Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA
Apr04

Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA

Bookmark this page now, folks. On Wednesday, April 10, I will be here, liveblogging the public debut of five drug candidates' structures. The "First Time Disclosures" Session at the ACS National Meeting in New Orleans runs from 2PM-4:55PM Central time. I am not able to conjure up a permalink to the session program, so here's a screengrab instead. 1:20PM I'm in hall R02, where the session's set to begin in about 40 minutes. Found a seat with a power outlet nearby, so I'm good to go! 2:29PM BMS-906024 Company: Bristol-Myers Squibb Meant to treat: cancers including breast, lung, colon, and leukemia Mode of action: pan-Notch inhibitor Medicinal chemistry tidbit: The BMS team used an oxidative enolate heterocoupling en route to the candidate-- a procedure from Phil Baran's lab at Scripps Research Institute. JACS 130, 11546 Status in the pipeline: Phase I Relevant documents: WO 2012/129353 3:02PM LGX818 Company: Novartis Institutes for Biomedical Research and Genomics Institute of the Novartis Research Foundation Meant to treat: melanoma with a specific mutation in B-RAF kinase: V600E Mode of action: selective mutant B-RAF kinase inhibitor Status in the pipeline: Phase Ib/II Relevant documents: WO 2011/023773 ; WO 2011/025927 3:47PM AZD5423 Company: AstraZeneca Meant to treat: respiratory diseases, in particular chronic obstructive pulmonary disease Mode of action: non-steroidal glucocorticoid receptor modulators Medicinal chemistry tidbit: This compound originated in part from a collaboration with Bayer Pharma. Status in the pipeline: Phase II Relevant documents: WO 2011/061527 ; WO 2010/008341 ; WO 2009/142568 4:17PM Birinapant (formerly known as TL32711) Company: TetraLogic Pharmaceuticals Meant to treat: cancer Mode of action: blocks the inhibitor of apoptosis proteins to reinstate cancer cell death Status in the pipeline: Phase II Relevant documents: US 8,283,372 5:00PM MGL-3196 (previously VIA-3196) Company: Madrigal Pharmaceuticals, acquired from VIA Pharmaceuticals, licensed from Roche Meant to treat: high cholesterol/high triglycerides Mode of action: mimics thyroid hormone, targeted to thyroid hormone receptor beta in the liver Medicinal chemistry tidbit: this molecule was discovered at Roche's now-shuttered Nutley site. Status in the pipeline: completed Phase I trials Relevant documents: WO 2007/009913 ; WO 2009/037172 And that's it, folks! Watch the April 22nd issue of C&EN for more on this...

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More On Malaria Open Innovation Announcement
May21

More On Malaria Open Innovation Announcement

A slew of molecules that might lead to the next antimalarial drug are up for grabs, now that GlaxoSmithKline, the Genomics Institute of the Novartis Research Foundation, and a consortium led by a St. Jude Children's Research Hospital team have released their data into the public domain. As I wrote today, this is great news for the malaria community, which has to do drug discovery on a shoestring compared to, say, the oncology community. But a large-scale data free-for-all like this one (GlaxoSmithKline says that their collection is the largest one that a pharmaceutical company has made universally available) is bound to set some precedents. We've blogged about open innovation for neglected diseases before, noting that skeptics may wonder if these efforts will lead to a warm fuzzy feeling rather than tangible scientific progress. Researchers need to think carefully about how they release and curate their data so that doesn't come to pass, says Sean Ekins of Collaborative Drug Discovery, the US-based informatics service provider that is one of the hosts for GSK's dataset. Collaborative Drug Discovery (CDD) is a spinout of Eli Lilly & Company that is now working with the Gates Foundation to foster collaboration and open innovation approaches for tuberculosis, while CDD are also working with researchers on other neglected diseases. CDD worked closely with GSK to make the malaria data broadly available to the scientific community. "How can we ensure that the next datasets that come through will have a high value? How can we avoid False positive and false negative issues in assays?" Ekins asks. The issues he raises, to me, are similar to the ones Derek Lowe brought up a few months back, when GSK first announced they would be making their data public. Another important issue that still needs examining is that of coordination, Ekins adds. Consortia and public-private partnerships have emerged to fill up the thin malaria pipeline, but there is still more that can be done, he says. "The bigger picture here should be the acceleration of hits to drugs," Ekins says. "How this data will work to catalyze malaria drug discovery is a matter of discussion, but releasing the data is an important first step." On a related note, on our previous open innovation blog entry Jean-Claude Bradley commented: "Are the biotechs trying to generate any income from participating – or is this strictly a humanitarian contribution?" I don't know about every case, but for this case I asked GSK: Suppose one of these compounds is successful in clinical trials and becomes a bona fide drug one day. How are the rights to the compound distributed? Here's the reply...

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