Actelion Ltd announced that the renin alliance with Merck & Co., Inc., has achieved its first milestone. Actelion has completed the technology transfer to Merck and the two companies have combined their research teams and efforts in this field. The completed know-how transfer triggers a milestone payment by Merck to Actelion of USD 15 million.

In December 2003, Actelion and Merck formed an exclusive worldwide renin alliance to combine their discovery, development and marketing capabilities with the goal to efficiently provide innovative and better medicines to patients suffering from cardio-renal diseases.

Through the formation of a joint committee, the parties will collaborate on the development of products. Research and development funding will be initially shared by both parties, with Merck fully responsible to fund pivotal Phase III and outcome studies. Merck will lead and fund commercialization. Actelion retains a worldwide option to co-promote any product resulting from this alliance as a paid-for sales force.

Upon signing, Actelion has received USD 10 million. Actelion will also be eligible to receive research, development and approval milestone payments of up to USD 262 million for the successful commercialization of the first collaboration product. Actelion will also be eligible to receive certain milestone payments for the successful commercialization of additional products. Merck will pay Actelion substantial royalties on the sale of all products resulting from this renin inhibitor alliance.

Of the USD 262 million, the now due USD 15 million payment follows the completion of the technology transfer, with Merck gaining unrestricted access to Actelion's multiple renin inhibitor classes currently in the selection phase. Out of these classes, the alliance's renin research group is expected to select a first candidate for full pre-clinical development.

Renin plays a key role in the regulation of blood volume, arterial pressure, and cardiac and vascular function by serving as the first component of the renin-angiotensin system. Renin is an enzyme that catalyzes the formation of the hormone angiotensin I, which is transformed by the angiotensin converting enzyme (ACE) to angiotensin II, which acts on specific receptors to increase blood pressure and modulate long term processes such as arteriosclerosis and remodeling of heart and kidney. Therapeutic manipulation of the renin-angiotensin pathway has become very important in treating hypertension and heart failure.

Renin inhibition is a novel pharmacological approach for hypertension, renal failure, and vascular diseases. Actelion has made substantial progress in improving the oral bioavailability of potent renin inhibitors up to 70 per cent, achieving strong effects on blood pressure in animal models.