Carbapenems API’s for Antibiotic Resistance

A new publication is out called “May 19, 2016 – Tackling Drug-Resistant Infections Globally: final report and recommendations” and it highlights the antibiotic-resistant infections which are being seen for the 1st time in the U.S.

The review says “superbugs” could kill 10 million people each year and cost the world $100 trillion in lost economic output by 2050.

For the first time, a 49-year-old woman in Pennsylvania was infected with an E. coli which carried a gene for resistance against the drug colistin. She was successfully treated with an antibiotic. But, the Centers for Disease Control and Prevention, says “Antibiotic resistance is exploding in numbers as well as severity and the trends are alarming”. Read Article

Pleconaril is a Possible Therapy to Combat Enterovirus D68

enterovirus D68The Enterovirus D68 has been in the headlines lately- and not for a positive reason. This rogue virus has parents and practitioners alarmed as it has progressed to severe illness in several children, leading to cases of possible paralysis. Treatment for this virulent strain of the Enterovirus is needed quickly, as some children have experienced not only serious respiratory effects but other children have endured polio like symptoms. New research published at the beginning of January 2015, by experts at Purdue’s Department of Biological Sciences, has pointed to the use of the antiviral compound Pleconaril as a potential therapy to fight this serious illness. As an effective antiviral treatment, Pleconaril not only has proven in R&D to destabilize the virus particle, but it also binds to the “pocket” and inhibits infection. While Pleconaril has not shown to be active against current strains of the Enterovirus D68, it has proven to be a formidable opponent against the original isolate. Future changes anticipated in the structure of Pleconaril through development are surmised to lead to inhibitors which would act against a wider spectrum of isolates.

pleconarilThe summer of 2014 was particularly rough for American children who were affected by the Enterovirus D68, with 1,149 cases confirmed in August. In addition to respiratory symptoms ranging from mild to severe, many children experienced neurological effects such as muscle weakness and paralysis. With no current vaccine or treatment, finding a remedy for this frightening illness is at the forefront of pharmaceutical research. Researchers at Purdue are working with the CDC to study the latest strains of Enterovirus D68 and determine the connection with cases of polio-like symptoms in California children as well. The poliovirus is considered to be an enterovirus and classified in the family of picornaviruses. The majority of enteroviruses, however, are non-polio viruses, and are most like the common cold. These typical enteroviruses cause between ten and fifteen million infections each year in the U.S.

Prior studies of Pleconaril have proven successful for treating picornavirus-associated viral respiratory infections. Phase II trials involved two randomized, multicenter studies of Pleconaril in both adolescents and adults ages 14 and older. These placebo-controlled, double-blind trials saw patients who sought medical care for picornavirus-associated viral respiratory infections at an outpatient facility within 36 hours of infection onset. The patients were diagnosed with moderate to severe respiratory illness that was deemed acute in nature. The first study of the Phase II trials had the patients receiving either Pleconaril 400 milligrams as a liquid form to take orally or a placebo. Pleconaril was dispensed 2 to 3 times a day to affected patients. In the second study patients were administered a 400 milligram Pleconaril tablet to take orally 3 times a day for seven days, or a placebo. Complete resolution of symptoms was the primary endpoint in the first study, with investigators marking the end of the patient’s six major viral symptoms which included nasal congestion, rhinorrhea, sore throat, cough, myalgia and exhaustion. The primary end point in the second study was the amount of time needed until the patient had either mild or absent symptoms for at least 48 hours. The first study demonstrated that treatment with Pleconaril three times daily reduced the time to complete resolution of symptoms by three days as compared to a placebo. The second study found that the time to illness alleviation was sizably shorter in the patient population who received Pleconaril. The safety profile of Pleconaril showed no statistically significant differences in adverse-events as compared to the placebo group. Common side effects from Pleconaril included nausea, stomach pain, diarrhea and headache. The patients who were given the tablet form of Pleconaril fared better than the patients who were administered the liquid form of this drug, as the tablet reduced the frequency of negative gastrointestinal effects.

