Faricimab

Chemical Information
Retinal vascular diseases (RVDs) such as diabetic macular edema (DME), age-related macular degeneration (AMD), and retinal vein occlusion (RVO) are typically caused by retinal ischemia and subsequent neovascularization (NV). Vascular endothelial growth factor A (VEGF-A) is a well-known mediator of retinal NV, and many currently approved RVD therapies such as [aflibercept] and [ranibizumab] solely target VEGF-A. However, another set of factors, the Tie/Ang axis, comprising the transmembrane Tie-2 receptor and its soluble ligands Ang-1 and Ang-2, has been shown to play critical roles in mediating VEGF-A-induced NV. Faricimab is an IgG1-derived bispecific antibody capable of simultaneously binding to and depleting VEGF-A and Ang-2, which has been developed to improve therapeutic efficacy, especially in patients that respond poorly to anti-VEGF-A monotherapy. Faricimab was approved by the FDA on January 28, 2022, and is currently marketed under the trademark VABYSMO by Genentech, Inc. It received subsequent approval for the same indications in Canada in May 2022. In July 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended faricimab be granted marketing authorization for the treatment of neovascular age-related macular degeneration and diabetic macular edema.
| CAS Number | 1607793-29-2 |
| PubChem CID | 91827367 |
| IUPAC Name | [6-chloro-1-[2-(dimethylamino)ethyl]-2,3-dihydroindol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone |
| Molecular Formula | C25H30ClN3O2 |
| Molecular Weight | 440.0 |
| XLogP | 3.2 |
| Topological Polar Surface Area | 36 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 31 |
| Formal Charge | 0 |
| Complexity | 651 |
| Property | Value |
|---|---|
| Molecular Weight | 440.0 |
| XLogP3 | 3.2 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Exact Mass | 439.2026549 |
| Monoisotopic Mass | 439.2026549 |
| Topological Polar Surface Area | 36 Ų |
| Heavy Atom Count | 31 |
| Formal Charge | 0 |
| Complexity | 651 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
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