Firm will couple technology with its siRNA delivery tools and small molecules.

Arrowhead Research is acquiring Alvos Therapeutics (formerly known as Mercator Therapeutics), which is leveraging an in vivo phage display technology to identify cancer-targeting peptides. Alvos was founded in 2010 by the developers of the technology, Renata Pasqualini, Ph.D., and Wadih Arap, M.D., Ph.D., from MD Anderson Cancer Center (MDACC).

The technology, designed to specifically bind and enter tumor cells and the vasculature supporting tumors, is thought to be the world’s largest library of human-derived targeting agents, representing thousands of unique peptide sequences, according to Arrowhead. These targeting sequences can be linked to Arrowhead’s siRNA delivery vehicles as well as to traditional small molecule drugs to preferentially shuttle them into target cells.

MDACC previously achieved clinical proof of concept in targeting metastatic prostate cancer with one of the sequences, and Alvos has multiple other anticancer development programs in the pipeline. At MDACC, Drs. Pasqualini and Arap’s work was performed in terminal cancer patients, therefore the novel receptors and targeting peptides were identified in human patients with spontaneous disease including metastases. The acquisition enables Arrowhead to further expand the library by working with Drs. Pasqualini and Arap to generate additional data with more patient screening at MDACC.

Arrowhead intends to apply the new technology for targeting its DPC and Rondel™ siRNA delivery platforms. In addition, the peptides can be linked to small molecule cancer drugs to create peptide-drug conjugates (PDCs).

“The work that Drs. Pasqualini and Arap have done is truly revolutionary in the sheer number of targeting sequences and new receptors that have been discovered, the exquisite specificity of many of the peptides, and the fact that these were generated in human patients rather than experimental animal models,” remarks Christopher Anzalone, Arrowhead’s CEO.

“Alvos has identified rapidly internalizing cell surface receptors for over 30 diseased and normal tissue types and peptides that efficiently target them,” Anzalone adds. “We do not believe that any other group in the world has generated data in humans that approaches this. Therefore it is unique, powerful, and immediately applicable to man.

“This substantially enhances our existing siRNA programs by providing us with a huge proprietary library of human-derived targeting ligands to couple with our well-established and well-tolerated DPC and Rondel delivery platforms. In addition, this acquisition allows for the creation of new PDCs against cancer and other indications, thereby expanding our business and capabilities in a cost-effective way. The unique potential of this technology offers substantial opportunities to partner with other biotech and pharmaceutical companies.”

Arrowhead plans to integrate development of the Alvos technology into its Madison, WI, facility. In exchange for all the outstanding shares of Alvos Therapeutics, Arrowhead issued an up-front payment of 315,467 shares in restricted Arrowhead common stock. Alvos stockholders are also eligible to receive additional issuances of stock valued at up to $23.5 million at the time of issuance based on the achievement of clinical and regulatory milestones. Alvos stockholders could receive additional Arrowhead stock as the first three drugs using the new technology achieve certain sales milestones.

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