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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Paliperidone Approved as Quarterly Therapy for Patients with Schizophrenia

Paliperidone Palmitate Approved as Quarterly Therapy for Patients with SchizophreniaThe FDA gave the green light in late May 2015 with their approval of a quarterly dosing schedule of Paliperidone Palmitate, also known as Invega Trinza. Marketed by Janssen Pharmaceuticals this novel dosing regimen is the first ever quarterly dosing therapy for patients with Schizophrenia. Paliperidone is dispensed to patients via an intramuscular injection every three months, offering patients freedom from daily medications. This novel administration not only helps to insure patient’s medication adherence, but it also takes the stress of remembering daily, weekly and monthly medications away. The only prerequisite for patients seeking to take this medication is an adequate, once a month therapy with Invega Sustenna for at least four months prior to beginning Invega Trinza (Paliperidone).

A comprehensive phase III maintenance trial determined the efficacy and safety of the Paliperidone three-month formula, comparing it with a placebo in regard to delaying the time gleaned before a relapse of schizophrenic symptoms returned. This randomized study included a three-week screening phase; a lengthy seventeen-week flexible dosing phase; an open-label transition phase; a double-blind phase which was open ended and a twelve-week open-label maintenance phase. Approximately 305 patients between the ages of 19 and 70 years of age participated in this successful study. The patients were assigned at random to receive either three months of Paliperidone Palmitate or a placebo, via injection. The group of patients who were administered the Paliperidone showed a distinct advantage in terms of time until a relapse of symptoms, as compared to the patients who received the placebo. A staggering 93 percent of patients who were dosed with Paliperidone (Invega Trinza) did not experience a significant return of schizophrenia symptoms while on the three-month dosage. There were some reports of minor side effects, such as akathisia, headache and slight weight gain.

As a chronic and very severe brain disorder Schizophrenia occurs in about one percent of the U.S. population. More than 21 million people around the globe suffer from Schizophrenia. Manifestation of Schizophrenia and the first “episode” is usually around 21 years of age for males and about 27 years of age for females. Men far outnumber the patient population with a Schizophrenia diagnosis by age 30. The good news is that this potentially debilitating condition is treatable with accurate diagnosis and proper medication and care.

LGM Pharma can assist clients as a supplier/distributor of the API Paliperidone, CAS #144598-75-4 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.

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.

Positive Study Results for Aripiprazole Will Lead to NDA

Aripiprazole-129722-12-9Alkermes excitedly announced extremely positive study data from a Phase 3 trial of Aripiprazole. This randomized, placebo-controlled and double-blind study gleaned better than expected results, leading pharmaceutical executives at Alkermes to set a plan in motion for an NDA by the third quarter of 2014. As a long acting and injectable antipsychotic treatment Aripiprazole Lauroxil is now available as a once a month dosage in either 441 milligrams or 882 milligrams.

Geared for patients with Schizophrenia, Bipolar Disorder and Major Depressive Disorder Aripiprazole is also known as the brand name Abilify, which is marketed by Bristol-Myers Squibb and Otsuka. Once injected the novel antipsychotic Aripiprazole Lauroxil converts to the molecule Aripiprazole, safely alleviating symptoms of mental illness for roughly one month. The Aripiprazole injectable dose has also proven to be efficacious for sufferers of Bipolar Disorder, as it works to help patients control the highs and lows of manic episodes. Complete Phase 3 study data revealed that not only were primary efficacy endpoints met for the patients who were administered the once a month injection of Aripiprazole, but also this unique form of delivery proved to be as effectual and tolerable as the oral dosage. Side effects from the injectable Aripiprazole were similar to those of the oral form of this drug, and included complaints of mainly headache and fatigue.

Schizophrenia is a severe form of mental illness which affects roughly seven of every thousand adults worldwide, with the vast majority of patients being between the ages of 15 and 35 years of age. One percent of Americans are diagnosed with Schizophrenia and both males and females are affected equally. Schizophrenia occurs across racial boundaries and is currently becoming more commonly diagnosed in children. With WHO estimating 24 million people to have a diagnosis of Schizophrenia worldwide the need for research and development of safe and effective drugs is urgent. The World Health Organization clearly states that Schizophrenia is a treatable condition, but has recently voiced concerns that over half of all patients diagnosed with this serious mental illness do not receive appropriate pharmaceutical care.

LGM Pharma provides the API Aripiprazole CAS# 129722-12-9 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.

 

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.