As a novel, systemically acting molecule with antiviral activity against rhinovirus serotypes Pleconaril is a formidable opponent for the common cold virus. The potential for this potent antiviral medication to be an effectual treatment for the Enterovirus D68 illness is hopeful. LGM Pharma can assist clients as a supplier/distributor of the API Pleconaril CAS# 153168-05-9 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.

Can Testosterone Be Used As a Preventative Treatment For Type 2 Diabetes In Men?

diabetes-researchIs Testosterone a potential preventative treatment for type 2 diabetes? Researchers at the University of Adelaide in Australia are hopeful that their latest research will be the kick-start for trials of testosterone as a preventative for this encompassing from of diabetes. Results from early stages of this current study, which were discussed at the 10th International Congress of Andrology in late February 2013, are hopeful and encouraging. Coined “The Wittert Study”, after Gary Wittert who is the leader of this study, this study is banking on being the first of many to address the worldwide epidemic of type 2 diabetes by using testosterone as a preventative treatment.

TestosteroneAccording to the National Institutes of Health approximately 5 million American men do not produce enough of the hormone Testosterone CAS# 58-22-0.  This data, coupled with the rising interest from men in testosterone replacement therapies makes the use of this API a win-win for researchers and patients. Axiron is one example of these highly profitable testosterone replacement therapies. With Lilly’s patent due to expire on February 19, 2017, Axiron generated over $48 million dollars in profit in 2011, making this drug a blockbuster in America and even worldwide. In Australia prescriptions for testosterone are copious, as described by David Handelsman, a professor of medicine at the University of Sydney. Professor Handelsman stated in regard to men and testosterone replacements, “They think testosterone is the essence of manhood and it will prolong their youthful vigor forever.” Handelsman, who is currently researching male reproductive health also stated, “They’re persuaded because sex sells and anything to do with sex and reproduction is easy to market.” The mood elevating side effect of testosterone replacement is a boon for patients, as well,  as is the ease of use. Currently testosterone replacement therapies are available in injectable forms, as well as gels, patches and pills.

IDF-Diabetes-AtlasThe International Diabetes Federation has stated that the cost to treat type 2 diabetes worldwide now hovers at 471 billion dollars. In the United States alone, 90-95 percent of the cases of Diabetes are Type 2, according to the Centers for Disease Control and Prevention. This number translates into one out of every ten adults in the U.S., but predictions from the CDC are ominous. By the year 2050 the CDC estimates that nearly one out of every three adults in the United States could have Type 2 Diabetes, putting the medical and pharmaceutical industry under great demands. These dire figures have led Australia’s National Health and Medical Research Council to commit $4.6 million dollars to a study which will establish whether testosterone is a safe and efficacious treatment to be used along with diet to mitigate diabetes in older men.

LGM Pharma provides API Testosterone, for research and development purposes. Clients can be assured of continuous support throughout the R&D process, as well as quality API products.

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.

Entecavir Versus a Staggering Number of Hepatitis B Cases Worldwide

Entecavir 209216-23-9Entecavir, CAS# 209216-23-9 may also be known by it’s brand name Baraclude. With the patent for Bristol-Myers Squibb’s Baraclude expiring on February 21, 2015, entecavir is on track to becoming a profitable generic product. Used to treat patients with chronic hepatitis B, entecavir is considered an antiviral medication. With a staggering 2 billion people around the world, or one out of every three, being infected with hepatitis B, entecavir is forecast for continued use worldwide.

Entecavir is effectual as it is able to prevent certain virus cells from multiplying in the affected patient’s body, thus reducing the amount of hepatitis B virus in the blood. In addition, entecavir is effective for not only those patients who have hepatitis B, but  also those who have liver damage due to an active case of the virus. Patients being treated for HIV should not take entecavir. There is a slight possibility that patients dosed with entecavir may develop a potentially life-threatening condition called lactic acidosis. Side effects may be mild nausea, vomiting, diarrhea, headache, temporary hair loss and upset stomach.

 

World prevalence of chronic hepatitis B
World prevalence of chronic hepatitis B. Source: CDC.

