8:47 PM
Nov 08, 2018
 |  BC Innovations  |  Tools & Techniques

HitGen’s DNA for small molecules

How HitGen is amplifying DNA-encoded library-based drug design

With more than 60 partnerships under its belt, HitGen Ltd. has become a major gateway for companies to access DNA-encoded library technology -- a high efficiency form of combinatorial chemistry that upstages high throughput screening.

The platform is fast becoming a staple in drug discovery organizations, having hovered on the periphery as a rarely used tool for difficult-to-drug targets.

DNA-encoded library (DEL) technology can generate and screen diverse small molecule libraries that are orders of magnitude larger than those processed by more established methods, without increasing cost or time.

HitGen CEO Jin Li told BioCentury typical high throughput screening (HTS) methods are limited to millions of compounds because of costs. “Doing billions of molecules in that same fashion would bankrupt the whole industry.”

The company has over 300 billion small molecules in its libraries and is on track to hit one trillion by 2019.

Li launched HitGen in 2012 to develop DEL technology in China, both as a partnering engine and as a drug company in its own right. HitGen raised a RMB250 million ($39.1 million) series B round in May. Before that, the company raised RMB110 million ($17.2 million) from undisclosed Chinese angel and series A investors.

Li told BioCentury HitGen accelerated its partnering activity in the last three years, during which it signed 15 of the 17 disclosed deals, including eight in the U.S., four in Europe and three in Asia. In addition, it formed one JV with undisclosed partners (see “Table: Hitting up HitGen”).

Table: Hitting up HitGen

Since its inception in 2012, HitGen Ltd. has signed over 60 deals to use its DNA-encoded library (DEL) platform to discover and develop small molecules. At least 17 of those deals (shown below) have disclosed partners, fifteen of which were signed in the last three years. HitGen’s 2015 collaboration with Cyclofluidic Ltd. is the only deal in which the target was disclosed; the companies partnered to discover allosteric inhibitors of glycogen synthase kinase 3 β (GSK3B) to treat neurodegenerative diseases. HitGen and its partners did not disclose the amounts of upfront and research payments and milestones for any of the deals. (A) Date of extension of deal to include licensing of identified compounds; original screening deal was not announced; (B) Deal expanded from screening to custom library design in July 2018; (C) In February 2017, Cancer Research UK licensed a lung cancer compound under the deal; Source: BCIQ: BioCentury Online Intelligence

Date announcedPartnerDeal typeIndications
Aug. 2018LG Chem Ltd. (KSE:051910)ScreeningUndisclosed
Aug. 2018Bill & Melinda Gates Foundation Screening; grantTuberculosis, malaria
July 2018Sanofi (Euronext:SAN; NYSE:SNY) ScreeningUndisclosed
May 2018Forma Therapeutics Inc. Custom library designUndisclosed
April 2018 (A)Simcere Pharmaceutical Group ScreeningUndisclosed
Nov. 2017Boehringer Ingelheim GmbH ScreeningUndisclosed
Sept. 2017Takeda Pharmaceutical Co. Ltd. (Tokyo:4502) ScreeningUndisclosed
Sept. 2017CoCrystal Pharma Inc. (OTCQX:COCP) / InterX Inc. Co-developmentViral infections
Aug. 2017Aduro Biotech Inc. (NASDAQ:ADRO)ScreeningCancer
Aug. 2017Leo Pharma A/S ScreeningDermatology
April 2017

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