Chemical entities SHINE in the top 10 fastest-growing drugs of 2016

Global pharmaceutical companies are increasingly focusing on the development of new biologics. In fact, in 2016, nine out of the top 15 pharmaceutical drugs by sales were of biologic origin. This makes us wonder what the future holds for manufacturers specializing in drugs that originate from chemical synthesis.

This week, PharmaCompass continued its analysis of the top pharma drugs by sales to evaluate the drugs that registered large sales growth in 2016.

Please note that these are not the top-selling drugs, but are the top 10 drugs that registered the maximum growth in global sales over 2015.

Interestingly, things didn’t appear that bad for drugs originating from chemical synthesis — while the top two drugs on the list were biologics, the remaining originated from chemical synthesis.

Here’s a list of drugs that witnessed the largest sales growth in 2016:

1. Opdivo (nivolumab) – Bristol-Myers Squibb

2016 sales: US$ 3,774 million

2015 sales: US$ 942 million

Sales growth: US$ 2,832 million

First approved in 2014, Bristol-Myers Squibb’s Opdivo and Merck’s Keytruda — also known as checkpoint inhibitors — continued to stay on track to be among the top 20 best-selling drugs in the world by 2020. They represent the hot new field of immunotherapy and are known to have given 90-year old Jimmy Carter (former President of the United States) hope in his fight against cancer.

With a sales growth of US$ 2.832 billion, Opdivo registered the highest sales growth of any single drug in 2016. However, Bristol-Myers Squibb received a nasty surprise last year when Opdivo did not demonstrate the desired slowdown in the progress of advanced lung cancer in a trial, as compared to conventional chemotherapy.

While Bristol-Myers’ stock price plunged on this news, Merck announced that not only did Keytruda succeed in a clinical trial as an initial treatment for advanced non-small cell lung cancer, but patients actually lived longer. Although Keytruda did not make it to our list of top 10 drugs by sales growth in 2016, it did register a sales increase of US$ 836 million, as its sales grew from US$ 566 million to US$ 1,402 million.

2. Humira (adalimumab) – AbbVie

2016 sales: US$ 16,078 million

2015 sales: US$ 14,012 million

Sales growth: US$ 2,066 million

Abbvie’s Humira (adalimumab) juggernaut continued as it not only remained the best-selling drug in the world, but also added another US$ 2 billion to its 2015 sales by generating record sales of US $16.078 billion in 2016.

Last year, the US Food and Drug Administration (FDA) approved Amgen’s Amjevita™ (adalimumab – atto) — a biosimilar of Humira®. Therefore, it remains to be seen if Humira will be able to sustain the momentum. Amjevita was approved for treating adults with a variety of medical conditions ranging from rheumatoid arthritis, plaque psoriasis, to ulcerative colitis.

3. Epclusa (sofosbuvir and velpatasvir) – Gilead

2016 sales: US$ 1,752 million (new launch)

Gilead’s third sofosbuvir-based regimen — Epclusa (sofosbuvir and velpatasvir) was approved by the US FDA in June 2016. It is the first and only all-oral, pan-genotypic single tablet regimen for chronic Hepatitis C virus infection. While Epclusa registered an impressive start, Gilead’s other two sofosbuvir-based treatments — Sovaldi (sofosbuvir) and Harvoni (sofosbuvir and lepidasvir) — saw their combined sales decline by almost US$ 6 billion.

4. Imbruvica (ibrutinib) — Johnson & Johnson / AbbVie

2016 sales: US$ 3,083 million

2015 sales: US$ 1,443 million

Sales growth: US$ 1,640 million

Abbvie’s 2015 US$ 21 billion buy of Pharmacyclics seems to be paying off. The Pharmacyclics buy was a way to get access to Imbruvica (ibrutinib), a cancer drug which is co-marketed with Johnson & Johnson. It generated sales of US$ 3.083 billion in 2016. Imbruvica works by blocking a specific protein called Bruton’s tyrosine kinase (BTK). In December 2011, Johnson & Johnson said it would pay Pharmacyclics as much as US$ 975 million to fund getting the drug to market in exchange for half the profits generated globally.

5. Eliquis (apixaban) – Bristol-Myers Squibb / Pfizer

2016 sales: US$ 3,342 million

2015 sales: US$ 1,860 million

Sales growth: US$ 1,483 million

Although apixaban was the third-to-market novel oral anticoagulant (NOAC), which is co-promoted by Pfizer and Bristol-Myers Squibb as Eliquis, it continues to unseat Johnson & Johnson’s Xarelto (rivaroxaban) as the leader in its class based on total prescriptions. Rivaroxaban’s total 2016 sales were US$ 5.392 billion.

