six week mark.

According to the National Institute of Mental Health approximately 2.4 million Americans are affected by schizophrenia. In most cases, schizophrenia will initially appear in men during their late teens or early 20s and in women during their 20s or early 30s. Continued research and development is needed to treat this often enigmatic illness.

LGM Pharma provides lurasidone for research and development purposes, and offers clients complete 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.



Schizophrenia Patients Have an Option with Iloperidone

SchizophreniaIloperidone, CAS# 133454-47-4 is an antipsychotic medication. Known as the brand name Fanapt, the patent for this efficacious medication expires for Novartis on November 15, 2016. Iloperidone is available as tablets in dosages of 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg and 12 mg, and is intended primarily for the treatment of schizophrenia. With more than 3.2 million Americans today suffering from Schizophrenia, this is an essential treatment. Iloperidone is typically given as an increasing dosage over the course of 7 days in a special starter pack. The starting low dose is important as it helps the patient avoid potential adverse effects like light-headedness or fainting.

On August 9, 2012 Vanda Pharmaceuticals, a biopharmaceutical company focused on the development and commercialization of products for the treatment of central nervous system disorders, announced that the Israeli Ministry of Health (MoH) granted market approval for Fanapt, or Iloperidone,  for the treatment of schizophrenia.  This exciting news comes on the heels of a recently released study investigating  why certain drugs have mixed success in treating schizophrenia, and tend to lose their effectiveness. This study, reported in the journal Nature Neuroscience, focused on scientific research which investigated the external genetic reasons, or epigenetic factors, that cause treatment-resistance to atypical antipsychotic drugs. Recent statistics gleaned from researchers at Mount Sinai School of Medicine revealed that 30% of patients with schizophrenia do not respond to currently available treatments. This was due to an enzyme called HDAC2, which was highly expressed in the brains of mice chronically treated with antipsychotic drugs, resulting in lower expression of the receptor called mGlu2. It is believed that the enzyme in the brains of schizophrenic patients begins to compensate for the prolonged chemical changes over time that are caused by antipsychotics, which results in a decrease in their efficacy. However, antipsychotic medications are currently the only viable treatment for this devastating mental illness. This information only solidifies the need for new and unique treatments for schizophrenia. Worldwide about 1% of the population is diagnosed with schizophrenia, and about 1.5 million people will be diagnosed with schizophrenia this year around the globe. New instances of this illness are most likely to occur in early adulthood, with a peak in patients between the ages of 16 and 25 years of age.

LGM Pharma provides API Iloperidone for research and development purposes, and offers continual support 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.