Drugs in Clinical Pipeline: Vanucizumab | Bi-Specific Monoclonal Antibody | Angiogenesis Inhibitor | A2V CrossMAB | Anti-Vascular Endothelial Growth Factor A (VEGF-A) | Anti-Angiopoietin-2 (Ang-2) | Cancer Treatment

Vanucizumab (also known as RO5520985; RG7221) is a novel bi-specific human Immunoglobulin G (IgG1) monoclonal antibody that simultaneously binds to two key angiogenic factors, Vascular Endothelial Growth Factor A (VEGF-A) and Angiopoietin-2 (Ang-2). The bi-specific monoclonal antibody comprise of two different heavy chains and two different light chains. One arm of the antibody binds Angiopoietin-2 (Ang2) Ang-2 which is based on LC06, an Ang-2 selective human IgG1 antibody. The other is based on Bevacizumab which binds Vascular Endothelial Growth Factor A (VEGF-A) [1, 2].

Drugs in Clinical Pipeline: Cabiralizumab | Monoclonal Antibodies (mAbs) | Cancer Treatment | Anti-Inflammatory Agents | Anti-CSF1R Antibody

Cabiralizumab (also known as FPA008) is a humanized IgG4 monoclonal antibody that binds to human colony stimulating factor 1 receptor (CSF1R), and blocks the ability of IL34 and CSF1 to activate CSF1R expressed on macrophages. Cabiralizumab specifically targets macrophages and monocytes, immune cells that are activated or elevated in multiple disease settings [1, 2].

Drugs in Clinical Pipeline: TGR-1202 | Orphan Drug | Kinase Inhibitor | Phosphoinositide 3-kinase delta (PI3Kδ) Inhibitors | Cancer Drug

TGR-1202 [(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one] is a potent, orally available, small molecule selective phosphoinositide 3-kinase (PI3K) delta (PI3Kδ;  IC₅₀ = 22.23 nM) kinase inhibitor with high selectivity over all other PI3K isoforms (48 – 10000 times) as well that for a 441-kinase panel. The selectivity and activity of TGR-1202 is credited to its design with a unique backbone compared to other PI3K inhibitors in development [1, 2].

TGR-1202 : 2D and 3D Structure

TGR-1202 is currently under clinical development for patients with relapsed and refractory hematological malignancies.

On Aug 24, 2016 TG Therapeutics, Inc. announced that the U.S. Food and Drug Administration (FDA) has granted orphan drug designation for the oral, next generation PI3K-delta (PI3Kδ) inhibitor, TGR-1202, in the treatment of patients with Chronic Lymphocytic Leukemia (CLL).

Magnetic and Photodynamic Nano-Liposomes in Tumor Eradication

Magnetic and Photodynamic Nano-Liposomes in Tumor Eradication

Researchers have designed an optimized smart nanoplatform based on dually loaded hybrid liposomes to achieve enhanced tumor therapy. 

The aqueous core was highly loaded with iron oxide nanoparticles, while the lipid bilayer was supplied with a photosensitizer payload. The double cargo translated into double functionality: generation of singlet oxygen under laser excitation and heat production under alternating magnetic field stimulation, coupling photodynamic therapy (PDT) to magnetic hyperthermia (MHT). These liposomes address both therapeutic agents within tumor cells, and the combined PDT/MHT therapy resulted in complete cancer cell death in vitro while total solid-tumor ablation was achieved in an in vivo rodent model.

Article citation: Di Corato, R.; et. al. Combining Magnetic Hyperthermia and Photodynamic Therapy for Tumor Ablation with Photoresponsive Magnetic Liposomes. ACS Nano 2015, 9 (3), 2904-2916.