HEPtune, which conjugates the polymer heparosan to a drug to prolong its half-life, will be licensed to Novo Nordisk exclusively for insulin products, and non-exclusively for delivery of other therapies including human growth hormones and treatments for obesity and inflammatory diseases.
Breca Tracy, VP and MD, Caisson, told In-Pharmatechnologist.com the platform is “a drug delivery vehicle for drugs needing half-life extension. The heparosan aids the drug to circulate in the blood stream.”
The technology already has an exclusive license for four undisclosed medicines, she said, adding it is working with partners other than Novo on “many different indication areas.”
Caisson said it will apply the platform to existing drugs, new medicines, and “also other formulations that may no longer be possible,” specifically for “patient populations that no longer can take drugs with competitor polymers such as PEG (polyethylene glycol) due to the occurrence of PEG antibodies.”
While conjugation of PEG to proteins has generated compounds now used in medicines, some patients are intolerant and produce PEG antibodies. These antibodies are present in 22-25% of healthy blood donations, according to a 2011 paper by scientists at INSERM.
They “may limit therapeutic efficacy and/or reduce tolerance of PEGylated proteins in some patients,” especially those with acute lymphoblastic leukaemia or chronic gout, said the researchers.
Caisson told us HEPtune “should be able to help capture this percentage of the market that has developed antibodies to the PEG polymer and delivery system. Since the heparosan is a naturally occurring polymer in the body and gets degraded (from what results have been shown to date), it is not expected that the body will generate antibodies to the heparosan.”
Immune acceptance
Heparosan is not recognised as a foreign substance when injected because it is naturally produced in the body during synthesis of heparan sulfate, an essential sugar molecule in mammals.
Caisson’s VP said as well as there being no evidence that patients produce antibodies against heparosan, “the polymer also does not seem to accumulate in the body, as to date it has been shown to be degraded by the body once it becomes internalized by cells. Studies to date also show the heparosan polymer being degraded once it reaches the lysosome and then being excreted in the urine.”
She added that heparosan has a stable shelf life before administration to patients, giving it “a very important advantage” over competing technologies which extend drug half-life inside the body.
Tailored polymers
Caisson produces the compounds with a proprietary method that creates “very distinct mono disperse polymers,” meaning they are all the same size. Competitors’ polymers, said Tracy, may have a range of molecular weights, meaning several different sizes are conjugated to the drug potential. This could alter the consistency of drug dosing.
The ability to create polymers at specific molecular weights allows tailoring according to the pharmacokinetics required, she said.
According to the agreement, Caisson will be eligible to receive milestone payments up to $167m from Novo Nordisk, plus royalties. Caisson’s CEO Glenn Nedwinn joined the company in 2012 with a remit to find partners for HEPtune.
Bioavailability Challenge 2014
Drug bioavailability is a hot topic for the drug industry, with both small molecule-focused pharmaceutical firms and biopharmaceutical developers increasingly interested in technologies that can help them make promising therapeutic candidates into sellable products.
On March 27 we are holding the second edition of our “Bioavailability Challenge 2014” a free to ‘attend’ online webinar series on March 20 focused on the difficulties developers face in ensuring their drug candidates are bioavailable.
Our editorial programme will feature contributions from Yorkshire Biotec and analysts group Frost & Sullivan will share its overview of the bioavailability services market.
The event will also feature presentations from scientists from Agere Pharmaceutical, Ashland, BASF, Dow and many more…
Click here to sign up for the show. See you on March 27.