CQDM

Encycle Therapeutics working with major pharmaceutical companies to design rules for drugs meant to be swallowed

CQDM and MaRS Innovation investing in new Encycle project to determine rules for making peptide drugs orally bioavailable

CQDM announcement — Encycle Therapeutics is generating a better understanding of the chemical properties required to make small peptide-like molecules, which Encycle calls nacellins, orally bioavailable. With these rules, Encycle will target many of the proteins that are currently regarded as undruggable.

PHILADELPHIA (June 16, 2015) — FiercePharma has predicted that the pharmaceutical industry stands to lose $44 billion in drugs going off patent in 2015. The industry is searching for new therapeutics to replenish their pipelines while tackling existing and new drug receptor targets within the cell, improve patient care and lower administrative costs. In this context, drugs that can be orally swallowed, known as orally-bioavailable drugs, are in great demand.

Encycle Therapeutics Inc., a biotechnology company founded by Dr. Andrei Yudin of the University of Toronto in partnership with MaRS Innovation, is a Canadian start-up emerging as a market leader in finding orally-bioavailable molecules. Today, the company announced $840,000 in funding from CQDM and MaRS Innovation to generate a better understanding of the chemical properties required to make small peptide-like molecules, which Encycle calls nacellins, orally bioavailable.

This release was covered in Biotechnology Focus and BioSpace.

This funding, generated through MaRS Innovation’s strategic partnerships programs with Pfizer Inc. and GSK, and CQDM’s global membership program with Pfizer Inc. and Merck, brings Encycle’s total funding to approximately $4 million, including an earlier investment in 2011 from Ontario Centres of Excellence.

Dr. Diane Gosselin, president and CEO of CQDM, together with Dr. Raphael (Rafi) Hofstein, president and CEO of MaRS Innovation, made the announcement this morning at the 2015 BIO International Convention in the presence of Dr. Reza Moridi, Ontario Minister of Research and Innovation and Minister of Training, Colleges and Universities, and Dr. Gaétan Barrette, Quebec Minister of Health and Social Services.

“Encycle’s proprietary cyclized peptides are very different from other types of therapeutics and should enable us to target many of the proteins that are currently regarded as undruggable,” says Dr. Jeffrey Coull, Encycle’s president and CEO. “Our research suggests that, due to their unique properties, it’s easier for our peptides to cross cell membranes than it is for other types, allowing them to be taken orally and access proteins on the inside of a cell. Working on this project together with Pfizer and Merck through CQDM, as well as Pfizer and GSK through MaRS Innovation, we now wish to develop a more precise understanding of the relationship between their structure and composition, and the ability to be delivered orally.”

SciBX covers Encycle’s partnership with IRICoR, MaRS Innovation and Merck

“The first disclosed grant under Merck & Co. Inc.’s Canadian translational initiative will bolster the ability of macrocycle-based Encycle Therapeutics Inc. to conduct lead optimization of its integrin [a₄b₇,] inhibitors for inflammatory bowel disease,” writes Michael J. Haas in SciBX’s feature on the partnership, “Merck Encycles through Canada.” The article appears in the publication’s December 4, 2014 issue.

Read the Encycle press release that prompted this article.

The article explores the current grant partnership between Merck, Encycle Therapeutics, MaRS Innovation, the Institute for Research in Immunology and Cancer–Commercialization of Research (IRICoR), and the Université de Montréal’s Institute for Research in Immunology and Cancer (IRIC), and takes an inside look at the company’s progress to date.

Here’s an excerpt:

Encycle is a spinout from the University of Toronto founded in 2012 to solve the primary challenges of macrocycle drugs–poor cell penetration and low oral availability.

According to Parimal Nathwani, the company was selected by MaRS Innovation and IRICoR (Institute for Research in Immunology and Cancer–Commercialization of Research), two of the three agencies originally tasked with disbursement and management of the Merck fund, because it was a good match with IRIC’s competencies. The third agency, The Centre for Drug Research and Development, is not involved in this deal. IRICoR is the commercialization arm of IRIC.

“Encycle has a good chemistry platform and nice early discovery work on its integrin [a₄b₇,] inhibitor program, which is now at the point where it needs to move through lead optimization,” said Nathwani. “IRIC scientists have strong expertise in medicinal chemistry and have worked with industry on optimization, pharmacokinetics, toxicity and other preclinical studies, so they can provide Encycle with pharma-grade optimization.”

BioCentury features Encycle Therapeutics

Encycle Therapeutics, a MaRS Innovation start-up company from the University of Toronto, was featured in a BioCentury emerging company profile by Michael J. Haas.

The company is currently raising a Series A financing round and employs eight people.

Haas’ profile, “Encycle: Oral Macrocycles,” is available behind a pay wall on the BioCentury website.

Here’s a short excerpt:

Macrocycle therapies can block protein-protein interactions that are undruggable with small molecules; however, oral availability and cell penetration remain key challenges. Encycle Therapeutics Inc.’s chemistry platform generates drug-like macrocycles against validated targets to treat diseases for which oral therapies are needed.

Marketed inhibitors of protein-protein interactions include biologics and other molecules large enough to target the wide, shallow surfaces involved in those interactions, but can only bind extracellular targets. Macrocycles can have sufficient size to block protein-protein interactions yet remain small enough to penetrate cells and block intracellular interactions that biologics and small molecules cannot.

Founded on chemistry from University of Toronto for cyclizing peptides and non-peptidic molecules, Encycle’s macrocycles incorporate three features that are not all found in other companies’ compounds — the absence of sulfur, the presence of intramolecular hydrogen bonding motifs, and an upper limit on size, according to President and CEO Jeffrey Coull.

Dr. Raphael (Rafi) Hofstein joins Quebec’s CQDM Board of Directors

February 21, 2014
Susanne Staer
Industry Partners

**Dr. Raphael Hofstein** has joined the Quebec Consortium for Drug Discovery (CQDM) Board of Directors.

MaRS Innovation’s President and CEO, Dr. Raphael (Rafi) Hofstein, was appointed to the Quebec Consortium for Drug Discovery (CQDM) Board of Directors on February 18.

CQDM is a Quebec-based not-for profit that funds and supports joint projects in private and biopharmaceutical sectors.

Here’s an excerpt from CQDM’s announcement:

Dr. Hofstein, actively involved in the field of biotechnology, partnerships and technology transfer for over 30 years, greatly contributed to defining Israel as a world leader in biotechnology. In Israel, Dr. Hofstein held various positions including R & D Manager and Chief of Immunochemistry with the International Genetic Scientific Partnership, Scientific Director at Biotechnological Applications Ltd., Scientific Director and Vice-President, Business Development at Ecogen Inc., prior to becoming President of Mindsense Biosystems Ltd., and then founder, President and CEO, and chairman of the Board of Hadasit Ltd.

Dr. Hofstein was also president of BIOMED, the annual biomedical conference of Israel for many years. He was also co-founder and member of the Israeli Life Sciences Industry Organization and co-founder and executive of Israel’s Tech Transfer Network. Dr. Hofstein now serves on various boards, including Life Sciences Ontario, Clinical Trials Ontario as well as the Organizing Committee of the Public Policy Forum on venture capital and innovation. Dr. Hofstein holds a Ph.D. in the life sciences and chemistry, and completed his postdoctoral studies at the Harvard Medical School.

SciBX covers Encycle’s partnership with IRICoR, MaRS Innovation and Merck

BioCentury features Encycle Therapeutics

Dr. Raphael (Rafi) Hofstein joins Quebec’s CQDM Board of Directors

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