Research and Development Articles

CANCER R&D IS BOOMING RIGHT NOW. At a time of poor ratings on both Wall Street and Main Street, pharma can at least point proudly to its oncology pipeline as proof that it still takes big risks to make big advances against big killers—and win. According to a recent IMS report, the cancer pipeline contains 380 compounds, with nearly 100 in Phase III. The long-established standard of care—surgery, radiotherapy, and chemo—is fast giving way to a high-tech array of targeted therapies. These molecules and antibodies are designed to block specific disease pathways, and they are proving both far more effective and far more tolerable than the sledgehammer status quo. Since 1996, the overall survival rate for patients has jumped by 30 percent, from one-half to two-thirds.

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That was the collective vow sworn by Big Pharma last December following Pfizer's $1 billion–down–the–tubes withdrawal of the cholesterol compound they had touted as the most important drug of the decade. The question is, What's the right organizational construct to support innovation—or at least to stop Phase III failures?

The large-cap pharmas are all carrying out interesting experiments in how they do R&D, hoping to save time and money at no cost to quality. With Januvia, its novel type 2 diabetes drug, Merck has shown that it can be done. With a new CEO, who believed in bringing all the voices in the company together as one, and the implementation of an integrated new R&D model, Merck got Januvia to market in record-breaking time. Now, a mere six years after it was born, the drug stands to earn $762 million in sales.

A modified procedure of a previous synthetic route for baicalein was developed in order to obtain more than ten grams of baicalein for in vivo test. There were several difficulties in applying the published experimental procedures for a large scale of synthesis. The modified synthetic work was successfully accomplished by reducing amount of strong Lewis acid in Fries rearrangement and using tetrabutylammonium iodide as an additive to speed up the demethylation reaction in refluxing HBr into completion.

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Seven flavonoids were isolated from the whole plants and fruits of Cayratia japonica through the activity-guided isolation of a methanol extract using a monoamine oxidase (MAO) inhibition assay as a monitor. The chemical structures of the isolates were assigned as apigenin-7- O-¥â-D-glucuronopyranoside (1), apigenin (2), luteolin (3), luteolin-7-O-¥â-D-glucopyranoside (4), (+)-dihydroquercetin (taxifolin) (5), (+)-dihydrokaempferol (aromadendrin) (6) and quercetin (7). Among the isolated compounds, flavones such as apigenin (2) and luteolin (3), as well as the flavonol, quercetin (7) showed potent inhibitory effects against the MAO activity with IC50 values of 6.5, 22.6, and 31.6 ¥ìM, respectively. However, the flavone glycosides, apigenin-7-O-¥â- D-glucuronopyranoside (1) and luteolin-7-O-¥â-D-glucopyranoside (4), showed mild MAO inhibition (IC50 values: 81.7 and 118.6 ¥ìM, respectively).

A pair of new phenolic glycosides, crassifoside G (5) and isocrassifoside G (6), along with five known phenolic compounds (1-4 and 7), were isolated from the ethanolic extract of the rhizomes of Curculigo crassifolia. Their structures were established by spectroscopic techniques and chemical methods. Most of the isolated compounds exhibited strong antioxidant activity in the 1, 1-diphenyl-2-picryldydrazyl (DPPH) radical scavenging assay.

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For many in the pharma industry, information and research are key business drivers. But what drives the information business?

The answer—at least in recent years—has been globalization. As the pharma industry has taken an increasingly global view, market research companies have had little choice but to follow suit.

Today the information industry, in many ways, looks a bit like the pharmaceutical industry—with bigger companies but fewer of them. But unlike the consolidation craze that swept the industry, the extended reach of the market research industry offers some clear-cut benefits.

Establish a GxP mindset, commit to process development, and then concentrate on a manufacturing strategy.

Building a compliant supply chain and preparing for product launch at an emerging biotechnology or pharmaceutical company can be a challenging task. The infrastructure and systems that larger companies take for granted need to be built from the ground up, usually on a just-in-time basis with limited resources and little room for contingency planning. Frequently, the focus of companies approaching their first commercial product is research-based, with a mission to generate proof-of-concept data, which will propel the product to a profile that justifies increased investment in building development infrastructure. In such an environment some companies find themselves playing catch-up in the areas of chemistry, manufacturing, and control (CMC), and risk serious, costly delays in product approval or launch.

In this century, we are unlikely to face biomedical issues more complex and controversial than that of human cloning coupled with embryonic stem cell research. With the stakes so high — promises of cures and therapies for a host of devastating diseases and medical conditions set against impassioned disputes about when life begins — the cloning debate has evolved beyond the realm of scientific discourse and into the spotlight of public opinion. Unfortunately, this intense scrutiny, largely fueled by the media, has resulted in the misrepresentation of facts, and the twisting of scientific opinions as statements about cloning are often taken out of their appropriate context. In an attempt to counteract this damaging trend, The Science Advisory Board decided to poll its members about some of the most controversial aspects of the cloning debate.

The Food & Drug Administration has accepted Pfizer and Sanofi-Aventis' new drug application for Exubera (inhaled human insulin powder). For the past 80 years subcutaneous injection has been the only route for delivering insulin to patients with diabetes mellitus, which affects over 17 million people in the United States. Insulin therapy is required for patients with Type 1 diabetes, and many patients with Type 2 diabetes will require insulin therapy either alone or as an adjunct to their oral medications. Lack of acceptance of continuous subcutaneous insulin delivery or multiple daily injections have been barriers to obtaining optimal HbA1c levels.

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