Date: 2014-09-23
Type of information: Licensing agreement
Compound: selective PI3K delta kinase inhibitors, including RP5264 and backup molecules
Company: Rhizen Pharmaceuticals (Switzerland) TG Therapeutics (USA - NY)
Therapeutic area: Cancer - Oncology - Autoimmune diseases
Type agreement: joint-venture
development
commercialisation
Action mechanism: The phosphoinositide-3-kinases (PI3Ks) are a family of enzymes involved in cellular functions, including cell proliferation and survival, cell differentiation, intracellular trafficking and immunity. The delta isoform of PI3K is strongly implicated in B-cell related lymphomas. Rhizen has developed novel selective inhibitors of PI3Kδ pathway, believed to be important in the proliferation and survival of B-cell lymphocytes. The lead candidate TGR-1202 (formerly known as RP5264) is an orally available PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. Inhibition of PI3K delta signaling with TGR-1202 has demonstrated robust activity in numerous pre-clinical models and primary cells from patients with hematologic malignancies.
Disease: haematological cancers, autoimmune diseases
Details: * On August 16, 2012, Rhizen Pharmaceuticals, a biopharmaceutical company focused on the discovery and development of novel therapeutics for the treatment of cancer, inflammation, autoimmune diseases and metabolic disorders, and TG Therapeutics, focused on developing and commercializing therapeutic products for cancer, have announced a joint venture collaboration for global development and commercialization of Rhizen’s Novel selective PI3Kδ kinase inhibitors.
The selected lead RP5264 (hereafter, to be developed as TGR-1202) is currently being positioned for the treatment of haematological malignancies. Beyond RP5264, Rhizen would contribute backup molecules providing multiple opportunities for TG to develop differentiated therapies against haematological cancers and autoimmune diseases while, retaining joint governance role in the joint-venture.
Financial terms: Under the terms of the current joint-venture agreement, TG will pay Rhizen an execution fee and predetermined milestone payments linked to clinical development of products till Phase II. The joint-venture has a built-in option for both TG and Rhizen to convert into a licensing agreement during development whereby, TG would in-licence and assume entire responsibility for developing and commercializing RP5264 globally. Rhizen would then be entitled to an up-front payment and other milestone payments of circa $250M plus royalties and profits on sublicensing. In addition, Rhizen retains global manufacturing and supply rights for API and formulation for clinical and commercial purposes.
Latest news: * On September 23, 2014, Rhizen Pharmaceuticals announced an out-licensing agreement for TGR-1202, a novel next generation PI3K-δ inhibitor. TG Therapeutics exercised its option for early conversion to a licensing agreement from a 50:50 joint venture partnership. In exchange for this licensing agreement, TG Therapeutics will pay Rhizen an upfront payment of $8.0 million ($4.0 million in cash and $4.0 million in TG Therapeutics common stock). In addition to the upfront payment, Rhizen will be eligible to receive regulatory filing, approval and sales based milestones in the aggregate of approximately $240 million, and tiered royalties based on net sales. Rhizen also retains global manufacturing and supply rights. TG Therapeutics will receive exclusive worldwide rights, excluding India, for the development and commercialization of TGR-1202 for all indications. TGR-1202 is now being prepared for Phase 3 clinical trials.
