• SMR Award Meeting: Recent Disclosures of Clinical Candidates - December 10th, London.


    There is, what looks like, an excellent meeting in London, full details are on the SMR website. I hope I feel better by then.


    SMR Award Meeting: Recent Disclosures of Clinical Candidates
    10th December 2009
         National Heart & Lung Institute, Kensington, London
    Programme:

    09.30
    		Registration and coffee
    10.00
    		SMR Award lecture: The Discovery and development of Januvia™, Dr. Ann Weber, Merck
    (Introduction by - Rob Williams,     Cancer Research UK)
    Session 1 - Chair: Mark Searcy, University of East Anglia
    11.00   
    		Chris Murray, Astex
    From fragment to clinic - the discovery of the hsp90 inhibitor, AT13387.
    11.45
    		George Muller, Celgene
    The discovery of apremilast.
    12.30
    		Lunch (Including SMR AGM 13.10-13.30)
    Session 2 - Chair: Diane Coe, GSK
    13.30
    		David Fox, Pfizer
    The discovery of a second generation long-acting PDE5 inhibitor.
    14.15
    		Simon Hodgson, GSK
    The discovery of a dual H1/H3 antagonist for allergic rhinitis.
    15.00
    		Tea
    Session 3 - Chair: David Fox, Pfizer
    15.30
    Karl Gibson, Pfizer
    The discovery of a progesterone receptor antagonist for endometriosis.
    16.15
    		Mairi Gibson, GSK
    Second generation EP1 antagonists for the treatment of pain.
    17.00
    		Close

  • ChEMBL-announce mailing list


    We have set up a mail list for ChEMBL related matters. To subscribe try clicking here

  • USANs and Clinical Development

    I was mailed about how USANs/INNs fit into the drug development process. There is an excellent and detailed overview on the AMA website, and I've taken the liberty of reproducing some of the most salient points here (however, the preceeding link and the content therein is the definitive source!). The other terms you'll often see in this sort of area are JAN and BAN (which are Japanese Approved Name and British Approved Name respectively), BANs with the exception of adrenaline/epinephrine are the same as INNs now.

    • Preclinical
      • Drug studies conducted in vitro and in animal models
      • Planned trade names may be filed, if known, with the United States Patent and Trademark Office (USPTO) and other trademark offices
      • Data about the mechanism of action and potential safety problems that could derail marketing are gathered
    • IND
      • Firm obtains permission to conduct clinical studies in the United States (US) from the FDA and receives an IND number
    • Phase 1
      • Small-scale safety studies conducted in healthy volunteers
      • Earliest time that US firms may request a United States Adopted Name (USAN), or non-US firms may request an International Nonproprietary Name (INN)
    • Phase 2
      • Small-scale efficacy studies in patients
      • Typical time for US firms to apply for a USAN
      • Ballots sent to USAN Council (USANC) for review
      • When firm and USANC reach consensus, USAN Program files to obtain an INN on behalf of the firm
      • Planned trade names may be filed for review by FDA, along with supporting documentation
    • Phase 3
      • Large-scale efficacy and safety studies in humans
      • Many firms publish results of earlier clinical and preclinical studies and want the USAN at this time
      • USAN usually adopted and published
      • Non-US firms with an INN obtain USAN status for this name
    • New Drug Application (NDA) or Biologics Licensing Application (BLA)
      • Firm requests clearance from the FDA to market the drug
      • USAN required for packaging and labeling negotiations, promotional materials
      • USP adds nomenclature information pertaining to dosage forms and delivery methods
      • Firm receives final approval of trade name from the FDA

    Thanks to xkcd for the cartoon above...

  • What Fraction of Drug Approvals Are Biologicals?

    Continuing some earlier posts, here is a brief update. Below is a graph of NME approvals (US FDA) for the period 2003-2009. As is plain, there is no clear upwards trend for biologicals over this time period, and looking at INN approved names, it looks as if small molecules will be around as the major drug class for some time to come. 'Small molecules' are in various shades of blue, while 'biologicals' are in various shades of bluepink.

    The cartoon at the top of this post was harvested from www.xkcd.com which is a site that is probably not safe for work (nsfw) - unless your work involves browsing cartoons with occasional adult humor.

  • Charles Darwin was mostly made from proteins

    Just a little diversion, but a nice one at that. I am a fan of LinkedIn - it really is the only way to maintain an address book in these volatile times! Anyway, I recently got in touch with a colleague from the past, and clicked his blog, listed on LinkedIn. Oh My Goodness Me! Very interesting and cool photos. But for those with a more scientific bent click below (and then keep clicking the image further and further).

    Darwin Image

  • ChEMBL interface: Call for Testers

    So, we have an initial interface for the ChEMBL SAR data, and we are looking for some interested people to do some testing, find issues with different OS, browsers, java versions, etc. The kinase SARfari testing we did was very helpful, and many, many thanks to those of you that helped, but rest assured, we will mail you for feedback, bugs, etc.

    If you wish to take part, please mail us

  • Kinase SARfari has been updated

    We have released an update to Kinase Sarfari, the major changes are:

    Frontend Changes

    1. Compound report card now displays smiles, inchi, inchi_key
    2. Bioactivity data download now includes smiles
    3. User guide updated
    4. Starlite references changed to ChEMBL

    Backend Changes

    1. Migrated kinasesarfari schema from chemdev to chempro (an internal trifle, but important to us ;)
    2. Schema clean up

    Thanks for all the feedback!

  • Todays Found Natural Product: 1: Xylindein

    Out with the dogs today I found something I had been looking for for years - Green Elf Cups, or less excitingly known as Green Wood Cups (Chlorociboria aeruginascens) a very small and elusive fungus that stains the dead wood (usually oak) it is growing in, a brilliant blue-green color. This stained wood has been prized since the middle ages for its decorative properties. This specimen had the fruiting bodies out and was quite striking. The blue-green color is due to a highly conjugated natural product Xylindein - a dimeric naphthoquinone.