The ChEMBL-og

Recently approved by the FDA, on September 25th 2009, was Ustekinumab, marketed under the trade name Stelara. Ustekinumab, previously known as CNTO-1275, is a first-in-class injectable biological drug blocking signalling of two distinct interleukins ( IL-12 and IL-23 ) and is indicated for the treatment of adults with moderate to severe plaque psoriasis . Psoriasis (ICD-10: L40 ) is a complex autoimmune disease, typically leading to the formation of scaly red or silvery-white plaques on the skin. Another drug with the same mechanism as Ustekinumab (blocking IL-12 and IL-23 signalling) is ABT-874, ABT-874 is currently still in clinical trials. Ustekinumab is dosed as a subcutaneous injection given at weeks 0 and 4, followed subsequently by every-12-week maintenance dosing. The recommended starting dose of is 45 mg for patients weighing 100 kg or less, and 90 mg for patients weighing more than 110 kg (the 45mg dose corresponds to a 0.31 umol dose). Ustekinumab is is a human IgG1қ mo...

The latest new drug approval, on 11th September 2009 was Telavancin - which was approved for the treatment of adults with complicated skin and skin structure infections (cSSSI) caused by susceptible Gram-positive bacteria , including Staphylococcus aureus , both methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) strains. Telavancin is also active against Streptococcus pyogenes , Streptococcus agalactiae , Streptococcus anginosus group (includes S. anginosus, S. intermedius and S. constellatus ) and Enterococcus faecalis (vancomycin susceptible isolates only). Telavancin is a semisynthetic derivative of Vancomycin. Vancomycin itself is a natural product drug, isolated originally from soil samples in Borneo, and is produced by controlled fermentation of Amycolatopsis orientalis - a member of the Actinobacteria . Telavancin has a dual mechanism of action, firstly it inhibits bacterial cell wall synthesis by interfering with the polymerization and cross-linking of peptid...

The European Commission and EFPIA (European Federation of Pharmaceutical Industries and Associations) has recently announced the 2nd round of the Innovative Medicines Initiative (IMI) scheme, the amount of funding available is quite substantial, but arguably more important to the research community is the embracing of open data and services, and in particular coordinated pre-competitive activities (there is a lovely recent paper on these sort of activities here , a subscription may be required) %J Nature Rev. Drug Discov. %D 2009 %P 701-708 %T Lowering industry firewalls: pre-competitive informatics initiatives in drug discovery %A Barnes MR %A Harland L %A Foord SM %A Hall MD %A Dix I %A Thomas S %A Williams-Jones BI %A Brouwer CR To quote from the EU Commissioner of Science and Research, Janez Potocnik. "We should see results from this exciting new research mechanism very soon and [...] new innovative medicines should reach European patients faster" To quote from Bi...

Kinase SARfari is now live and online - free and open to one and all. We'll keep an eye on machine logs for the next couple of weeks, and so we may bounce it now and then. Please let us know if you have any issues with using it, and please tell us OS and browser versions for any bug reports. The URL for kinase SARfari is http://www.sarfari.org/kinasesarfari Full source code is also available, licensed under a very permissive Creative Commons licence. Mail us if you want this, but as soon as we sort out our downloads area, it will also be available from there. The data in the backend database is in the process of being updated to a more recent data cut, and when this is done, we'll post details. We're also resurrecting the rhodopsin-like GPCR version. There is also an email address for sarfari support issues .

Here is a paper (subscription required). It is written by Lee Harland (Pfizer Regenerative Medicine) and Anna Gaulton (ex Pfizer, but now in the ChEMBL group at the EMBL-EBI). It is an overview of Drug Targets, and some of the general principles of 'druggability' and ways to assess target tractability for drug discovery. In particular, the challenges of data integration are discussed. %A L. Harland %A A. Gaulton %T Drug Target Central %J Expert Opin. Drug. Disc. %V 4 %P 857-872 %D 2009