—Good Inhibitors Come In Twos “Researchers develop another direct inhibitor of the ‘undruggable’ cancer-associated protein K-Ras” Inhibitors of the cancer-associated protein K-Ras have been scarcer than hen’s teeth. But now two groups have popped up with them virtually simultaneously. Scientists had considered mutant Ras proteins to be “undruggable” because years-long efforts had yielded no direct inhibitors.
by Stu Borman | December 09, 2013
—Sweeter Enzyme Inhibitor “A novel glycosyltransferase inhibitor could aid glycobiology research and drug discovery” A glycosyltransferase (GT) inhibitor with a novel mechanism of action could aid glycobiology research and drug discovery, according to a report in Nature Chemical Biology (DOI: 10.1038/nchembio.343).
by Stuart A. Borman | April 19, 2010
But early data suggest that first eliminating a tumor’s protective environment with IDO inhibitors and then subjecting the tumor to checkpoint inhibitors, a class of drugs that release the brakes of immune cells, can form a powerful therapy. The field’s front-runner is Incyte’s IDO1 inhibitor epacadostat, currently in a Phase III clinical trial in combination with Merck & Co.’s checkpoint inhibitor Keytruda.
by Ryan Cross | March 30, 2018
—Inhibitor Targets Glycoprotein Of Unknown Structure “A fragment-based approach homes in on an inhibitor, even though the corresponding protein's structure is unavailable to help” Fragment-based drug discovery, combinatorial chemistry, and in situ click chemistry have been teamed together to rapidly identify a carbohydrate-like inhibitor for a key glycoprotein of unknown structure (Angew.
by Stuart A. Borman | August 09, 2010
—JAK Inhibitors Target Arthritis “” Incyte has earned a $50 million milestone payment from Eli Lilly & Co. for the initiation of Phase III trials on baricitinib, Incyte’s oral treatment for rheumatoid arthritis. Incyte disclosed the payment a week after FDA approved Pfizer’s oral rheumatoid arthritis drug Xeljanz. Both drugs are JAK inhibitors, which target signaling pathways inside cells that play a role in the inflammation involved in arthritis. Pfizer says Xeljanz is the first JAK inhibitor for rheumatoid arthritis and the first new oral rheumatoid drug in more than 10 years. /articles/90/i48/JAK-Inhibitors-Target-Arthritis.html 20121126 Concentrates 90 48 /magazine/90/09048.html JAK Inhibitors Target Arthritis JAK inhibitor, rheumatoid arthritis con bus Rick Mullin pharmaceuticals JAK Inhibitors Target Arthritis Chemical & Engineering News JAK Inhibitors Target Arthritis JAK Inhibitors Target Arthritis
by Rick Mullin | November 26, 2012
—Novartis, Array In MEK Inhibitor Pact “” Novartis has agreed to pay Boulder, Colo.-based Array BioPharma up to $477 million for access to ARRY-162, a MEK inhibitor in Phase I trials as a treatment for solid tumors. Array snags a $45 million up-front payment in the deal, which includes backup MEK inhibitors.
by Lisa M. Jarvis | April 26, 2010
—Genentech licenses Relay’s SHP2 inhibitor “” Genentech will pay $75 million to license RLY-1971, Relay Therapeutics’ SHP2 inhibitor, which is in a Phase 1 trial to treat solid tumors. The deal gives Genentech access to a promising partner for its experimental inhibitor of KRAS G12C, a notoriously difficult target for cancer drugs. SHP2 helps KRAS cycle between its “on” and “off” states, and researchers think dampening its effects could increase the efficacy of KRAS inhibitors, which bind to the protein’s “off” state. /pharmaceuticals/oncology/Genentech-licenses-Relays-SHP2-inhibitor/98/i48 20201217 Concentrates 98 48 /magazine/98/09848.html Genentech licenses Relay’s SHP2 inhibitor Cancer, KRAS, oncology, SHP2, Genentech con bus Lisa M. Jarvis pharmaceuticals oncology biological-chemistry cancer Genentech licenses Relay SHP2 inhibitor Chemical & Engineering News Genentech licenses Relay’s SHP2 inhibitor Genentech licenses Relay’s SHP2 inhibitor
by Lisa M. Jarvis | December 17, 2020
—Loxo buys BTK inhibitor “” Loxo Oncology will pay Redx Pharma $40 million for the full rights to an inhibitor of BTK, an enzyme involved in B-cell development. Imbruvica, a B-cell cancer treatment marketed by AbbVie, and other BTK inhibitors in clinical studies all covalently bind to the enzyme, a mechanism Loxo argues drives resistance to those molecules through a specific mutation. By reversibly binding to BTK, Redx’s lead molecule, RXC005, could help people with cancer who no longer respond to the covalent inhibitors. Now known as LOXO-305, the compound is expected to begin human trials next year. /articles/95/i32/Loxo-buys-BTK-inhibitor.html 20170807 Concentrates 95 32 /magazine/95/09532.html Loxo buys BTK inhibitor oncology, BTK inhibitor, leukemia con bus Lisa M. Jarvis pharmaceuticals Loxo buys BTK inhibitor Chemical & Engineering News Loxo buys BTK inhibitor Loxo buys BTK inhibitor
by Lisa M. Jarvis | August 07, 2017