While Pfizer’s reports its sales as part of Alliance revenues, and exact sales are not known, Bristol-Myers Squibb results alone put Eliquis in the top 10 list. Generics are hot on their tail as, last month, Pfizer and Bristol-Myers’ filed suits against 16 generic makers to uphold their patents for apixaban.

6. Genvoya (elvitegravir, cobicistat, emtricitabine, tenofovir alafenamide) — Gilead

2016 sales: US$ 1,484 million

2015 sales: US$ 45 million

Sales growth: US$ 1,439 million

Genvoya has been the most successful HIV treatment launch since the introduction of Atripla (the first single-tablet regimen launched a decade ago). Gilead is the dominant HIV player in the US market and has the top three most-prescribed HIV regimens in the US.

Genvoya adds Tenofovir Alafenamide (TAF) to already known treatments. TAF based drugs have demonstrated a better safety profile. They would also allow Gilead to maintain its dominance in the HIV market.

7. Ibrance (palbociclib) — Pfizer

2016 sales: US$ 2,135 million

2015 sales: US$ 723 million

Sales growth: US$ 1,412 million

Discovered in Pfizer laboratories and approved by the US FDA in February 2015, Ibrance is used in combination with Letrozole as a first-line treatment of postmenopausal women with estrogen receptor-positive, human epidermal growth factor receptor 2-negative (ER+/HER2-) metastatic breast cancer.

8. Triumeq (abacavir, dolutegravir, lamivudine) – GlaxoSmithKline

2016 sales:US$ 2,151 million

2015 sales: US$ 905 million

Sales growth: US$ 1,246 million

GlaxoSmithKline’s HIV drugs business — ViiV Healthcare — has been enjoying sales growth with the introduction of Triumeq ® in its portfolio. While GSK is the major shareholder in ViiV Healthcare, Pfizer and Shionogi also have a stake. Triumeq® is the company’s first fixed-dose combination tablet for a once-daily single pill regimen that combines dolutegravir, an integrase inhibitor, with the nucleoside reverse transcriptase inhibitors — abacavir and lamivudine.

9. Revlimid (lenalidomide) – Celgene

2016 sales: US$ 6,974 million

2015 sales: US$ 5,801 million

Sales growth: US$ 1,173 million

Celgene’s Revlimid (lenalidomide) — a thalidomide-derivative introduced in 2004 as an immunomodulatory agent for the treatment of various cancers such as multiple myeloma — brought in US$ 5.8 billion in 2015, and grew another 20 percent this year, to US $6.974 billion. Revlimid now contributes more than 60 percent to Celgene’s total sales of US$ 11.229 billion.

10. Xarelto (rivaroxaban) – Johnson & Johnson (US) and Bayer

2016 sales: US$ 5,392 million

2015 sales: US$ 4,255 million

Sales growth: US$ 1,137 million

Bayer’s Xarelto, which is promoted by Johnson & Johnson in the United States, provided patients with an alternative to the old-guard therapy — warfarin. While rivaroxaban is competing with other novel oral anticoagulants (NOAC) like Eliquis (apixaban) and Pradaxa (dabigatran), rivaroxaban has the class lead in indications.

Xarelto recently posted positive results in a large-scale Phase 3 study —COMPASS, involving 27,402 patients, that assessed the effect of the blood thinner in preventing major adverse cardiac events (MACE).

The trial was stopped a year early on the advice of an independent Data Monitoring Committee, after the primary endpoint of prevention of MACE (which includes cardiovascular death, myocardial infarction and stroke) reached its pre-specified criteria for superiority over aspirin.

Our view

In QuintilesIMS Institute’s new annual drug spending report, analysts have forecasted that over the coming five years the industry should continue to receive 40 to 45 new drug approvals every year.

A quarter of all the drugs in late-stage development are now focused on oncology. The rate of oncology drug development has hit such a rapid pace that new drugs are superseding old ones in a matter of a few years.

It’s clear that this compilation will see radical changes next year. However, with eight out of the 10 fastest-selling drugs coming from chemical synthesis, traditional generic manufacturers still have a lot of opportunities to explore.


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New Raltegravir Potassium Merck Agreement Proves to be a Major Improvement Over the Status Quo

Raltegravir potassium CAS 871038-72-1

Product name and CAS#: Raltegravir potassium CAS# 871038-72-1

Raltegravir potassium is a human immunodeficiency virus integrase strand transfer inhibitor. The drug is soluble in water and slightly soluble in ethanol and methanol as well. The pharmaceutically acceptable salt has been approved for the treatment of HIV-1.

The multinational pharmaceutical, Merck has signed an agreement with MPP (Medicines Patent Pool) to license its intellectual property relating to the formulation of Raltegravir, the company’s integrase HIV drug. According to reports, the new agreement should clear the way for cheaper formulations which can be developed for some middle income countries. The license is royalty free, and because of the terms of Agreement, drug manufacturers from around the world can now develop the drug formulations of Raltegravir along with other novel combinations.

