OREANDA-NEWS. Amgen (NASDAQ:AMGN) today announced that the Japanese Ministry of Health, Labour and Welfare has approved the cholesterol-lowering medication Repatha® (evolocumab) Injection, the first proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor to be approved in Japan. Repatha is a human monoclonal antibody that inhibits PCSK9, a protein that reduces the liver's ability to remove low-density lipoprotein cholesterol (LDL-C), or "bad" cholesterol, from the blood. Repatha was developed in Japan by Amgen Astellas BioPharma K.K. (AABP), a joint venture between Amgen and Astellas Pharma Inc., a pharmaceutical company headquartered in Tokyo.

In Japan, Repatha is indicated for the treatment of patients with familial hypercholesterolemia (FH) or hypercholesterolemia who have high risk of cardiovascular events and do not adequately respond to HMG-CoA reductase inhibitors (statins).

"Today's approval of Repatha, the first PCSK9 inhibitor approved in Japan, is an important milestone for patients and physicians who need additional treatment options to lower LDL cholesterol," said Sean E. Harper, M.D., executive vice president of Research and Development at Amgen. "High LDL cholesterol is a modifiable risk factor for cardiovascular disease and many patients are unable to appropriately control their LDL cholesterol with statin therapy alone. We are excited to bring Repatha to patients in Japan and will continue to work with regulatory authorities to make this innovative medicine available to patients worldwide."

"This approval is significant for patients and physicians in Japan and is a testament to the ongoing collaboration between Amgen and Astellas," said Eiichi Takahashi, general manager, AABP. "We are proud of the progress we are making toward our common goal of addressing the critical needs of Japanese patients with high LDL cholesterol who struggle to control their condition."

Results from Phase 3 studies showed that adding Repatha to background lipid-lowering therapy that included statins resulted in intensive reductions in LDL-C. YUKAWA-2, a pivotal Phase 3 study in Japanese patients with high cardiovascular risk and high cholesterol, demonstrated that subcutaneous Repatha 140 mg every two weeks or 420 mg every four weeks, compared to placebo, in combination with daily doses of atorvastatin, reduced LDL-C by 67 to 76 percent from baseline at week 12 and at the mean of weeks 10 and 12. The adverse events that occurred in greater than 2 percent of the Repatha group were nasopharyngitis (16.8 percent Repatha; 17.8 percent placebo), gastroenteritis (3.0 percent Repatha; 1.0 percent placebo) and pharyngitis (2.5 percent Repatha; 2.5 percent placebo). Results from TAUSSIG, a global, open-label, single-arm study in patients with homozygous FH, including patients in Japan, showed Repatha reduced LDL-C by approximately 23 percent. The adverse events that occurred in greater than 5 percent of patients were nasopharyngitis (9.0 percent) and influenza (7.0 percent).

"In Japan, LDL cholesterol levels are not adequately controlled for many patients who are at high risk of cardiovascular events and taking statins, nearly half of whom have not reached their desired LDL cholesterol goal," said Tamio Teramoto, M.D., Ph.D., director of Teikyo Academic Research Center and investigator for the Phase 2 YUKAWA-1 trial. "As the first in a new class of medicines in Japan, Repatha offers physicians an important treatment option for patients who require additional LDL cholesterol reduction."

Elevated LDL-C is an abnormality of cholesterol and/or fats in the blood. Familial hypercholesterolemia (FH) is an inherited condition caused by genetic mutations which lead to high levels of LDL-C at an early age, and it is estimated that less than 1 percent of people with FH in Japan are diagnosed. Patients can have either one of two types of FH. Heterozygous FH is the more common type of FH and in Japan, occurs in approximately one in 500 individuals. It can cause LDL-C levels twice as high as normal (e.g., >180 mg/dL). Individuals with heterozygous FH have one altered copy of a cholesterol-regulating gene. Homozygous FH is a rare, more severe form. It can cause LDL-C levels more than six times as high as normal (e.g., 500-1,000 mg/dL). Individuals with homozygous FH have two altered copies of cholesterol-regulating genes (one from each parent).

Repatha is also approved in the European Union, United States and Canada.

About Repatha® (evolocumab)
Repatha® (evolocumab) is a human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). Repatha binds to PCSK9 and inhibits circulating PCSK9 from binding to the low-density lipoprotein (LDL) receptor (LDLR), preventing PCSK9-mediated LDLR degradation and permitting LDLR to recycle back to the liver cell surface. By inhibiting the binding of PCSK9 to LDLR, Repatha increases the number of LDLRs available to clear LDL from the blood, thereby lowering LDL-C levels.

GLAGOV, the intravascular ultrasound study, is underway to determine the effect of Repatha on coronary atherosclerosis in approximately 950 patients undergoing cardiac catheterization to test the hypothesis of robust LDL-C reduction leading to a reduction or a change in the build-up of plaque in the arteries. Results from the GLAGOV study are expected in the second half of 2016.

The FOURIER outcomes trial is designed to evaluate whether treatment with Repatha in combination with statin therapy, compared to placebo plus statin therapy, reduces the risk of recurrent cardiovascular events in patients with high cholesterol and clinically evident cardiovascular disease, and completed patient enrollment in June 2015. Top-line results from the approximately 27,500-patient event-driven FOURIER study are anticipated in the second half of 2016.

About Amgen Cardiovascular
Building on more than three decades of experience in developing biotechnology medicines for patients with serious illnesses, Amgen is dedicated to addressing important scientific questions to advance care and improve the lives of patients with cardiovascular disease, the leading cause of morbidity and mortality worldwide. Amgen's research into cardiovascular disease, and potential treatment options, is part of a growing competency at Amgen that utilizes human genetics to identify and validate certain drug targets. Through its own research and development efforts, as well as partnerships, Amgen is building a robust cardiovascular portfolio consisting of several approved and investigational molecules in an effort to address a number of today's important unmet patient needs, such as high cholesterol and heart failure.

About Amgen
Amgen is committed to unlocking the potential of biology for patients suffering from serious illnesses by discovering, developing, manufacturing and delivering innovative human therapeutics. This approach begins by using tools like advanced human genetics to unravel the complexities of disease and understand the fundamentals of human biology.

Amgen focuses on areas of high unmet medical need and leverages its biologics manufacturing expertise to strive for solutions that improve health outcomes and dramatically improve people's lives. A biotechnology pioneer since 1980, Amgen has grown to be one of the world's leading independent biotechnology companies, has reached millions of patients around the world and is developing a pipeline of medicines with breakaway potential.