Thursday, July 22, 2010

Bottom of the pyramid

 Indian patients no longer have to wait for the drug to become generic. Recently BMS and Astra Zeneca launched their new oral pill Saxagliptin (DDP 4 inhibitors ) to treat type 2 diabetes in India, less than one year after its US approval. India is the first Asian country where the drug is available at affordable price which is 1/5 of its US cost.


Pharma Companies are now realizing that there is tremendous opportunity in emerging markets, not only because they entail low operating costs but also because of the fast growing middle class population, they are emerging as a huge market for global products. As the economy grows life style associated diseases grow along with it, Therefore companies try to launch drugs for these life style related diseases such as diabetes. Forecasts suggest 50% of business will be in those markets by 2020. Acquisition of Daichi to Ranbaxy and Abbot by Piramals make it clear that big pharma companies want to make a strong market presence in India.

“Rather than trying to find a use for approved medicines that were developed for a non-Asian phenotype, the move is to discover and develop medicines specifically to treat Asian diseases,” explains Paul Bolno, VP of Oncology R&D, Business Development at GSK. Here is a Nature article

But it will take a long time for the local doctors here in Inida to stop giving the pills without any label and any expiry dates on it. (pic; which I was given by a local hospital for a mild fever, you have to remember the tablets by its color)

Wednesday, July 21, 2010

PhD fellowships

Faculty of Pharmaceutical Sciences, University of Copenhagen is announce that eight PhD fellowships will be available from 1 October 2010.You can read more about here

Tuesday, April 27, 2010

Kinase Inhibitors: beyond Oncology


We just published a paper in Bioorganic and Medicinal Chemistry, targeting Interleukin-2 inducible T-cell kinase (ITK) for treating Asthma.
Protein kinases are prime targets for anticancer therapies, but achieving specificity for a particular kinase is challenging because of their close structural similarities. This leads to unwanted side effects and the toxic outcome may also be due the result of tissue distribution of kinase inhibitors. Imatinib has been highly successful in the treatment of both chronic myelogenous leukaemia , gastrointestinal stromal tumours and other cancers,but associated with severe, cardio toxicity. Toxicity may be of less concern with oncologic kinases, What about non- cancer indications? Emerging clinical evidence (Nature Drug Discovery) of oral kinase inhibitors other than cancer shows that kinases could be effective at inhibiting number of inflammatory pathways.

Almost all the p38MAPK inhibitors having hepatotoxicity issue, SCIO 469 and Arry 797 initially developed for RA but went in to clinic for post operative dental pain , here the potential toxicity problems won’t show up because the drugs is used only for a very short time, Are BMS-582949 and VX 702 still in development? Hundreds of millions have been spent by different companies on P38 with nothing to show at the end.

Tasocitinib may be the first kinase inhibitor (JAK3) for non-oncology indication and the first oral DMARD for RA in a decade, if it successfully completes the Phase III

Friday, April 16, 2010

Naked Discovery

 Unlike the highest secrecy in closed door traditional drug discovery by pool of rigid mindset scientists,  the Open Source Drug Discovery (OSSD) Program aims to address the issue by attempting to capture the youngest and brightest minds around the globe to be a part of developing drugs to treat drug resistant TB, malaria and HIV. Open source software may have been around for many years, but using an open source model to speed up drug discovery is a relatively new idea
"Research labs in India are filled more with technicians, as opposed to creative minds. You really don’t need to have a doctorate in pharmacy to contribute to developing a drug"said Samir Brahmachari, Director General of India’s Council of Scientific and Industrial Research (CSIR), and he believes that the OSDD can be as successful as Linux or a Wikipedia.

Tuberculosis kills at least 3,30,000 Indians annually and 1.7 million people Globally.The incidence of multi- and extensively drug resistant strains of TB ( MRD- and XRD- TB ) demands renewed efforts in the development of novel class of fast acting anti TB chemotherapeutics. Recently, Indian scientists have mapped the Mtb tuberculosis genome under the OSDD initiative of CSIR, giving hope of discovering new drugs for TB. This is the first time that comprehensive mapping of the Mtb genome has been accumulated, confirmed and made available publicly

This Connect to decode‘S (C2D) finding may contain critical data to unlock previously undiscovered details of TB resulting in development opportunities for urgently needed new drugs in India and other developing countries

Thursday, March 25, 2010

Retropharmacology: From Drug to lead

Drug discovery is a lengthy, high risk and costly endeavor; many strategies exist to accelerate the development process to provide the highest quality of the candidate. The diminished interest in Natural products drug discovery as the industry embraced promising and exciting new technologies, particularly combinatorial chemistry, but these new technologies promise to fill drug development pipeline with small molecule candidates is unfulfilled. Learning from the past with the appropriate strategy for the future is essential to make a significant difference
Valerian (valeriana officinalis) has been used as a medicinal herb science at least the time of ancient Greece and Rome as a sedative, migraine treatment, pain reliever , insomnia and other disorders as an alternative to benzodiazepine drugs
Valerenic acid which is a major constituent of common valerian is a potent modulator of GABA-A receptors. Inorder to develop a broader understanding of structural requirements for GABA-A modulatory activity of valerenic acid Kopp s et al (chem med chem) synthesized several analogues, and found that some of the derivatives such as tetrazole (pic) are proved to be the most potent allosteric potentiators of GABA-induced ion currents, and its activity is exceeds the activity of valerenic acid and Diazepam

This reverse pharmacology approach, relates to reversing the routine ‘laboratory-to-clinic’ progress to ‘clinics-to-laboratories’(inspired by traditional medicine), can offer a smart strategy for new drug candidates

Thursday, March 4, 2010

Small molecules or biopharmaceuticals

The movement of big pharma into biologics (biopharmaceuticals) understandably has a direct effect on pharmaceutical landscape. Companies shows a diminishing portfolio revenue from small molecules drugs, primarily because of patent expiration on blockbuster drugs (small molecules) and also due to the reallocation of industry resources towards biologics.



Biologics represent one of the most promising frontiers in pharmacotherapy, USFDA approved more biologics in 2009, the figure include 19 new molecular entities (NMEs) and six novel biologics. In 2008 FDA approved 21 NMEs and 3 novel biologics. A substantial improvement in biologics approvels in 2009. (fig.1, Nature medicine,139,16,2010) and it is expected to take over from small molecule field in the coming years( fig 2, Nature reviews/drug discovery ), But their cost can be substantial, reaching $ 200,000 or more annually for treatment (Cerezyme) and the large molecules drugs are administered via injection – a less popular option with patients.



Biologics are gradually going to replace the traditional approach to drug design. Students need to understand industries changing need, if they plan on carriers in this area.