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QuickView for Nepafenac (compound)

Name: nepafenac
PubChem Compound ID: 151075
Molecular formula: C15H14N2O2
Molecular weight: 254.284 g/mol
78281-72-8; Benzeneacetamide, 2-amino-3-benzoyl-; Nevanac; Nepafenac; Nepafenac [USAN]; 2-Amino-3-benzoylbenzeneacetamide; AHR 9434; AL 6515
Name: nepafenac
Name (isomeric): DB06802
Drug Type: small molecule
Amfenac amide
Brand: Nevanac
Category: Anti-inflammatory Agents, Locally Applied, Prodrugs, Nonsteroidal Anti-inflammatory Agents (NSAIAs)
CAS number: 78281-72-8
Indication: For the treatment of pain and inflammation associated with cataract surgery.
Low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects 2 and 3 hours postdose, respectively, following bilateral topical ocular TID dosing of nepafenac ophthalmic suspension, 0.1%. The mean steady-state Cmax for nepafenac and for amfenac were 0.310 ± 0.104 ng/ml and 0.422 ± 0.121 ng/ml, respect...
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Mechanism of Action: Nepafenac is a prodrug. After penetrating the cornea, nepafenac undergoes rapid bioactivation to amfenac, which is a potent NSAID that uniformly inhibits the COX1 and COX2 activity.
Absorption: Nepafenac rapidly cross the cornea (6 times faster than diclofenac in vitro).
Protein binding: Amfenac has high affinity toward serum albumin proteins. In vitro, the percent bound to human albumin and human serum was 95.4% and 99.1% respectively.
Biotransformation: Nepafenac (prodrug) is deaminated to amfenac (active compound) in the ciliary body epithelium, retina, and choroid by intraocular hydrolases. Subsequently, amfenac undergoes extensive metabolism to more polar metabolites involving hydroxylation of the aromatic ring leading to glucuronide conjugate formation.
Route of elimination: After oral administration of 14C-nepafenac to healthy volunteers, urinary excretion was found to be the major route of radioactivity elimination, accounting for approximately 85% of the dose, while fecal excretion represented approximately 6% of the dose. Nepafenac (prodrug) and amfenac (active compound) were not quantifiable in the urine.
Toxicity: Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.