 

Most efficacious when taken on an empty stomach, at least 2 hours before or 2 hours after eating, entecavir should be taken with a full glass of water. Entecavir is available in both tablets, .5 and 1 milligram, and as a liquid 0.05-milligram/milliliter dose. Patients with an active case of hepatitis B will usually receive .5 mg once daily. Entecavir may be used for treating children infected with the virus, but doses should be individualized based on the child’s weight, disease progression and overall health factors. According to the Hepatitis B Foundation, while the vast majority of adults exposed to the hepatitis B infection will recover and develop protective antibodies, 5-10% will not. Unfortunately these patients will be unable to get rid of the virus, and therefore develop chronic infections. The statistics for infants and children are extremely morose. An incomprehensible 90% of infants and almost 50% of young children infected with hepatitis B will develop chronic infections. While the vaccinations for hepatitis B are offered worldwide, cases of this debilitating disease continue to grow. Roughly 10-30 million people worldwide become infected with hepatitis B each year. In the United States up to 100,000 new people will become infected each year. Surprising to many, the hepatitis B virus is 100 times more infectious than the AIDS virus.

One particular study, a multinational and double-blind study compared 0.5 milligrams of a once daily entecavir (Barracuda)  to 100 milligrams of lamivudine once a day. This lengthy 52 week study found entecavir to be superior to lamivudine in the primary efficacy endpoint of histologic improvement. As a formidable medication for hepatitis B, entecavir is shaping up to be a worthy opponent against the rising numbers of this devastating disease around the world.

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.

The Facts About Herpes and Treatment with Famciclovir

famciclovirAs an effectual antiviral drug, Famciclovir, CAS number 104227-87-4, is a key treatment for infections caused by the herpes virus. Novartis holds the patent for Famvir, which is the brand name for famciclovir, but that is expiring on September 1, 2015. While famciclovir is not a cure for herpes, it will slow the growth and spread of the herpes virus so that the body can fight off the infection. Famvir is efficacious at treating several types of infections caused by the herpes virus, including genital herpes, cold sores, and shingles.

According to the CDC almost 1 out of every 3 people in the United States will develop shingles, also known as zoster or herpes zoster. There are an estimated 1 million cases each year in the United States. Many myths surround shingles, and how one can contract it, but the CDC reports that anyone who has recovered from chickenpox may develop shingles, including children. The risk of disease increases as people age, and about half of all cases occur among men and women 60 years of age and older. Shingles is caused by the varicella zoster virus, the same virus that causes chickenpox. Upon recovery from the chickenpox, the virus lies dormant in the body in an inactive state. Scientists have not yet pinpointed the exact reason why this occurs, but some people experience a reactivation of the virus, thus causing shingles. This is not the same form of herpes which causes genital herpes, which is a sexually transmitted disease.

Patients allergic to famciclovir or penciclovir cream (Denavir) should not take famciclovir. Treatment is most effectual when started at the first signs of shingles, such as  tingling, burning and blistering of the skin. Side effects from famciclovir include stomach pain, gas, nausea, diarrhea, exhaustion, dizziness, headache, itching and numbness.

Famciclovir may also be used to treat patients with repeat outbreaks of herpes virus cold sores or fever blisters in people with a normal immune system. People with repeat outbreaks of genital herpes, or as a prevention of anticipated outbreaks will also find relief from treatment with famciclovir. Available as a tablet to be taken orally, either with or without food, famciclovir is typically dosed at 500 milligrams three times daily for one week for those patients with shingles. Those patients suffering from a genital herpes outbreak should receive 1000 milligrams, to be taken twice for one day. However, if used for the prevention of future outbreaks of genital herpes, famciclovir should be taken twice a day, 250 milligrams each dose, for up to one year. In the treatment of cold sores famciclovir is effective as a single dose of 1500 milligrams. LGM Pharma offers the API famciclovir, as well as the TEVA API famciclovir. LGM Pharma is proud to be a Sole Distributor of Teva for their extensive API portfolio, for the US pharmacy compounding market.

 

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.