Small is beautiful for Genentech

Related tags Genentech Protein Epidermal growth factor receptor

Genentech's strategy of expanding beyond its traditional territory
of protein-based drugs and into small molecules was reinforced
earlier this week by its new agreement with Array BioPharma.

The two companies entered into an agreement to discover and develop small-molecule cancer drugs against two molecular targets. Genentech is hoping to spread the risk in its oncology franchise as biologics for cancer - i.e. Herceptin (trastuzumab) for breast cancer and Rituxan (rituximab) for non-Hodgkin's lymphoma - begin to mature.

This marks a general trend in the biotechnology sector to develop capabilities outside therapeutic proteins, according to market research firm Datamonitor.

In June 2003, Genentech licensed Curis' small molecule inhibitors of the Hedgehog signaling pathway for novel applications in cancer therapy. Among them is CUR-61414, a compound that is being investigated as a potential treatment for basal cell carcinoma, the most common form of cancer in the US with more than 800,000 new cases diagnosed each year.

Meanwhile Genentech, with the help of is partner OSI Pharmaceuticals, is hoping to launch its first anticancer small molecule Tarceva (erlotinib HCl) before the end of 2004. This is an active tyrosine kinase inhibitor targeted against the epidermal growth factor receptor (EGFR) found in non-small cell lung and pancreatic cancers.

Tarceva is expected to perform well either alone or, even better, in combination with Avastin (bevacizumab), an antibody drug that Genentech has developed which also hits EGFR. Despite competition from AstraZeneca's Iressa (gefitinib) and ImClone Systems, Bristol-Myers Squibb and Merck KGaA's Erbitux (cetuximab) - both recently approved for marketing - Tarceva should generate sales of around $520 million in 2008, according to Datamonitor.

But Genentech is not the only protein expert to start investing in small molecules. For example, Amgen has licensed Biovitrum's small molecule 11 beta HSD1 enzyme inhibitors for the treatment of metabolic diseases and certain other medical disorders.

And yesterday Amgen signed an additional agreement with Infinity Pharmaceuticals to develop a series of small-molecule drugs against various targets. The biotechnology bellwether made a $25 million (€19.5m) investment in Infinity as part of the deal, giving it a 15 per cent stake in the firm.

As the area of therapeutic proteins continues to mature, current leading biotech houses will be forced to expand their expertise. They will need to invest in new technologies that can realistically achieve satisfactory clinical efficacies in complex diseases where molecules with higher penetrative power are needed. And small molecules - with their oral bioavailability and ease of administration - fulfil these criteria.

Related topics Ingredients

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