Cellzome Inc (headquartered in Boston, Massachusetts and with operating companies in Heidelberg, Germany and Cambridge, UK), a privately-held drug discovery company, and GlaxoSmithKline (GSK) (LONDON, UK) announced a worldwide strategic alliance to discover, develop, and market small-molecule kinase-targeted therapeutics to treat inflammatory diseases. The alliance gives GSK access to Cellzome’s expertise in identifying and developing selective kinase inhibitors and its proprietary Kinobeads™ technology which, by screening compounds in a physiological setting, is designed to improve the predictability of these drug candidates’ performance in clinical testing. Kinobeads technology uses native kinases directly isolated from human cells and tissues such as blood or synovial fluid. The companies will be working to discover and develop improved approaches to existing biologic therapies which cannot access intracellular signaling mechanisms.

Under the agreement, GSK has exclusive options to license drug candidates from Cellzome’s kinase programs directed against four identified targets, and three additional targets to be identified by both companies. In the alliance, Cellzome will utilize its proprietary Kinobeads technology to discover novel small molecule inhibitors of these targets, and then will develop the most promising product candidates through to completion of a clinical proof-of-concept trial, unless GSK elects to exercise its option earlier.

Cellzome is eligible to receive milestone payments from GSK as product candidates are advanced. Upon Cellzome’s achievement of clinical proof-of-concept for a product candidate for a particular kinase target, GSK would have an exclusive option to license all product candidates from that program. GSK would then assume full responsibility for further clinical development and commercialization on a worldwide basis. Cellzome retains the right to continue the development and commercialization of drug candidates if GSK chooses not to exercise its option to that program.

Under the terms of the agreement, Cellzome will receive upfront payments of £14.4 million (~US $25 million) comprising both cash and equity. Cellzome is eligible for up to £118 million (~US $207 million) per program in potential development, regulatory, and commercial milestones and up to double digit royalties on net sales of products resulting from the alliance.

Cellzome’s Kinobeads technology enables the screening and profiling kinases in disease-relevant cells and tissues. Cellzome is applying its technology to the discovery and development of small-molecule kinase inhibitors targeting key inflammatory mediators such as PI3Kγ (a dual lipid-protein kinase and a key mediator of directed movement of immune cells towards chemoattractants), PI3Kδ (which signals downstream of B-cell and T-cell receptors), Zap-70 (a member of the protein tyrosine-kinase class of drug targets and which activates Itk and other proteins after T-lymphocyte stimulation by antigen binding to the T-cell receptor), Jak3 (a cytoplasmic protein tyrosine kinase that associates with the common gamma chain (γC) of the type I cytokine receptor family), and mTOR (a serine/threonine protein kinase that regulates cell growth, proliferation and survival); as potential oral therapeutics for rheumatoid arthritis, lupus, inflammatory bowel disease, psoriasis, multiple sclerosis, and asthma.