Focus

Anticoagulant Xarelto registered in the European Union

Leverkusen – Bayer HealthCare has achieved a significant breakthrough in product development: At the end of September, the European Commission granted marketing authorization for the innovative anticoagulant Xarelto®. The active ingredient rivaroxaban can now be orally administered for prophylaxis of venous thromboembolism (VTE) following hip or knee replacement surgery in adult patients. Studies show that the substance is more effective than the current standard therapy and has a comparable safety profile.

Successful drug discoverers: Bayer HealthCare researchers Dr. Susanne Röhrig and Dr. Alexander Straub observe crystals of a test substance under a microscope. The two scientists played key roles in the development of Xarelto®.

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Successful drug discoverers: Bayer HealthCare researchers Dr. Susanne Röhrig and Dr. Alexander Straub observe crystals of a test substance under a microscope. The two scientists played key roles in the development of Xarelto®.

“The successful Xarelto® development program offers impressive proof of Bayer’s innovative capability,” commented Bayer Management Board Chairman Werner Wenning. He described the novel anticoagulant as a major scientific breakthrough offering hope to millions of patients worldwide. The launch of Xarelto®, he said, is an important milestone for Bayer, especially as the drug has the potential to become a “blockbuster” medicine.

The Xarelto® approval in the E.U. is based on the results of an extensive trial program that included three Phase III studies with rivaroxaban involving nearly 10,000 patients who received the new active ingredient for thrombosis prophylaxis following hip or knee replacement surgery.

The studies documented the superior efficacy of rivaroxaban, both in a direct comparison and in a comparison between five-week prophylaxis with rivaroxaban and short-term, two-week prophylaxis with the current standard therapy. In all three studies, the active substance demonstrated a comparable safety profile and comparably lower rates of severe bleeding.

Hope in major surgical procedures

VTE is a serious and often life-threatening event. In the E.U., more than 1.5 million patients each year develop blood clots in the veins, and some 544,000 of them die as a result. More people die from VTE, for example, than from breast cancer, prostate cancer, HIV/AIDS and road-traffic accidents together.

People who undergo major orthopedic surgery have a high risk for developing VTE. This is because the implantation of a prosthetic knee or hip damages the major veins in the legs that transport blood back to the heart. Major orthopedic surgery can lead to a thrombus in 40 to 60 percent of patients who do not receive prophylaxis.

In the five largest member states of the E.U., more than 450,000 hip and knee operations in which artificial joints are implanted take place each year.

Promising new product: Bayer HealthCare employee Frank Schaell monitors the production of Xarelto® tablets.

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Promising new product: Bayer HealthCare employee Frank Schaell monitors the production of Xarelto® tablets.

“The medicines currently available have certain disadvantages, especially with regard to efficacy and use. This novel anticoagulant, which can be taken once daily in tablet form, does not require routine blood coagulation monitoring,” says Dr. Bengt Eriksson. The orthopedic surgeon at Sahlgrenska University Hospital/Östra in Gothenburg, Sweden – who is also one of the principal investigators in the trial program – considers the development of this drug product “a major step forward in preventing blood clots.”

Xarelto® received its first marketing authorization in mid-September in Canada, where the drug is now approved for prevention of VTE in patients following elective hip or knee replacement surgery. Marketing of the new product began immediately following its registration.

The registration documentation was submitted to the U.S. Food and Drug Administration (FDA) in July 2008. Once it is approved in the United States, Xarelto® will be marketed there by Ortho-McNeil, a division of Ortho-McNeil-Janssen Pharmaceuticals. Registration submissions for Xarelto® are currently being reviewed in a further 10 countries.

Additional indications being evaluated

Rivaroxaban is currently the most thoroughly researched active substance in its class. The intention is to include a total of some 50,000 patients worldwide in the extensive clinical study program. Xarelto® is currently being investigated in the prophylaxis and therapy of thrombosis in a broad spectrum of indications – including treatment of venous thromboembolism, stroke prophylaxis in patients with atrial fibrillation, prevention of VTE in hospitalized, medically ill patients, and secondary prevention of acute coronary syndrome.

Xarelto® was discovered in Bayer’s laboratories in Wuppertal, Germany, and is being jointly developed by Bayer HealthCare and Johnson & Johnson Pharmaceutical Research & Development, L.L.C.