ARTICLE | Product R&D

SHP-2 sets sail

How NIBR made the first drug-like SHP-2 inhibitor

August 11, 2016 7:00 AM UTC

Novartis AG researchers have revived a once-promising cancer target - a protein tyrosine phosphatase - by departing from the rote strategy of blocking its active site, and arresting the molecule in its inactive form instead. The company has created a preclinical inhibitor of the much-researched SHP-2, and believes the approach opens a new avenue for inhibiting more members of the class as well as other problematic enzymes.

Protein tyrosine phosphatases have been a highly sought-after class of cancer targets for nearly 20 years, but attempts to inhibit the proteins have never made it through clinical trials. Ionis Pharmaceuticals Inc. is the only company with a disclosed PTP inhibitor in human trials and has taken a different tack. The company's antisense oligonucleotide IONIS-PTP1BRx targets the mRNA of a different family member, PTP-1B, and is in Phase II for diabetes...