By following in the footsteps of some of the biggest names in the pharmaceutical industry, Merck has now actually made it possible for manufacturers to sell pediatric versions of their medication, but only in licensed countries and under the agreed terms. This deal between the company and MPP is the first of its kind and has made it easier for people who are living with HIV in developing countries to get easy access to a cheap medication that can very well save their lives.

According to reports, the whole idea behind the deal is to lower the price of the drug, by facilitating in the drug’s development, especially for third world countries, which now have a better chance at surviving HIV. The Agreement covers 92 countries and according to the MPP, 98.1% of children with HIV are living in those developing countries.

As suppliers/distributors, LGM Pharma is able to assist you in acquiring Raltegravir potassium CAS# 871038-72-1 in order to carry out clinical trials specifying new formulation, dosages and delivery systems. Rest assured, we will provide you with premium quality API products along with the continuous support of our team throughout the entire R&D process.

General Disease Facts

HIV or human immunodeficiency virus is a virus that is responsible for the AIDS pandemic. The virus comes in two strains, HIV-1 and HIV-2. The main reason for this is that each time the HIV is able to replicate itself, small changes occur which lead to the various forms of HIV. Out of the two, the most predominant virus is HIV-1, and it’s the one that is generally talked about when discussing HIV or AIDS. This strain can also be classified into four groups, the most common one of the group being ‘M’ or ‘Major’.

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.

Sofosbuvir and Ledipasvir Offers 6 Week Hepatitis C Cure

Sofosbuvir and Ledipasvir Hep CSofosbuvir is popular in the pharmaceutical headlines as of late, with more positive news for the patient population with Hepatitis C. An NIH (National Institute of Allergy and Infectious Diseases) study released exciting data which showed the use of Sofosbuvir and Ledipasvir elicited a cure rate in only six weeks’ time for patients with the Hepatitis C virus. This phenomenal time frame was unexpected by study investigators, but certainly welcomed by patients and practitioners. The study involved adult patients with Hepatitis C infections. Taking place at the National Institutes of Health, the aforementioned patients received a combination of three direct-acting drug therapies. This oral course of treatment was offered for approximately six and twelve weeks and the results were presented in the latest issue of The Lancet. The first trial saw 20 trial participants who received Sofosbuvir alongside both Ledipasvir and an experimental drug coined GS-9669. None of the clinical trial patients had previously undergone treatment of any kind for the Hepatitis C virus. Remarkably 19 of these patients who received these three therapies had a complete recovery at the 12 week mark. A second group of 20 patients were given a combination treatment of Sofosbuvir, Ledipasvir and a different experimental drug, coined GS-9451 for 6 weeks’ time. Again, this patient group had not been previously treated for the Hepatitis C virus. At the conclusion of the six week therapy a startling 19 of these patients exhibited zero signs of the Hepatitis C virus. Finally, a third group of 20 patients were administered Sofosbuvir and Ledipasvir only. This group also showed an astounding cure rate, with all 20 participants demonstrating no signs of the disease at the 12 week mark. The six week trial group’s success proved that a shorter time period for treatment was as efficacious in this instance as compared to a 12 week course of treatment.

HepCIn addition to patient cure rates being incredibly good, there were no reports of patients experiencing adverse effects from any of these Hepatitis C drug therapy combinations. The advent of these novel therapies, to be dispensed in shorter periods of time makes treatment for this virulent disease easier and efficacious for a wide swath of patients. The need for immediate treatment is urgent for patients suffering from the Hepatitis C virus, as roughly 85 percent of untreated or improperly treated cases end up leading to chronic Hepatitis C. The development of this chronic and long-term liver infection is devastating for patients.

LGM Pharma can assist clients as a supplier/distributor of the APIs Ledipasvir, CAS # 1256388-51-8 and Sofosbuvir, CAS # 1190307-88-0 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.

NRTI Lamivudine Looks Promising for AMD Treatment

As an efficacious treatment for the HIV virus, the NRTI Lamivudine is now showing promise as a drug to combat age-related macular degeneration, known also as AMD. Nucleoside reverse transcriptase inhibitors, or NRTIs are the most commonly used class of anti-HIV medications and they are touted to successfully act on the enzyme reverse transcriptase, prohibiting the replication of the HIV virus which causes AIDS. A milestone study, recently released from the Kentucky University’s Department of Ophthalmology and Visual Sciences investigated nucleoside reverse transcriptase inhibitors (NRTIs), a class of drugs that has been used to treat HIV/AIDS for the past 30 years, and revealed innovative research regarding the NRTI Lamivudine for the treatment of AMD. Patients suffering from age-related macular degeneration experience a collection of the toxic molecule RNA in the retina, causing this debilitating condition. The toxic RNA molecule is remarkably similar to the HIV virus, as both need the reverse transcriptase enzyme to conclude their life cycle. These landmark findings have extended the possibilities for the use of not only Lamivudine for the treatment of AMD, but also many other NRTIs like Zidovudine, CAS # 30516-87-1 and Stavudine, CAS # 3056-17-5.

