Drugs in Clinical Pipeline: Erenumab | AMG 334 | Prevention of Migraines | CGRP Receptor Antagonist Monoclonal Antibody

Erenumab (AMG 334) is the first human monoclonal antibody antagonist against the Calcitonin Gene-Related Peptide Receptor (CGRP) receptor. Like the small-molecule CGRP-receptor antagonists, Erenumab fully antagonizes CGRP-receptor function and is dose-dependently effective in an in vivo target coverage model that exhibits translatability to humans.

Erenumab fully inhibited CGRP-stimulated cAMP production with an IC₅₀ of 2.3 nM in cell-based functional assays (human CGRP receptor) and was 5000-fold more selective for the CGRP receptor than other human calcitonin family receptors, including adrenomedullin, calcitonin, and amylin receptors.

Drugs in Clinical Pipeline: LY3041658 | Treatment of Skin Diseases | Monoclonal Antibody | Chemokine (CXC) Antagonist

LY3041658 is (expected to be a) monoclonal antibody that targets and specifically bind seven human ELR+ CXC chemokines. Such antibodies are useful for treating various inflammatory/autoimmune diseases, such as inflammatory bowel disease (IBD), plaque psoriasis, and palmoplantar pustulosis; and cancer, such as renal cancer or ovarian cancer.

Alirocumab | Monoclonal Antibody | Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor | Management of High Cholesterol

Alirocumab is a fully human monoclonal antibody (IgG1) targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). It is developed as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with hyperlipidaemia, including hypercholesterolaemia and heterozygous familial hypercholesterolaemia (HeFH) [1, 2].

Alirocumab is a human monoclonal antibody of the IgG1 isotype. Chemically, it is made of two disulfide-linked human heavy chains, each disulfide-linked to a human light chain. It has an approximate molecular weight of 146 kDa. It is produced using Chinese hamster ovary cells transfected with recombinant DNA.

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: THR-317 I Monoclonal Antibody (mAbs) I Angiogenesis Inhibitors | Placenta Growth Factor (PIGF) Inhibitors | Eye Disorder Therapies

THR-317 (also known as TB-403; RO5323441; αPIGF) is a humanized recombinant immunoglobulin (Ig) G₁ monoclonal antibody directed to the receptor-binding site of placental growth factor (PlGF). Inhibition of angiogenesis as a therapeutic strategy in oncology has been validated by treatments that block VEGF or its receptors, vascular endothelial growth factor receptor (VEGFR-1, -2, -3). Several antiangiogenesis inhibitors targeting VEGF or its receptors have been approved, such as the monoclonal antibody bevacizumab and the tyrosine kinase inhibitors Sorafenib and Sunitinib [1, 2].