biokine

BKT150

admin — Wed, 02 Feb 2011 15:41:00 +0000

The chemokines receptor CCR6 and its ligand CCL20 are involved in the progression of certain cancers such as colon, prostate and lung as well as in the development of various inflammatory diseases such as Multiple Sclerosis.

Biokine initiated the preclinical development program of a CCL20 antagonist in 2011.

Pipeline

admin — Mon, 31 Jan 2011 14:14:32 +0000

Biokine has developed a suite of unique approaches to target cancer and inflammation and is conducting preclinical and clinical research on several molecules discovered in-house.

BKT140

admin — Mon, 31 Jan 2011 14:14:13 +0000

The company’s lead compound, BKT140, is a unique CXCR4 antagonist which is developed for a variety of CXCR4 based therapeutics including stem cell mobilization, cancer treatment, tissue regeneration, inflammation and autoimmunity.

The BKT140 drug product is being developed for subcutaneous (SC), intravenous (IV), and oral administration.

BKT130

admin — Mon, 31 Jan 2011 14:14:05 +0000

BKT130 is a unique chemokine antagonist which inhibits in vitro and in vivo the bioactivity of inflammatory chemokines.

Furthermore, BKT130 is effective in treatment of Multiple Sclerosis in mice models (EAE), inhibits delayed type hypersensitivity (DTH) in mice model, inhibits disease symptoms in rat model for myasthenia gravis (MG) (experimental autoimmune MG (EAMG)), and effectively blocks lymphocytes entrance to the site of inflammation of Rheumatoid Arthritis joints in animal model. Biokine has embarked on the preclinical development of BKT130 for the treatment of Rheumatoid Arthritis.

BKT130

admin — Sun, 30 Jan 2011 10:50:48 +0000

Chemokines combinatorial function governs autoimmunity and inflammation. Thus, targeting a single chemokine or chemokine receptor, has produced meager results in autoimmunity and inflammation. Biokine has developed a pipeline of anti inflammatory leads, targeting multiple inflammatory chemokines.

Biokine lead compound, BKT130, is a unique peptibody which can inhibit the response of immune cells to key inflammatory chemokines: MCP-1, MIP-1a, RANTES, Eotaxin, IP-10, Mig, and I-TAC.In animal models for autoimmunity and inflammation BKT130 inhibits the development and progression of inflammation and autoimmune diseases such as Multiple Sclerosis, Rheumatoid Arthritis and Myasthenia Gravis.

Figure Legend – Significant inhibition of MNCs accumulation and tissue damage in the joints of mice following single administration of BKT130. Mouse model of antigen-induced arthritis (AIA)

BKT140

admin — Sun, 30 Jan 2011 07:43:28 +0000

BKT140 is a highly selective inverse agonist of CXCR4, with a high affinity (0.8nM) and a low rate of dissociation from its receptor. These biochemical characteristics are unique for BKT140 and enhance its potential as a therapeutic compound.

Pre-clinical studies in animal models with BKT140 showed a robust mobilization of hematopoietic stem cells. Furthermore, BKT140 also showed a direct and indirect anti-tumor effect in vitro and in vivo against a variety of human-derived tumors, such as multiple myeloma, lymphoma, leukemia, neuroblastoma, retinoblastoma and lung cancer.

BKT140 directly stimulates apoptosis (cell death) of certain types of tumors, interferes with CXCR4 mediated drug-resistance of tumor cells (CAM-DR), and enhances the therapeutic potential of anti-cancer drugs that fail to eliminate residual disease and cancer stem cells.

Tumors cells (black arrow) treated with BKT140 undergo apoptotic cell death and necrosis which lead to inflammatory response (red arrow). Biokine has also shown BKT140 to stimulate the regeneration of damaged tissues, such as the skin and bone marrow.

Clinical trials – Phase I/IIa

Biokine has recently finalized a Phase I/IIa, non-randomized, open label, single dose, dose-escalation, safety and efficacy study of BKT140 in multiple myeloma patients that undergo stem cell mobilization for transplantation.

BKT140 had an excellent safety profile and was well tolerated at all doses tested (30-900 µg/kg). BKT140 was rapidly absorbed with no observed lag time, with peak plasma concentrations occurring 0.5h after administration. Clearance was rapid, with a median terminal half-life of 0.3-0.7h at 300 and 900 µg/kg respectively.

BKT140 induced a robust and dose dependent mobilization of progenitor stem cells and lymphocytes from the bone marrow to the peripheral blood in all patients tested. At high doses (0.3, 0.9 mg/Kg) mobilization of stem cells and lymphocyte was fast, within 2-4 hr, and remained for more than 24hr.

BKT140 Induced a dose dependent robust collection of CD34+ cells for transplantation. At the highest dose of BKT140 the number of collection events reduces to one and the average number of CD34+ collected was 20×10*6/per Kg. At the highest dose BKT140 the number of CD138+ multiple myeloma cells was reduced.

To validate the safety and efficacy of BKT140 as a mobilizer of stem cells and as an anti-multiple myeloma agent, Biokine is planning to initiate Phase II/III studies in multiple myeloma patients in 2011.