Age- related macular degeneration is a serious disease that leads to progressive vision loss and is currently untreatable in 90 percent of patients. The two forms of AMD are classified as dry and wet. The most common form is dry AMD, as it accounts for most cases. Wet AMD is less common, occurring in less than 10 percent of cases, however it can become virulent quickly. Statistics show that over 11 million adults in the United States have partial or total blindness due to AMD, and this figure is expected to double by the year 2050. Worldwide cases of AMD are estimated to surpass 200 million people worldwide by 2020. The FDA has not approved any therapies to combat dry AMD to date.

Research gleaned has indicated that NRTIs, specifically Lamivudine, staves off cell death in mice. A pleasant surprise for researchers was the ability of NRTIs to block the group of proteins coined inflammasones. These overactive inflammasones contribute to AMD and are believed to purport several other diseases such as atherosclerosis, diabetes and Alzheimer’s disease. Concern regarding adverse effects among scientists using Lamivudine and other NRTIs to treat AMD is apparent, however it is a minor concern. The re-purposing of NRTIs for the treatment of dry AMD relies on the past research and development of these crucial drugs, with the majority of adverse effects originally associated with these drugs being allayed by perfecting their use. While negative side effects were of concern when NRTIs were initially administered there has been a plethora of safety information gathered by R&D over the past several decades. Reduced dosing regimens, alongside newer compounds with effectual safety profiles makes the use of NRTIs for conditions other than HIV prudent. Lamivudine, in specific, has been deemed to be a remarkably safe and effective drug, with virtually no negative side effects. Perhaps this information is why researchers are looking at Lamivudine as a possible treatment for Ebola as well. The “off-label” use and acceptability of NRTIs is becoming widely praised across the globe, leading to hope and excitement for the future of pharmaceutical research. LGM Pharma can assist clients as a supplier/distributor of the API Lamivudine, CAS # 134678-17-4, 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.

Winning the Fight Against AIDS One Drug at a Time

December 1, 2014 marked World AIDS Day, with roughly 40 million deaths worldwide over the past three decades attributed to this virulent disease. While there is no known cure for AIDS the advent of multiple drug regimens has made the treatment of the HIV virus which causes AIDS manageable for many patients globally. Unfortunately there are still countries who have limited access to the variety of AIDS drug cocktails, causing experts from UNAIDS, or The United Nations AIDS agency, to caution against declaring a victory just yet.

HIV International Stats

As of June 2014 a recorded 13.6 million people across the globe received AIDS medications, which was a positive step compared to the 5 million patients who were administered treatment in 2010 worldwide. However, a large patient population remains untreated in sub-Saharan Africa due to the lack of timely treatment and awareness. The number of people infected with HIV who can live for many years with the administration of antiretroviral drugs can dramatically improve with the implementation of worldwide education and greater treatment options. Experts believe that with the push for treatment and care, as well as education regarding medication adherence, rates of infection will continue to decline. An astounding 13.6 million people are able to keep their HIV levels ultra-low due to antiretroviral drug cocktails, which in turn not only keeps them well but also prevents them from readily infecting others. The aforementioned cocktails are mandatory for treating the 55 million people worldwide who are expected to be suffering from AIDS by the year 2030.

Antiretroviral therapy has revolutionized treatment options for patients with AIDS, offering people newer and more effectual drug cocktails that may be administered in as little as one pill a day. The U.S. National Library of Medicine National Institute of Health currently recommends an optimal drug cocktail to fight the HIV virus which includes one NNRTI (Non-Nucleoside Reverse Transcription Inhibitor), two NRTIs (Nucleoside Reverse Transcriptase Inhibitors) and a Protease Inhibitor, or PI.

Ritonavir is a commonly prescribed PI which effectively disables the protease protein, thus rendering the HIV virus unable to replicate.

Similar to fellow Protease Inhibitors, the following Non-Nucleoside Reverse Transcription Inhibitors target the HIV virus by curtailing the replication of it:

Nucleoside Reverse Transcriptase Inhibitors work by creating faulty versions of the building blocks which are integral to the replication of the HIV virus, rounding out this efficacious combination cocktail. There are many efficient drugs which are commonly used as operative NRTIs, like:

LGM Pharma can assist clients as a supplier/distributor of the aforementioned APIs 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.