Ranibizumab Chemical Properties

form 

Liquid

color 

Colorless to light yellow

InChI

InChI=1S/C11H12N2O2/c1-8-7-12-11(14)13(8)9-3-5-10(15-2)6-4-9/h3-7H,1-2H3,(H,12,14)

InChIKey

NHUPEUMBGMETKD-UHFFFAOYSA-N

SMILES

C1(=O)NC=C(C)N1C1=CC=C(OC)C=C1

CAS DataBase Reference

347396-82-1

Ranibizumab Usage And Synthesis

Description

Ranibizumab is a recombinant, humanized, IgG1 monoclonal antibody fragment (Fab) that neutralizes all active forms of vascular endothelial growth factor A (VEGF-A), and it is indicated for the treatment of neovascular age-related macular degeneration (AMD). It consists of a nonbinding human sequence and a high-affinity binding epitope (Fab fragment) derived from the mouse. The full-length RhuMab VEGF (bevacizumab) was launched previously by Genentech for the treatment of colorectal cancer. Both the antibody fragment and the full-length antibody bind to and inhibit all active forms of VEGF-A and are derived from the same mouse monoclonal antibody. However, ranibizumab has been genetically engineered through a process of selective mutation to increase its affinity for binding and inhibiting the growth factor.

Originator

Genentech (US)

History

Ranibizumab, sold under the brand name Lucentis among others, is a monoclonal antibody fragment (Fab) created from the same parent mouse antibody as bevacizumab. It works by keeping new blood vessels from forming under the retina (a sensory membrane that lines the inside of the eye). In people with certain types of eye disorders, new blood vessels grow under the retina where they leak blood and fluid.
Ranibizumab was developed by Genentech and marketed by them in the United States, and elsewhere by Novartis, under the brand name Lucentis. Ranibizumab (Lucentis) was approved for medical use in the United States in June 2006, and in the European Union in January 2007.

Uses

Ranibizumab, a humanized antigen binding portion of a murine anti- VEGF monoclonal antibody with a mature high affinity for all VEGF isoforms, has been approved as an intravitreal treatment for neovascular AMD and is the first such treatment to improve visual acuity (VA) in neovascular AMD.
CRUISE is multicenter, randomized, double-masked, sham injectioncontrolled Phase III study of 392 participants designed to assess the efficiency and safety profile of ranimizumab for macular edema associated to CRVO. The month 6 result showed that 46.2% (61/132) of patients received 0.3 mg of ranimizumab and 47.7% (62/130) received 0.5 mg of ranimizumab had their vision improved by 15 letters or more compared to 16.9% (22/130) of patients receiving sham injections and mean gain was observed beginning at day seven with an 8.8 and 9.3 letter gain in the 0.3 mg and 0.5 mg study arms of ranimizumab, respectively, compared with 1.1 letters in the sham injection arm.

Uses

antiangiogenic monoclonal antibody macular degeneration therapy

brand name

Lucentis

in vivo

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