Washington Editor

BioLineRx Ltd. is padding its portfolio with the addition of a peptide for obesity.

The Jerusalem firm in-licensed exclusive worldwide rights to the orally available compound, called BL-3020, from Yissum, the technology transfer company of the Hebrew University of Jerusalem.

"Obesity is an epidemic," BioLineRx CEO Morris Laster told BioWorld Today, later adding he likes "the potential of orally available MC-4 agonists."

BL-3020 is designed to reduce food intake by binding to those receptors on the brain, which "have been known for years" to control appetite, Laster said. But small molecules synthesized to act on MC-4, he noted, have lacked potency.

In contrast, the BL-3020 agonist is "a very potent version" of the MC-4 ligand, an elusive target because it has yet to be affected orally. Chemical structure modifications enable it to cross the blood-brain barrier, despite its size as a peptide, and increase its stability and absorption in the digestive tract.

And early on, it has worked.

Preclinical experiments in mice conducted at the university, where BL-3020 was discovered by Haim Gilon and Amnon Hoffman, resulted in a decrease in food consumption. Also importantly, the mice did not show any clinical or behavioral abnormalities after its administration.

BioLineRx plans to conduct additional preclinical work throughout this year and next - in vivo feasibility studies, lead optimization and full preclinical development - with clinical trials expected to begin in 2008. The company will develop the compound through its BioLine Innovations Jerusalem subsidiary under an Israeli government grant.

That funding, awarded in November 2004, makes up about half of BioLineRx's capitalization; since its inception earlier that year, it has brought in about $43 million in venture capital and grant money.

The company was founded to in-license early stage therapeutic candidates - 13 have been brought in to date - complete preclinical feasibility testing and advance them into clinical studies if appropriate. Failures are weeded out quickly - already five programs have been terminated - and attention shifts to others in the pipeline, which is designed to include a base of 10 compounds at any given time. (See BioWorld Today, March 6, 2006.)

Though specific financial terms of the latest deal were not disclosed, Laster said its structure is a typical revenue-sharing arrangement for BioLineRx. Going forward, the company will foot the bill for BL-3020's development through proof-of-concept studies, after which it plans to out-license the product.

Obesity, of course, has gained attention as an emerging health and economic crisis for developed countries. It is estimated that 60 million people are obese in the U.S., where the problem has increased by 60 percent over the past decade.

"It's a cause of a tremendous amount of morbidity and mortality," Laster said, "vis- -vis cardiovascular disease, diabetes, metabolic disease, etc."

Global revenue from obesity drugs is forecast to reach $2.5 billion by 2012, and Laster said such products could effectively complement behavioral changes to fight that growing problem.

Prescription pharmaceuticals already in the space include Accomplia (rimonabant, Sanofi Aventis Group), which he praised for its ability to act through the central nervous system, and Xenical (orlistat, F. Hoffmann-La Roche Ltd.), which is less patient-friendly because it can cause diarrhea, with many more in development.

Elsewhere in BioLineRx's pipeline is a single clinical-stage compound, BL-1020, a neurotransmission modulator for schizophrenia that is in Phase I. The randomized, double-blind, placebo-controlled trial is expected to end later this year, with Phase II to come early next year.

In addition, a number of other products are nearing the clinic.

Preclinical studies of BL-2040, an oral small molecule for hypertension and metabolic syndrome, have demonstrated its ability to reduce weight and other symptoms of those conditions.

An exploratory microdosing Phase 0 study is expected to begin late this year or early next year. BL-1040, a biodegradable alginate polymer scaffold designed to treat acute myocardial infarction, should enter a Phase I/II trial early next year under an investigational device exemption. Lastly, the company plans to begin a Phase I/II feasibility study of a newly in-licensed product called BL-3010 for acute and chronic pain in a couple of months.

The coming clinical work might prompt BioLineRx to seek additional funding at some point next year, Laster said, though he noted that its existing money would sustain operations for the next 18 months.

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