As Invokana® Begins To Take Over From Januvia®, Merck Turns To “Next Gen” Diabetes R&D — In Collaboration With Abide

The truth is that this Abide Therapeutics approach, while extremely promising, is likely close to a decade away from an approvable, patient specific drug product. So, this may actually be “next, next” generation — in the land of diabetes disease management approaches.

Even so, it is fascinating (and truly a breakthrough technological acheivement) that the serine hydrolases are modeled “in situ” — while still in the patient’s body — and, presumably, a small molecule target is selected, on a specific receptor region — for blocking the serine hydrolases expression (click graphic at right to enlarge — see Abide’s website for more). That could indeed yield a very very effective diabetes medication.

As an aside, with my provocative headline, I don’t mean to entirely write Januvia® off — and consign it to the dust-bin of history, just yet. But it is clear that with Invokana® approved, and J&J’s evident willingness to engage in aggressive price competition — Januvia isn’t likely to see 30 percent quarter over quarter growth again, any time soon (or ever). Especially so, since Invokana soundly beat Januvia in a head to head efficacy trial. So, Merck has begun to look to the next market opportunity, for diabetes — including the Pfizer deal — and this one, in serial order.

I still think the joint Pfizer-Merck deal is likely to yield a product that will be largely leap-frogged — by competing candidates, each of which are perhaps almost two years closer to approvability than the ones offered by Pfizer/Merck. We shall see.

Beyond that horizon, though, this Abide approach, if development goes well, could truly be revolutionary — in about a decade. Here’s a bit, from Xconomy | BioTech — but do go read it all:

. . . .Serine hydrolases play a key role in a host of physiological processes that include nervous system signaling (and chronic pain), blood clotting, digestion, metabolism, inflammation, autoimmune disorders, and the life cycles of pathogens. There are scores of these enzymes, and many regulatory functions have been validated. But Abide says the therapeutic potential of modulating or inhibiting the activity of serine hydrolases remains largely undeveloped.

Abide says its proprietary technology can identify small molecules that block the activity of serine hydrolases. It is based on a 2010 breakthrough at the Scripps Research Institute by Abide co-founders Ben Cravatt, professor and chair of the department of chemical physiology, and Dale Boger, professor of chemistry. Their method first uses a probe to permanently label the active site of serine hydrolases in cell and tissue assays. Abide then screens libraries of compounds to find molecules that block the activity of the labeled site.

“We can interrogate these enzymes in their native configurations in all tissues,” Ezekowitz said. “I don’t believe anyone else has this capability. . . .”

This is shaping up to be a very interesting, high-stakes “Kentucky Derby” for the next big thing, in diabetes. Speaking of which, we’ll travel to enjoy the Downs, this weekend. Travel safely, one and all!


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